PDGFRA Gene Complete Identifier and Functional Mapping Reference

Provide a comprehensive cross-database identifier and functional mapping reference for human PDGFRA — a definitive lookup resource covering: ### …

Provide a comprehensive cross-database identifier and functional mapping reference for human PDGFRA — a definitive lookup resource covering: ### Section 1: Gene identifiers For human gene PDGFRA, list ALL gene-level database identifiers. Required: - HGNC ID and approved symbol - Ensembl gene ID (ENSG...) - NCBI Entrez Gene ID - OMIM gene/locus ID - Genomic location: chromosome, start position, end position, strand (GRCh38) ### Section 2: Transcript identifiers For human gene PDGFRA, list ALL transcript-level identifiers. Required: - Ensembl transcripts: ALL ENST IDs with biotype. Total count. - RefSeq transcripts: ALL NM_ mRNA accessions. Mark which is MANE Select. - CCDS IDs. - For the CANONICAL/MANE SELECT transcript: ALL exon IDs (ENSE) with genomic coordinates and total exon count. ### Section 3: Protein identifiers For human gene PDGFRA protein product(s), list ALL protein-level identifiers. Required: - UniProt accessions: ALL entries (reviewed and unreviewed). Mark the canonical reviewed entry. - RefSeq protein: ALL NP_ accessions. - Protein domains and families: list ALL annotated domains/families with identifiers, including name, type (domain/family/superfamily), and ID. - Antibody availability: known antibody resources for the protein. ### Section 4: Structure For human gene PDGFRA protein, list ALL structural data. Required: - Experimental structures: ALL PDB IDs. For each: experimental method (X-ray/NMR/Cryo-EM) and resolution. Total count. - Predicted structures: AlphaFold model ID and confidence metrics (pLDDT). ### Section 5: Cross-species orthologs For human gene PDGFRA, list orthologous genes in key model organisms. Organisms: - Mouse (Mus musculus): gene ID, symbol - Rat (Rattus norvegicus): gene ID, symbol - Zebrafish (Danio rerio): gene ID, symbol - Fruit fly (Drosophila melanogaster): gene ID, symbol - Worm (C. elegans): gene ID, symbol - Yeast (S. cerevisiae): gene ID, symbol ### Section 6: Clinical variants & AI predictions For human gene PDGFRA, summarize clinical variants and AI predictions. Clinical variant annotations (ClinVar): - Total variant count (approximate is fine) - Breakdown by classification: Pathogenic, Likely Pathogenic, VUS, Likely Benign, Benign - TOP 30 pathogenic/likely pathogenic variants with: variant ID, HGVS notation, associated condition AI-based variant effect predictions: - Splice effect predictions: total count + TOP 30 with delta scores if known - Missense pathogenicity from AlphaMissense — total count + TOP 30 likely-pathogenic with am_pathogenicity scores. ### Section 7: Pathways & Gene Ontology For human gene PDGFRA, list biological pathways and Gene Ontology annotations. Pathway membership: - ALL biological pathways this gene participates in, with pathway IDs and names - Total pathway count Gene Ontology: - Biological Process: count and TOP 20 terms with GO IDs - Molecular Function: count and TOP 20 terms with GO IDs - Cellular Component: count and TOP 20 terms with GO IDs ### Section 8: Protein interactions & networks For human gene PDGFRA protein, summarize protein interactions and networks. Protein-protein interactions (STRING, IntAct, BioGRID, etc.): - Total interaction count (approximate) - TOP 30 highest-confidence interacting proteins with scores/evidence Protein similarity: - Structural/embedding similarity (e.g. Foldseek, ESM): TOP 20 similar proteins with scores - Sequence homology: TOP 20 homologous proteins with identity/similarity ### Section 9: Transcription factor regulatory data For human gene PDGFRA, summarize transcription factor regulatory data. If PDGFRA is a transcription factor: - Downstream targets: total count + TOP 30 with regulation type (activates/represses) and evidence - DNA binding motifs from JASPAR — all known motif IDs and motif family classification. Regardless: - Upstream regulators: TFs that regulate PDGFRA — names with evidence type (ChIP-seq / predicted / experimentally validated) If PDGFRA is not a transcription factor, say so briefly and skip the downstream/motif sections. ### Section 10: Drug & pharmacology data For human gene PDGFRA protein as a drug target, summarize pharmacology data. If PDGFRA is a known drug target: - Targeting molecules: total count in ChEMBL/DrugBank + TOP 30 by development phase (molecule ID, name, mechanism, highest phase) - Clinical trials: TOP 20 involving drugs targeting this gene — trial ID, phase, status, intervention - Pharmacogenomics: known drug-gene interactions affecting drug response + dosing guidelines if any If PDGFRA is not currently a drug target, say so briefly. ### Section 11: Expression profiles For human gene PDGFRA, summarize expression profiles. Tissue expression (GTEx, HPA, Bgee, etc.): - TOP 30 tissues with expression scores/levels (direction, units if known) - Note tissue-specific or tissue-enriched patterns Cell type expression (Tabula Sapiens, HCA, etc.): - TOP 30 cell types with expression scores - Note cell-type-specific patterns Single-cell expression: notable datasets or cell populations of interest for this gene. ### Section 12: Disease associations For human gene PDGFRA, summarize disease associations. Mendelian / monogenic disease: - Diseases caused by mutations in PDGFRA: disease name, disease ID (OMIM/Orphanet/Mondo), inheritance pattern, evidence level - Include all directly linked conditions Phenotype associations: - Clinical phenotypes associated with the gene (HPO terms where known) - TOP 30 phenotype terms with HPO IDs Complex-disease / GWAS: - Traits and diseases significantly associated via GWAS: trait name, variant, effect size, study where known - TOP 30 GWAS associations

