PGF
gene geneOn this page
Also known as PlGF-2SHGC-10760D12S1900PIGFPLGF
Summary
PGF (placental growth factor, HGNC:8893) is a protein-coding gene on chromosome 14q24.3, encoding Placenta growth factor (P49763). Growth factor active in angiogenesis and endothelial cell growth, stimulating their proliferation and migration.
Enables growth factor activity. Involved in positive regulation of cell population proliferation. Predicted to be located in extracellular region. Predicted to be active in extracellular space. Implicated in several diseases, including brain ischemia; diabetic neuropathy; glioblastoma; myocardial infarction; and pancreatic endocrine carcinoma. Biomarker of several diseases, including artery disease (multiple); autoimmune disease of musculoskeletal system (multiple); epilepsy (multiple); limited scleroderma; and pancreatic endocrine carcinoma.
Source: NCBI Gene 5228 — RefSeq curated summary.
At a glance
- GWAS associations: 6
- Clinical variants (ClinVar): 38 total
- Druggable target: yes
- MANE Select transcript:
NM_002632
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:8893 |
| Approved symbol | PGF |
| Name | placental growth factor |
| Location | 14q24.3 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | PlGF-2, SHGC-10760, D12S1900, PIGF, PLGF, PlGF |
| Ensembl gene | ENSG00000119630 |
| Ensembl biotype | protein_coding |
| OMIM | 601121 |
| Entrez | 5228 |
Gene structure
Transcript identifiers
Ensembl transcripts: 11 — 7 protein_coding, 4 retained_intron
ENST00000238607, ENST00000405431, ENST00000553716, ENST00000555234, ENST00000555253, ENST00000555567, ENST00000556939, ENST00000557748, ENST00000863243, ENST00000863244, ENST00000965660
RefSeq mRNA: 3 — MANE Select: NM_002632
NM_001207012, NM_001293643, NM_002632
CCDS: CCDS55932, CCDS73664, CCDS9835
Canonical transcript exons
ENST00000555567 — 7 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001195853 | 74946213 | 74946275 |
| ENSE00002468846 | 74955168 | 74955597 |
| ENSE00002473068 | 74941834 | 74942733 |
| ENSE00003482136 | 74949357 | 74949553 |
| ENSE00003526402 | 74946379 | 74946408 |
| ENSE00003607518 | 74953904 | 74953946 |
| ENSE00003664306 | 74948507 | 74948583 |
Expression profiles
Bgee: expression breadth ubiquitous, 287 present calls, max score 99.60.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 8.3667 / max 403.8345, expressed in 985 samples.
FANTOM5 promoters (1 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 144092 | 8.3667 | 985 |
Top tissues by expression
293 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| renal medulla | UBERON:0000362 | 99.60 | gold quality |
| cardia of stomach | UBERON:0001162 | 99.49 | gold quality |
| pylorus | UBERON:0001166 | 99.41 | gold quality |
| nipple | UBERON:0002030 | 99.38 | gold quality |
| ventral tegmental area | UBERON:0002691 | 99.35 | gold quality |
| trigeminal ganglion | UBERON:0001675 | 99.27 | gold quality |
| inferior vagus X ganglion | UBERON:0005363 | 99.26 | gold quality |
| lateral globus pallidus | UBERON:0002476 | 99.25 | gold quality |
| superior surface of tongue | UBERON:0007371 | 99.25 | gold quality |
| substantia nigra pars reticulata | UBERON:0001966 | 99.24 | gold quality |
| subthalamic nucleus | UBERON:0001906 | 99.22 | gold quality |
| superior vestibular nucleus | UBERON:0007227 | 99.20 | gold quality |
| superficial temporal artery | UBERON:0001614 | 99.19 | gold quality |
| medulla oblongata | UBERON:0001896 | 99.19 | gold quality |
| substantia nigra pars compacta | UBERON:0001965 | 99.13 | gold quality |
| lateral nuclear group of thalamus | UBERON:0002736 | 99.09 | gold quality |
| endothelial cell | CL:0000115 | 99.00 | gold quality |
| mucosa of paranasal sinus | UBERON:0005030 | 98.99 | gold quality |
| pericardium | UBERON:0002407 | 98.98 | gold quality |
| synovial joint | UBERON:0002217 | 98.94 | gold quality |
| buccal mucosa cell | CL:0002336 | 98.91 | gold quality |
| dorsal motor nucleus of vagus nerve | UBERON:0002870 | 98.90 | gold quality |
| penis | UBERON:0000989 | 98.87 | gold quality |
| sperm | CL:0000019 | 98.85 | gold quality |
| urethra | UBERON:0000057 | 98.82 | gold quality |
| male germ cell | CL:0000015 | 98.79 | gold quality |
| saphenous vein | UBERON:0007318 | 98.76 | gold quality |
| inferior olivary complex | UBERON:0002127 | 98.75 | gold quality |
| pharyngeal mucosa | UBERON:0000355 | 98.73 | gold quality |
| epithelium of nasopharynx | UBERON:0001951 | 98.68 | gold quality |
Single-cell (SCXA)
Detected in 6 experiment(s), a significant marker in 6.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-10018 | yes | 5469.95 |
| E-MTAB-10662 | yes | 2802.17 |
| E-MTAB-6701 | yes | 1193.67 |
| E-HCAD-5 | yes | 325.75 |