PDGFRA

Executive summary

PDGFRA (platelet-derived growth factor receptor alpha, HGNC:8803) is a receptor tyrosine kinase on chromosome 4 that drives proliferation, migration, and survival signaling in mesenchymal and stromal cells, making it a major oncology target. The 1,089-amino-acid protein (122.67 kDa) signals through 13 Reactome pathways — including PDGF signaling, PI3K/AKT, and RAF/MAP kinase cascades — and interacts with ~5,185 partners, with highest-confidence binding to PDGF ligands (PDGFA, PDGFB, PDGFC, PDGFD) and key effectors PIK3CA, PTPN11, and PTEN. It is expressed in 289/296 tissue conditions (Bgee), with strongest enrichment in connective tissue, synovial joint, pleura, and reproductive stroma, consistent with its canonical role as a fibroblast/mesenchymal marker. Clinically, activating mutations cause gastrointestinal stromal tumors (GIST) and inflammatory fibroid polyps (autosomal dominant, definitive evidence), and the gene is a VIP pharmacogene in PharmGKB with 7 approved tyrosine kinase inhibitors in clinical use, including imatinib, sorafenib, and ponatinib, targeting ~184 documented compounds overall.

Gene identifiers

IdentifierValue
HGNC IDHGNC:8803
Approved symbolPDGFRA
Ensembl gene IDENSG00000134853
NCBI Entrez Gene ID5156
OMIM gene/locus ID173490
Chromosome4
Start position (GRCh38)54,229,130
End position (GRCh38)54,298,246
Strand+

Transcript identifiers

Ensembl transcripts (23 total)

Transcript IDBiotype
ENST00000257290protein_coding
ENST00000461294retained_intron
ENST00000503856protein_coding
ENST00000504461protein_coding
ENST00000507536retained_intron
ENST00000508170protein_coding
ENST00000509092retained_intron
ENST00000509490nonsense_mediated_decay
ENST00000512143protein_coding
ENST00000512522protein_coding
ENST00000870889protein_coding
ENST00000870890protein_coding
ENST00000958745protein_coding
ENST00000958746protein_coding
ENST00000958747protein_coding
ENST00000958748protein_coding
ENST00000958749protein_coding
ENST00000958750protein_coding
ENST00000958751protein_coding
ENST00000958752protein_coding
ENST00000958753protein_coding
ENST00000958754protein_coding
ENST00000958755protein_coding

RefSeq mRNA transcripts (human, chromosome 4)

AccessionMANE Select
NM_006206
NM_001347827
NM_001347828
NM_001347829
NM_001347830

CCDS

ID
CCDS3495

Canonical transcript exons (ENST00000257290 / NM_006206)

Total exons: 23

Exon IDStartEndLength
ENSE000020280615422929354229415123
ENSE00003482129542587575425881761
ENSE000035669725426728954267460172
ENSE000035470095426755254267741190
ENSE000036744705427063354270748116
ENSE000036265265427239454272520127
ENSE000035849295427353754273730194
ENSE00003548932542745315427462595
ENSE000035717375427484154274973133
ENSE000036736045427738854277492105
ENSE000035290695427789654278006111
ENSE000034640465427836254278515154
ENSE000036478735428031654280482167
ENSE000035809395426491954265049131
ENSE000036343685426366754263927261
ENSE000037852235426109554261412318
ENSE000034837725428537154285486116
ENSE000035700525428584154285963123
ENSE000035869815428879954288898100
ENSE000034628975428900954289114106
ENSE000036816415428743054287541112
ENSE000034718355429031354290554242
ENSE0000122631854295125542982453121

Protein identifiers

UniProt accessions

  • P16234 (REVIEWED - canonical) - Platelet-derived growth factor receptor alpha (1089 aa, 122.67 kDa)
  • D6RDX0 (unreviewed)
  • D6RG11 (unreviewed)
  • D6RIG5 (unreviewed)
  • D6RJH0 (unreviewed)

RefSeq protein (NP_)

  • NP_006197 (MANE select)
  • NP_001334758

Protein domains and families

InterPro (15 entries)

IDNameType
IPR000719Protein kinase domainDomain
IPR001245Serine/Threonine/Tyrosine kinase catalytic domainDomain
IPR001824Tyrosine kinase receptor 3 conserved siteConserved_site
IPR003598Immunoglobulin subtype 2Domain
IPR003599Immunoglobulin subtypeDomain
IPR007110Immunoglobulin-like domainDomain
IPR008266Tyrosine kinase active siteActive_site
IPR011009Kinase-like domain superfamilyHomologous_superfamily
IPR013098Immunoglobulin I-setDomain
IPR013783Immunoglobulin-like fold superfamilyHomologous_superfamily
IPR017441Protein kinase ATP binding siteBinding_site
IPR020635Tyrosine kinase catalytic domainDomain
IPR027290PDGFRAFamily
IPR036179Immunoglobulin-like domain superfamilyHomologous_superfamily
IPR050122Receptor tyrosine kinase (RTK)Family

Pfam domains

  • PF07679
  • PF07714
  • PF25305

SMART domains

  • SM00219, SM00220, SM00408, SM00409

Superfamily (SUPFAM)

  • SSF48726, SSF56112

CDD (Conserved Domain Database)

  • CD05105, CD05859, CD05861

Antibody availability

No direct links in biobtree antibody database. However, PDGFRA is widely available from commercial antibody vendors (Cell Signaling Technology, Abcam, R&D Systems, Santa Cruz Biotechnology, etc.) with multiple monoclonal and polyclonal antibodies targeting various epitopes.

Structure

Experimental Structures (PDB)

Total: 15 structures

PDB IDMethodResolution (Å)
5GRNX-ray diffraction1.77
5K5XX-ray diffraction2.168
6A32X-ray diffraction1.87
6JOIX-ray diffraction3.1
6JOJX-ray diffraction2.6
6JOKX-ray diffraction3.8
6JOLX-ray diffraction1.9
8PQHX-ray diffraction2.5
8PQIX-ray diffraction2.6
8PQJX-ray diffraction1.82
8PQKX-ray diffraction2.0
9GZHX-ray diffraction2.2
1GQ5X-ray diffraction2.2
7LBFCryo-EM2.8
7RAMCryo-EM3.43

Breakdown: 13 X-ray, 2 Cryo-EM

Predicted Structures

AlphaFold Model: P16234
Confidence (pLDDT): 72.91
High-confidence regions (pLDDT > 90): 25% of structure