| E-MTAB-6678 | yes | 16.64 |
| E-ANND-3 | no | 0.00 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): DLX3, EGR1, FOXD1, FOXG1, GCM1, HIF1A, MTF1, NR3C2, RELA, STAT3
miRNA regulators (miRDB)
52 targeting PGF, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-6833-3P | 100.00 | 70.63 | 3197 |
| HSA-MIR-4768-5P | 100.00 | 69.49 | 2861 |
| HSA-MIR-6873-3P | 100.00 | 71.42 | 2626 |
| HSA-MIR-574-5P | 100.00 | 66.01 | 989 |
| HSA-MIR-34A-5P | 99.99 | 71.21 | 1784 |
| HSA-MIR-449A | 99.99 | 71.05 | 1776 |
| HSA-MIR-3692-3P | 99.98 | 70.27 | 2139 |
| HSA-MIR-34C-5P | 99.97 | 70.45 | 1577 |
| HSA-MIR-449B-5P | 99.97 | 70.26 | 1580 |
| HSA-MIR-6845-3P | 99.94 | 66.88 | 1439 |
| HSA-MIR-515-5P | 99.92 | 69.82 | 2343 |
| HSA-MIR-519E-5P | 99.92 | 69.62 | 2358 |
| HSA-MIR-605-3P | 99.88 | 69.22 | 1833 |
| HSA-MIR-3121-3P | 99.82 | 71.96 | 3630 |
| HSA-MIR-6794-5P | 99.76 | 66.38 | 1048 |
| HSA-MIR-548AU-3P | 99.70 | 68.22 | 1373 |
| HSA-MIR-4530 | 99.69 | 66.47 | 1509 |
| HSA-MIR-6887-3P | 99.66 | 67.83 | 1778 |
| HSA-MIR-5197-5P | 99.64 | 69.08 | 1494 |
| HSA-MIR-6126 | 99.62 | 68.09 | 996 |
| HSA-MIR-12123 | 99.52 | 71.79 | 2990 |
| HSA-MIR-3123 | 99.47 | 67.15 | 2693 |
| HSA-MIR-103A-1-5P | 99.39 | 67.78 | 1545 |
| HSA-MIR-103A-2-5P | 99.39 | 67.72 | 1577 |
| HSA-MIR-3064-5P | 99.26 | 66.13 | 1497 |
| HSA-MIR-3085-3P | 99.26 | 66.16 | 1490 |
| HSA-MIR-6504-5P | 99.26 | 65.95 | 1487 |
| HSA-MIR-6837-5P | 99.25 | 65.47 | 1632 |
| HSA-MIR-4685-5P | 99.25 | 65.99 | 1563 |
| HSA-MIR-4291 | 99.20 | 68.88 | 2969 |
Literature-anchored findings (GeneRIF, showing 40)
- Maternal serum placenta growth factor concentration was elevated in Down syndrome pregnancies (PMID:11810642)
- Effect of placenta growth factor-1 on proliferation and release of nitric oxide, cyclic AMP and cyclic GMP in human epithelial cells expressing the FLT-1 receptor (PMID:11811792)
- Placental growth factor promotes recruitment of VEGFR1(+) hematopoietic stem cells from a quiescent to a proliferative bone marrow microenvironment, favoring differentiation, mobilization and reconstitution of hematopoiesis. (PMID:12091880)
- increased inflammatory response, associated with more pronounced vascular enlargement, edema, and inflammatory cell infiltration in transgenic mice (PMID:12393422)
- Vitreous levels are altered in patients with proliferative diabetic retinopathy (PMID:12453985)
- This protein and its receptor VEGR-1 are novel therapeutic targets for angiogenic disorders (REVIEW) (PMID:12543719)
- placenta growth factor-to-human chorionic gonadotropin ratios were increased significantly in patients with persistent gestational trophoblastic disease (PMID:12548207)
- postulate that decreased placental growth factor production results in abnormalities of placental angiogenesis through direct and indirect effects on other vasculotropic growth factors (PMID:12548214)
- findings point to a role for PlGF in rapid restoration of tumor blood supply after treatment and thus, to enhanced likelihood of tumor regrowth (PMID:12673673)
- Placenta growth factor contributes to the inflammation observed in sickle cell disease and increases the incidence of vaso-occlusive events. (PMID:12714517)
- alteration of PlGF-2 and PlGFR-1 mRNA expressions in the placenta are related to the pathogenesis of pregnancy induced hypertension (PMID:12808329)
- paracrine role for mesenchynmal stem cell-derived PlGF in the angiogenesis and hematopoiesis that accompany BMP-2-induced bone formation. (PMID:13678785)
- Ang2, PIGF and VEGF-C play a role in promote endothelial survival and vascular remodeling by human cytotrophoblast. (PMID:14568550)
- findings suggest that production of placental growth factor is sensitive to the cyclic changes in ovarian steroids and may contribute to the pathogenesis of endometriosis (PMID:14645176)
- crystal structure of placental growth factor in complex with domain 2 of vascular endothelial growth factor receptor-1 (PMID:14684734)
- VEGF and PlGF induced expression of both full-length FosB mRNA and an alternatively spliced variant. (PMID:14741347)
- vascular endothelial growth factor and placental growth factor-2 effects in dorsal root ganglion neurons are mediated via neuropilin-1 and cyclooxygenase-derived prostanoid production (PMID:15126502)
- a basis for understanding molecular recognition between PlGF-1 and VEGFR1 (PMID:15272021)
- effect of VEGFA and PLGF on gene expression profiles obtained for HUVEC, dose effect, and variability between cells obtained from different individuals (PMID:15516835)
- vascular endothelial growth factor induced the production of PlGF protein (PMID:15710418)
- In contrast to preeclampsia, sFlt-1 does not appear to contribute substantially to decreased circulating free PlGF in small for gestational age pregnancies in the absence of a maternal syndrome (PMID:15886253)
- Altered expression of Fas, FasL and PGF in trophoblasts of placenta influence the pathogenesis of pre-eclampsia. (PMID:15938782)
- These findings are consistent with the idea that the chemotactic effect of VEGF-A on mesenchymal progenitor cells (MPC) is mediated via VEGFR-1, and that VEGF-A and PlGF-1, have a functional role for recruitment of osteoprogenitor cells. (PMID:16005848)
- growth stimulation of ALL cells by PlGF was confirmed by the increase of S phase cells; the growth promoting effect of PlGF was cancelled by simultaneous addition of VEGFR1/Fc), but was not cancelled by VEGFR2/Fc (PMID:16146532)
- Correlation of placenta growth factor expression and placental perfusion suggests that placenta growth factor may contribute to assuring adequate vascular development/function of the placenta early in gestation. (PMID:16635470)
- Therapeutically administered human PIGF-1 demonstrates a desirable biological activity for promoting the growth of functionally relevant vasculature in mice. (PMID:16702473)
- Overexpression of VEGF but not PIGF exacerbated the lipopolysaccharide-mediated toxic effects, supporting a pathophysiological role for VEGF in mediating the sepsis phenotype. (PMID:16702604)
- Neither the hyperpermeability in response to simultaneous stimulation of VEGFR-1 and VEGFR-2 nor VEGFR-1-mediated severe inflammation was associated with VEGF-E(NZ7)/PIGF-induced angiogenesis. (PMID:16794222)
- iodide at high concentration decreases the expression of the angiogenic factors VEGF-A, VEGF-B, and PG (PMID:16839256)
- The strong positivity for both PlGF and VEGF observed, implies that the t(10;14)(p13;q24) most likely involves PlGF, which may be one of the genes driving oncogenesis in these tumors. (PMID:16843105)
- The expression and localization of placenta growth factor (PlGF) within middle ear cholesteatoma were defined (PMID:16864484)
- These data suggest that mechanical stretch of bronchial airway epithelial cells induces iNOS expression and induces PIGF release in an erk1/2 activation-dependent manner. (PMID:17028267)
- placental growth factor-expression within human atherosclerotic lesions is associated with plaque inflammation and microvascular density (PMID:17157858)
- May be a potential regulation target for the control of diabetic retinal and macular oedema. (PMID:17187248)
- The plasma PIGF level in coronary artery disease group was significantly higher than that in the control group (PMID:17593833)
- PGF and VEGFR1 may have an important role in the pathogenesis of the neovascular response in cirrhosis. (PMID:17696935)
- Promoter is methylated, and methylation may be one of the mechanisms that contributes to the low PGF expression level in human lung and colorectal tumor tissues and cell lines. (PMID:17704140)
- Preeclampsia trophoblast cells produce more sEng, sFlt-1, and PlGF than normal TCs. Lowered oxygen conditions promote sEng and sFlt-1, but reduce PlGF, productions by PE TCs. (PMID:17956952)
- anlalysis of levels of circulating PIGF, SDF-1 and sVCAM-1 in patients with systemic lupus erythematosus (PMID:17964973)
- sFlt-1 and PlGF and their ratio relative to one another may play a role in the development of preeclampsia (PMID:17982238)
Cross-species orthologs
4 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | pgfb | ENSDARG00000076767 |
| danio_rerio | ENSDARG00000115359 | |
| mus_musculus | Pgf | ENSMUSG00000004791 |
| rattus_norvegicus | Pgf | ENSRNOG00000005650 |
Paralogs (4): VEGFA (ENSG00000112715), VEGFC (ENSG00000150630), VEGFD (ENSG00000165197), VEGFB (ENSG00000173511)
Protein
Protein identifiers
Placenta growth factor — P49763 (reviewed: P49763)
All UniProt accessions (3): P49763, G3XA84, Q53XY6
UniProt curated annotations — full annotation on UniProt →
Function. Growth factor active in angiogenesis and endothelial cell growth, stimulating their proliferation and migration. It binds to the receptor FLT1/VEGFR-1. Isoform PlGF-2 binds NRP1/neuropilin-1 and NRP2/neuropilin-2 in a heparin-dependent manner. Also promotes cell tumor growth.
Subunit / interactions. Antiparallel homodimer; disulfide-linked. Also found as heterodimer with VEGFA/VEGF. Isoform PlGF-3 is found both as homodimer and as monomer.
Subcellular location. Secreted.
Tissue specificity. While the three isoforms are present in most placental tissues, PlGF-2 is specific to early (8 week) placenta and only PlGF-1 is found in the colon and mammary carcinomas.
Post-translational modifications. N-glycosylated.
Domain organisation. Isoform PlGF-2 contains a basic insert which acts as a cell retention signal.
Similarity. Belongs to the PDGF/VEGF growth factor family.
Isoforms (4)
| UniProt ID | Names | Canonical? |
|---|---|---|
| P49763-1 | PlGF-3, PlGF-203 | yes |
| P49763-2 | PlGF-1, PlGF-131 | |
| P49763-3 | PlGF-2, PlGF-152 | |
| P49763-4 | PlGF-4, PlGF-224 |
RefSeq proteins (3): NP_001193941, NP_001280572, NP_002623* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000072 | PDGF/VEGF_dom | Domain |
| IPR023581 | PD_growth_factor_CS | Conserved_site |
| IPR029034 | Cystine-knot_cytokine | Homologous_superfamily |
| IPR050507 | PDGF/VEGF_growth_factor | Family |
Pfam: PF00341
UniProt features (24 total): strand 6, disulfide bond 5, splice variant 2, helix 2, region of interest 2, compositionally biased region 2, glycosylation site 2, signal peptide 1, chain 1, sequence conflict 1
Structure
Experimental structures (PDB)
2 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 1FZV | X-RAY DIFFRACTION | 2 |
| 1RV6 | X-RAY DIFFRACTION | 2.45 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P49763-F1 | 71.00 | 0.38 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Disulfide bonds (5): 83–128, 86, 87–130, 52–94, 77
Glycosylation sites (2): 33, 101
Function
Pathways and Gene Ontology
Reactome pathways
2 pathways
| ID | Pathway |
|---|---|
| R-HSA-194313 | VEGF ligand-receptor interactions |
| R-HSA-195399 | VEGF binds to VEGFR leading to receptor dimerization |
MSigDB gene sets: 534 (showing top):
RNGTGGGC_UNKNOWN, HORIUCHI_WTAP_TARGETS_DN, GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, BUYTAERT_PHOTODYNAMIC_THERAPY_STRESS_DN, GOBP_PHOSPHATIDYLINOSITOL_METABOLIC_PROCESS, GOBP_VASCULAR_ENDOTHELIAL_GROWTH_FACTOR_SIGNALING_PATHWAY, PAX4_01, GOBP_MYELOID_LEUKOCYTE_MIGRATION, HARRIS_HYPOXIA, MORF_MSH3, GOBP_CELL_CHEMOTAXIS, GOBP_GLYCOLIPID_BIOSYNTHETIC_PROCESS, PEREZ_TP63_TARGETS, REACTOME_SYNTHESIS_OF_GLYCOSYLPHOSPHATIDYLINOSITOL_GPI, MORF_BRCA1
GO Biological Process (13): response to hypoxia (GO:0001666), sprouting angiogenesis (GO:0002040), signal transduction (GO:0007165), cell-cell signaling (GO:0007267), positive regulation of cell population proliferation (GO:0008284), cell differentiation (GO:0030154), vascular endothelial growth factor signaling pathway (GO:0038084), vascular endothelial growth factor receptor signaling pathway (GO:0048010), induction of positive chemotaxis (GO:0050930), positive regulation of cell division (GO:0051781), positive regulation of mast cell chemotaxis (GO:0060754), angiogenesis (GO:0001525), positive chemotaxis (GO:0050918)
GO Molecular Function (6): vascular endothelial growth factor receptor binding (GO:0005172), growth factor activity (GO:0008083), heparin binding (GO:0008201), chemoattractant activity (GO:0042056), protein binding (GO:0005515), receptor ligand activity (GO:0048018)
GO Cellular Component (3): extracellular region (GO:0005576), obsolete extracellular space (GO:0005615), membrane (GO:0016020)
Reactome top-level categories
Rollup of top-2 pathways:
| Category | Pathways |
|---|---|
| Signaling by VEGF | 1 |
| VEGF ligand-receptor interactions | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cell communication | 2 |
| signaling | 2 |
| positive regulation of cellular process | 2 |
| cell surface receptor protein tyrosine kinase signaling pathway | 2 |
| receptor ligand activity | 2 |
| cellular anatomical structure | 2 |
| response to stress | 1 |
| response to decreased oxygen levels | 1 |
| angiogenesis | 1 |
| cellular process | 1 |
| regulation of cellular process | 1 |
| cellular response to stimulus | 1 |
| cell population proliferation | 1 |
| regulation of cell population proliferation | 1 |
| cellular developmental process | 1 |
| cellular response to vascular endothelial growth factor stimulus | 1 |
| positive regulation of positive chemotaxis | 1 |
| cell division | 1 |
| regulation of cell division | 1 |
| mast cell chemotaxis | 1 |
| positive regulation of leukocyte chemotaxis | 1 |
| regulation of mast cell chemotaxis | 1 |
| blood vessel morphogenesis | 1 |
| anatomical structure formation involved in morphogenesis | 1 |
| chemotaxis | 1 |
| cytokine receptor binding | 1 |
| growth factor receptor binding | 1 |
| glycosaminoglycan binding | 1 |
| sulfur compound binding | 1 |
| positive chemotaxis | 1 |
| binding | 1 |
| signaling receptor binding | 1 |
| signal transduction | 1 |
| signaling receptor activator activity | 1 |
Protein interactions and networks
STRING
1372 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| PGF | FLT1 | P16057 | 999 |
| PGF | KDR | P35968 | 998 |
| PGF | FLT4 | P35916 | 997 |
| PGF | NRP1 | O14786 | 997 |
| PGF | NRP2 | O60462 | 968 |
| PGF | FN1 | P02751 | 942 |
| PGF | VEGFB | P49765 | 888 |
| PGF | ENG | P17813 | 884 |
| PGF | VTN | P01141 | 880 |
| PGF | PDGFC | Q9NRA1 | 876 |
| PGF | SPP1 | P10451 | 850 |
| PGF | ANGPT2 | O15123 | 822 |
| PGF | HGF | P14210 | 800 |
| PGF | PAPPA | Q13219 | 798 |
| PGF | TEK | Q02763 | 764 |
IntAct
4 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| FLT1 | VEGFA | psi-mi:“MI:0915”(physical association) | 0.820 |
| FLT1 | PGF | psi-mi:“MI:0407”(direct interaction) | 0.610 |
| VEGFA | PGF | psi-mi:“MI:2364”(proximity) | 0.270 |
BioGRID (9): VEGFA (Co-localization), PGF (Affinity Capture-MS), VEGFA (Co-purification), PGF (Co-purification), PGF (Reconstituted Complex), PGF (Affinity Capture-Western), PGF (Reconstituted Complex), PGF (Affinity Capture-RNA), PGF (Affinity Capture-RNA)
ESM2 similar proteins: A2APT9, A6NKQ9, A6QNY1, B0BN44, B6VH76, B6VH77, B6VH79, F8WCM5, O00220, O75298, P0C2N6, P0CG36, P0CG37, P22618, P48778, P49763, P97766, Q1L6U9, Q29100, Q3U4N7, Q4R6Y5, Q4TUC0, Q5DRQ5, Q5F267, Q5HZW5, Q5RA67, Q63572, Q7TQH7, Q7Z3H0, Q80W87, Q866Y3, Q86VZ4, Q8BLH5, Q8C310, Q8CB67, Q8IXA5, Q8K1T6, Q8QZY4, Q8R2S1, Q8TDX9
Diamond homologs: B0VXV3, B0VXV4, C0HM96, C0K3N1, C0K3N2, C0K3N3, C0K3N4, C0K3N5, O35251, O35485, O35757, O43915, O73682, P0DL42, P0DW97, P0DW98, P15691, P15692, P16612, P26617, P49151, P49763, P49764, P49765, P49766, P49767, P50412, P52584, P52585, P67860, P67861, P67862, P67863, P67964, P67965, P82475, P83906, P83942, P97946, P97953
SIGNOR signaling
1 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| Aflibercept | “down-regulates activity” | PGF | “chemical inhibition” |
Disease & clinical
Clinical variants and AI predictions
ClinVar
38 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 32 |
| Likely benign | 1 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
2233 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 14:74946374:CTTA:C | donor_loss | 1.0000 |
| 14:74946375:TTAC:T | donor_loss | 1.0000 |
| 14:74946376:TACC:T | donor_loss | 1.0000 |
| 14:74946377:A:AC | donor_gain | 1.0000 |
| 14:74946377:ACCTT:A | donor_loss | 1.0000 |
| 14:74946378:C:CC | donor_gain | 1.0000 |
| 14:74946378:CCTTT:C | donor_gain | 1.0000 |
| 14:74946404:GAGGC:G | acceptor_gain | 1.0000 |
| 14:74946405:AGGC:A | acceptor_gain | 1.0000 |
| 14:74946406:GGC:G | acceptor_gain | 1.0000 |
| 14:74946407:GC:G | acceptor_gain | 1.0000 |
| 14:74946408:CC:C | acceptor_gain | 1.0000 |
| 14:74946409:C:CC | acceptor_gain | 1.0000 |
| 14:74946418:C:CT | acceptor_gain | 1.0000 |
| 14:74946419:A:T | acceptor_gain | 1.0000 |
| 14:74946422:C:CT | acceptor_gain | 1.0000 |
| 14:74948502:CCTA:C | donor_loss | 1.0000 |
| 14:74948503:CTA:C | donor_loss | 1.0000 |
| 14:74948505:A:AC | donor_gain | 1.0000 |
| 14:74948505:ACC:A | donor_loss | 1.0000 |
| 14:74948506:C:CA | donor_loss | 1.0000 |
| 14:74948506:C:CC | donor_gain | 1.0000 |
| 14:74948506:CCGG:C | donor_gain | 1.0000 |
| 14:74948584:C:CC | acceptor_gain | 1.0000 |
| 14:74949355:A:AC | donor_gain | 1.0000 |
| 14:74949356:C:CA | donor_loss | 1.0000 |
| 14:74949356:C:CC | donor_gain | 1.0000 |
| 14:74949356:CCTG:C | donor_gain | 1.0000 |
| 14:74949549:TACCA:T | acceptor_gain | 1.0000 |
| 14:74949550:ACCA:A | acceptor_gain | 1.0000 |
AlphaMissense
1093 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 14:74949454:A:C | F73C | 0.996 |
| 14:74949544:A:C | F43C | 0.996 |
| 14:74948533:G:C | F122L | 0.994 |
| 14:74948533:G:T | F122L | 0.994 |
| 14:74948534:A:C | F122C | 0.994 |
| 14:74948535:A:G | F122L | 0.994 |
| 14:74949448:G:T | P75Q | 0.994 |
| 14:74949419:C:A | G85C | 0.993 |
| 14:74949531:C:A | W47C | 0.993 |
| 14:74949531:C:G | W47C | 0.993 |
| 14:74948534:A:G | F122S | 0.992 |
| 14:74949522:G:C | S50R | 0.992 |
| 14:74949522:G:T | S50R | 0.992 |
| 14:74949524:T:G | S50R | 0.992 |
| 14:74949439:A:T | V78D | 0.991 |
| 14:74949449:G:A | P75S | 0.991 |
| 14:74949517:C:G | C52S | 0.991 |
| 14:74949518:A:T | C52S | 0.991 |
| 14:74949391:C:G | C94S | 0.990 |
| 14:74949392:A:T | C94S | 0.990 |
| 14:74949424:C:G | C83S | 0.990 |
| 14:74949425:A:G | C83R | 0.990 |
| 14:74949425:A:T | C83S | 0.990 |
| 14:74949517:C:T | C52Y | 0.990 |
| 14:74949391:C:T | C94Y | 0.989 |
| 14:74949453:G:C | F73L | 0.989 |
| 14:74949453:G:T | F73L | 0.989 |
| 14:74949454:A:G | F73S | 0.989 |
| 14:74949455:A:G | F73L | 0.989 |
| 14:74949516:G:C | C52W | 0.988 |
dbSNP variants (sampled 300 via entrez): RS1000086247 (14:74943547 T>C), RS1000195446 (14:74950851 T>TG), RS1000200855 (14:74950606 A>G), RS1000209830 (14:74951336 G>T), RS1000255903 (14:74948083 C>G,T), RS1000346229 (14:74953222 T>C), RS1000347195 (14:74945519 G>A,T), RS1000459970 (14:74942489 T>G), RS1000517901 (14:74946103 A>G), RS1000688734 (14:74944394 G>A), RS1000801233 (14:74952038 G>A), RS1000883765 (14:74953413 G>C), RS1001256920 (14:74949033 T>C), RS1001486788 (14:74954975 C>A), RS1001548108 (14:74955654 G>A)
Disease associations
OMIM: gene MIM:601121 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
6 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST005237_3 | Mood instability | 1.000000e-06 |
| GCST005238_3 | Mood instability | 3.000000e-09 |
| GCST006585_2645 | Blood protein levels | 4.000000e-07 |
| GCST009731_77 | Blood protein levels in cardiovascular risk | 3.000000e-09 |
| GCST010002_156 | Refractive error | 7.000000e-25 |
| GCST90011900_113 | Serum alkaline phosphatase levels | 4.000000e-15 |
EFO canonical traits (3, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0008475 | mood instability measurement |
| EFO:0010626 | placenta growth factor measurement |
| EFO:0004533 | alkaline phosphatase measurement |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL1697671 (SINGLE PROTEIN)
PharmGKB: 1 entry (VIP=true, CPIC=false)
ChEMBL bioactivities
36 potent at pChembl≥5 of 40 total, top 36 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 10.00 | Kd | 0.1 | nM | CHEMBL1689483 |
| 9.52 | Kd | 0.3 | nM | CHEMBL1689479 |
| 9.52 | Kd | 0.3 | nM | CHEMBL1689481 |
| 9.40 | IC50 | 0.4 | nM | CHEMBL1689483 |
| 9.00 | IC50 | 1 | nM | CHEMBL1689481 |
| 8.70 | IC50 | 2 | nM | CHEMBL1689460 |
| 8.52 | IC50 | 3 | nM | CHEMBL1689482 |
| 8.40 | IC50 | 4 | nM | CHEMBL1689463 |
| 8.40 | Kd | 4 | nM | CHEMBL1689460 |
| 8.40 | Kd | 4 | nM | CHEMBL1689466 |
| 8.30 | Kd | 5 | nM | CHEMBL1689463 |
| 8.30 | Kd | 5 | nM | CHEMBL1689465 |
| 8.22 | Kd | 6 | nM | CHEMBL1689473 |
| 8.10 | Kd | 8 | nM | CHEMBL1689464 |
| 8.10 | Kd | 8 | nM | CHEMBL1689482 |
| 8.09 | Kd | 8.2 | nM | AMENTOFLAVONE |
| 8.05 | Kd | 9 | nM | CHEMBL1689470 |
| 8.05 | Kd | 9 | nM | CHEMBL1689483 |
| 7.96 | Kd | 11 | nM | CHEMBL2335722 |
| 7.64 | Kd | 23 | nM | GERANIN B |
| 7.00 | Kd | 100 | nM | CHEMBL1689460 |
| 6.82 | IC50 | 150 | nM | CHEMBL1689460 |
| 6.70 | Kd | 200 | nM | CHEMBL1689461 |
| 6.41 | Kd | 394 | nM | PROANTHOCYANIDIN A1 |
| 6.00 | IC50 | 1000 | nM | CHEMBL1689461 |
| 6.00 | Kd | 1000 | nM | CHEMBL1689456 |
| 6.00 | IC50 | 1000 | nM | CHEMBL1689456 |
| 6.00 | IC50 | 1000 | nM | CHEMBL1689457 |
| 6.00 | IC50 | 1000 | nM | CHEMBL1689458 |
| 6.00 | IC50 | 1000 | nM | CHEMBL1689459 |
| 5.30 | IC50 | 5000 | nM | CHEMBL1689452 |
| 5.30 | IC50 | 5000 | nM | CHEMBL1689455 |
| 5.22 | IC50 | 6000 | nM | CHEMBL1689454 |
| 5.05 | IC50 | 9000 | nM | CHEMBL1689447 |
| 5.05 | IC50 | 9000 | nM | CHEMBL1689448 |
| 5.05 | IC50 | 9000 | nM | CHEMBL1689450 |
PubChem BioAssay actives
36 with measured affinity, of 56 total; 26 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| (4S)-5-[[(2S)-1-[[(4R,7S,13S,16S,19S,22S,25S,28R)-4-[[(2R,3R)-1-[[(2S)-6-acetamido-1-[(1-amino-2-methyl-1-oxopropan-2-yl)amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]carbamoyl]-19-[(2S)-butan-2-yl]-22-[(4-hydroxyphenyl)methyl]-7,25-bis(1H-imidazol-5-ylmethyl)-10,10-dimethyl-13-(2-methylpropyl)-6,9,12,15,18,21,24,27-octaoxo-16-[4-[[2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetyl]amino]butyl]-1,2-dithia-5,8,11,14,17,20,23,26-octazacyclononacos-28-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamidopropanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]propanoyl]amino]-3-phenylpropanoyl]-methylamino]-5-oxopentanoic acid | 587577: Binding affinity to human PlGF-1 | kd | 0.0001 | uM |
| (4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-carboxypropanoyl]amino]propanoyl]amino]propanoyl]amino]-3-phenylpropanoyl]amino]-5-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2R,3R)-1-[[(2R)-1-[[(2R)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]carbamoyl]-9-[(2S)-butan-2-yl]-12-[(4-hydroxyphenyl)methyl]-15,26-bis(1H-imidazol-5-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-6-[4-[[2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetyl]amino]butyl]-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-oxopentanoic acid | 587577: Binding affinity to human PlGF-1 | kd | 0.0003 | uM |
| (4S)-4-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]-5-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]carbamoyl]-9-[(2S)-butan-2-yl]-12-[(4-hydroxyphenyl)methyl]-15,26-bis(1H-imidazol-5-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-6-[4-[[2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetyl]amino]butyl]-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-oxopentanoic acid | 587577: Binding affinity to human PlGF-1 | kd | 0.0003 | uM |
| (3S)-3-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]-4-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-oxo-1-[[2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetyl]amino]hexan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]-15-(4-aminobutyl)-6-[(1R)-1-hydroxyethyl]-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | 587565: Inhibition of human PlGF-1-VEGFR-1 interaction by ELISA | ic50 | 0.0020 | uM |
| (4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamidopropanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]propanoyl]amino]-3-phenylpropanoyl]-methylamino]-5-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2R,3R)-1-[[(2R)-1-[[(2R)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]carbamoyl]-9-[(2S)-butan-2-yl]-12-[(4-hydroxyphenyl)methyl]-15,26-bis(1H-imidazol-5-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-6-[4-[[2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetyl]amino]butyl]-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-oxopentanoic acid | 587565: Inhibition of human PlGF-1-VEGFR-1 interaction by ELISA | ic50 | 0.0030 | uM |
| (3S)-3-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]-4-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-6-[[2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetyl]amino]hexan-2-yl]carbamoyl]-15-(2-amino-2-oxoethyl)-6-[(1R)-1-hydroxyethyl]-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | 587577: Binding affinity to human PlGF-1 | kd | 0.0040 | uM |
| (3S)-4-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-6-acetamido-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1-oxo-6-[[2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetyl]amino]hexan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]-15-(2-amino-2-oxoethyl)-6-[(1R)-1-hydroxyethyl]-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]-4-oxobutanoic acid | 587565: Inhibition of human PlGF-1-VEGFR-1 interaction by ELISA | ic50 | 0.0040 | uM |
| (3S)-4-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-6-acetamido-1-[[(2S)-1-[[(2S)-6-amino-1-oxo-1-[[2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetyl]amino]hexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]-15-(2-amino-2-oxoethyl)-6-[(1R)-1-hydroxyethyl]-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]-4-oxobutanoic acid | 587577: Binding affinity to human PlGF-1 | kd | 0.0050 | uM |
| (3S)-4-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-6-acetamido-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]-6-[(1R)-1-hydroxyethyl]-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-15-[4-[[2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetyl]amino]butyl]-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]-4-oxobutanoic acid | 587577: Binding affinity to human PlGF-1 | kd | 0.0060 | uM |
| (3S)-4-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-6-acetamido-1-[[(2S)-1-[[(2S)-6-amino-1-oxo-1-[[2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetyl]amino]hexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]-15-(4-acetamidobutyl)-6-[(1R)-1-hydroxyethyl]-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]-4-oxobutanoic acid | 587577: Binding affinity to human PlGF-1 | kd | 0.0080 | uM |
| 8-[5-(5,7-dihydroxy-4-oxochromen-2-yl)-2-hydroxyphenyl]-5,7-dihydroxy-2-(4-hydroxyphenyl)chromen-4-one | 730066: Binding affinity to recombinant PIGF1 (unknown origin) measured for 60 seconds by surface plasmon resonance assay | kd | 0.0082 | uM |
| (3S)-4-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-6-acetamido-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]-15-(2-amino-2-oxoethyl)-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-6-[4-[[2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetyl]amino]butyl]-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]-4-oxobutanoic acid | 587577: Binding affinity to human PlGF-1 | kd | 0.0090 | uM |
| (2R,3S)-8-[(2S,4R)-5,7-dihydroxy-2-(4-hydroxyphenyl)-3,4-dihydro-2H-chromen-4-yl]-2-(4-hydroxyphenyl)-3,4-dihydro-2H-chromene-3,5,7-triol | 730066: Binding affinity to recombinant PIGF1 (unknown origin) measured for 60 seconds by surface plasmon resonance assay | kd | 0.0110 | uM |
| (1R,5R,6S,13S,21R)-13-(3,4-dihydroxyphenyl)-5-(4-hydroxyphenyl)-4,12,14-trioxapentacyclo[11.7.1.02,11.03,8.015,20]henicosa-2(11),3(8),9,15,17,19-hexaene-6,9,17,19,21-pentol | 730066: Binding affinity to recombinant PIGF1 (unknown origin) measured for 60 seconds by surface plasmon resonance assay | kd | 0.0230 | uM |
| (3S)-4-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]-15-(4-aminobutyl)-6-[(1R)-1-hydroxyethyl]-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxo-3-[[(2S)-2-[[2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetyl]amino]-3-phenylpropanoyl]amino]butanoic acid | 587577: Binding affinity to human PlGF-1 | kd | 0.2000 | uM |
| (1R,5R,6S,13S,21R)-5,13-bis(3,4-dihydroxyphenyl)-4,12,14-trioxapentacyclo[11.7.1.02,11.03,8.015,20]henicosa-2(11),3(8),9,15,17,19-hexaene-6,9,17,19,21-pentol | 730066: Binding affinity to recombinant PIGF1 (unknown origin) measured for 60 seconds by surface plasmon resonance assay | kd | 0.3940 | uM |
| (3S)-3-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]-4-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-15-(4-aminobutyl)-23-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1,6-diamino-1,6-dioxohexan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]-6-[(1R)-1-hydroxyethyl]-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | 587565: Inhibition of human PlGF-1-VEGFR-1 interaction by ELISA | ic50 | 1.0000 | uM |
| (3S)-3-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]-4-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1,6-diamino-1,6-dioxohexan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]-15-(2-amino-2-oxoethyl)-6-[(1R)-1-hydroxyethyl]-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | 587565: Inhibition of human PlGF-1-VEGFR-1 interaction by ELISA | ic50 | 1.0000 | uM |
| (3S)-3-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]-4-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]-15-(4-aminobutyl)-6-[(1R)-1-hydroxyethyl]-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | 587565: Inhibition of human PlGF-1-VEGFR-1 interaction by ELISA | ic50 | 1.0000 | uM |
| (3S)-3-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]-4-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]-15-(2-amino-2-oxoethyl)-6-[(1R)-1-hydroxyethyl]-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | 587565: Inhibition of human PlGF-1-VEGFR-1 interaction by ELISA | ic50 | 1.0000 | uM |
| (3S)-3-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]-4-[[(2S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-15-(4-aminobutyl)-23-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]-6-[(1R)-1-hydroxyethyl]-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | 587565: Inhibition of human PlGF-1-VEGFR-1 interaction by ELISA | ic50 | 5.0000 | uM |
| (3S)-3-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]-4-[[(2S)-1-[[(4R,7S,10S,13S,19S,22S,25S,28R)-4-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]-25-(2-amino-2-oxoethyl)-7-(1H-imidazol-5-ylmethyl)-22-(1H-indol-3-ylmethyl)-10-methyl-13-(2-methylpropyl)-6,9,12,15,18,21,24,27-octaoxo-19-propan-2-yl-1,2-dithia-5,8,11,14,17,20,23,26-octazacyclononacos-28-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | 587565: Inhibition of human PlGF-1-VEGFR-1 interaction by ELISA | ic50 | 5.0000 | uM |
| (3S)-3-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]-4-[[(2S)-1-[[(3S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]-15-(4-aminobutyl)-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | 587565: Inhibition of human PlGF-1-VEGFR-1 interaction by ELISA | ic50 | 6.0000 | uM |
| (3S)-3-[[(2S)-2-acetamido-3-(4-hydroxyphenyl)propanoyl]amino]-4-[[(2S,3S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]-15-(4-aminobutyl)-9-[(2S)-butan-2-yl]-6-(3-carbamimidamidopropyl)-12-[(4-hydroxyphenyl)methyl]-26-(1H-imidazol-5-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-oxobutanoic acid | 587565: Inhibition of human PlGF-1-VEGFR-1 interaction by ELISA | ic50 | 9.0000 | uM |
| (3S)-3-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]-4-[[(2S)-1-[[(3S,9S,12S,15S,18R,23R,26S,29S)-23-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]-15-(2-amino-2-oxoethyl)-26-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-9-propan-2-yl-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | 587565: Inhibition of human PlGF-1-VEGFR-1 interaction by ELISA | ic50 | 9.0000 | uM |
| (3S)-3-[[(2S)-2-acetamido-3-(4-hydroxyphenyl)propanoyl]amino]-4-[[(2S,3S)-1-[[(3S,6S,9S,12S,15S,18R,23R,26S,29S)-15-(4-aminobutyl)-23-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]-9-[(2S)-butan-2-yl]-6-(3-carbamimidamidopropyl)-12-[(4-hydroxyphenyl)methyl]-26-(1H-imidazol-5-ylmethyl)-3-(2-methylpropyl)-2,5,8,11,14,17,25,28-octaoxo-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-18-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-oxobutanoic acid | 587565: Inhibition of human PlGF-1-VEGFR-1 interaction by ELISA | ic50 | 9.0000 | uM |
CTD chemical–gene interactions
105 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Cadmium Chloride | affects expression, decreases expression, increases expression, affects reaction | 6 |
| sodium arsenite | decreases expression, increases abundance, increases expression | 4 |
| Benzo(a)pyrene | increases expression, increases methylation | 4 |
| nickel sulfate | affects cotreatment, increases expression | 3 |
| Resveratrol | affects cotreatment, decreases expression, increases expression | 3 |
| Particulate Matter | decreases expression, increases abundance, affects expression, increases expression | 3 |
| perfluorooctane sulfonic acid | decreases reaction, increases expression, decreases expression | 2 |
| entinostat | increases expression, affects cotreatment | 2 |
| Sunitinib | increases expression | 2 |
| Air Pollutants | increases abundance, decreases expression, affects expression | 2 |
| Arsenic | increases abundance, increases expression | 2 |
| Estradiol | affects cotreatment, increases expression | 2 |
| Colforsin | increases expression, decreases reaction | 2 |
| Nickel | increases expression | 2 |
| Tetrachlorodibenzodioxin | decreases expression | 2 |
| Tobacco Smoke Pollution | increases expression | 2 |
| Valproic Acid | increases expression, increases methylation | 2 |
| Zinc | affects cotreatment, increases expression | 2 |
| aristolochic acid I | increases expression | 1 |
| 6,7-dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine | increases expression | 1 |
| GSK2656157 | decreases reaction, increases expression | 1 |
| ammonium 2,3,3,3-tetrafluoro-2-(heptafluoropropoxy)-propanoate | decreases expression | 1 |
| ODN2006 | decreases secretion | 1 |
| PF-06840003 | decreases expression, decreases reaction | 1 |
| 4-methylumbelliferone 8-carbaldehyde | increases expression, decreases reaction | 1 |
| propionaldehyde | increases expression | 1 |
| pirinixic acid | affects binding, decreases expression, increases activity | 1 |
| lead acetate | affects cotreatment, increases expression | 1 |
| sodium arsenate | increases expression, increases abundance | 1 |
| 2-methyl-4-isothiazolin-3-one | increases expression | 1 |
ChEMBL screening assays
7 unique, capped per target: 7 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1692887 | Binding | Binding affinity to human PlGF-2 | Evolution of potent and stable placental-growth-factor-1-targeting CovX-bodies from phage display peptide discovery. — J Med Chem |
Cellosaurus cell lines
9 cell lines: 6 cancer cell line, 3 embryonic stem cell
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_A5H1 | SEES3-1V human PGF, clone1 | Embryonic stem cell | Male |
| CVCL_A5H2 | SEES3-1V human PGF, clone2 | Embryonic stem cell | Male |
| CVCL_A5H3 | SEES3-1V human PGF, clone3 | Embryonic stem cell | Male |
| CVCL_B8MG | Abcam HCT 116 PGF KO | Cancer cell line | Male |
| CVCL_B9A7 | Abcam MCF-7 PGF KO | Cancer cell line | Female |
| CVCL_B9PM | Abcam A-549 PGF KO | Cancer cell line | Male |
| CVCL_D7WV | Ubigene A-549 PGF KO | Cancer cell line | Male |
| CVCL_TD00 | HAP1 PGF (-) 1 | Cancer cell line | Male |
| CVCL_TD01 | HAP1 PGF (-) 2 | Cancer cell line | Male |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.