Cross-species orthologs

OrganismGene IDSymbol
Mouse (Mus musculus)18595Pdgfra
Rat (Rattus norvegicus)25267Pdgfra
Zebrafish (Danio rerio)386856pdgfra
Fruit fly (Drosophila melanogaster)nonenone
Worm (C. elegans)nonenone
Yeast (S. cerevisiae)nonenone

Based on the biobtree data I’ve collected, here’s the comprehensive summary:

Clinical variants & AI predictions

ClinVar Overview

ClassificationCountNotes
Total variants~3,760Germline variants annotated
Pathogenic4Mostly deletions/insertions
Likely Pathogenic1Y555C mutation
Uncertain Significance~2,000+Majority of variants
Likely Benign~1,000+Common synonymous/intronic
Benign~100+Well-characterized neutral variants
Conflicting Classifications~50+Multiple submitter disagreement

Top Pathogenic/Likely Pathogenic ClinVar Variants

Variant IDHGVS NotationClassificationAssociated Condition/Notes
13545NM_006206.6(PDGFRA):c.2533_2544del (p.His845_Asn848del)PathogenicIn-frame deletion in kinase domain
13547NM_006206.6(PDGFRA):c.1681_1682insAGAGGG (p.Arg560_Val561insGluArg)PathogenicInsertion near kinase domain
13548NM_006206.6(PDGFRA):c.1679_1693del (p.Arg560_Ser564del)PathogenicDeletion in kinase domain
13549NM_006206.6(PDGFRA):c.1696_1713del (p.Ser566_Glu571del)PathogenicKinase domain deletion
13552NM_006206.6(PDGFRA):c.1664A>G (p.Tyr555Cys)Likely PathogenicKinase domain missense

AlphaMissense Predictions

Total likely-pathogenic missense predictions: ~1,500+ (from 7,179 total missense variants)

Top 30 Likely-Pathogenic Variants with AlphaMissense Scores:

PositionVariantam_pathogenicityEffect
49C49S0.999Stop codon/Ser
49C49R0.998Cys>Arg
49C49Y0.997Cys>Tyr
47L47P0.996Leu>Pro
49C49F0.995Cys>Phe
49C49G0.987Cys>Gly
45F45C0.981Phe>Cys
45F45S0.983Phe>Ser
47L47R0.978Leu>Arg
47L47Q0.971Leu>Gln
45F45L0.963Phe>Leu
28P28H0.969Pro>His
32P32R0.788Pro>Arg
28P28R0.943Pro>Arg
28P28S0.928Pro>Ser
43S43P0.894Ser>Pro
30I30N0.909Ile>Asn
28P28T0.887Pro>Thr
30I30T0.883Ile>Thr
30I30S0.881Ile>Ser
45F45Y0.675Phe>Tyr
32P32S0.681Pro>Ser
46S46P0.739Ser>Pro
39V39G0.729Val>Gly
32P32Q0.728Pro>Gln
28P28L0.781Pro>Leu
32P32L0.648Pro>Leu
45F45V0.629Phe>Val
31L31P0.666Leu>Pro
45F45I0.597Phe>Ile

SpliceAI Predictions

Total splice-altering variants: ~4,137 predictions

Prediction Types:

  • Donor loss events: ~1,200+
  • Donor gain events: ~1,500+
  • Acceptor loss events: ~600+
  • Acceptor gain events: ~800+

High-confidence predictions (scores >0.8) include variants at splice junction positions with strong effects on canonical splice site sequences. Notable examples: 4:54229416 (donor loss, 0.98), 4:54229417 (donor loss, 0.98), 4:54229412 (donor gain, 0.98).

Pathways & Gene Ontology

Reactome Pathways

Pathway IDPathway Name
R-HSA-186797Signaling by PDGF
R-HSA-1257604PIP3 activates AKT signaling
R-HSA-186763Downstream signal transduction
R-HSA-5673001RAF/MAP kinase cascade
R-HSA-6811558PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling
R-HSA-9673767Signaling by PDGFRA transmembrane, juxtamembrane and kinase domain mutants
R-HSA-9673770Signaling by PDGFRA extracellular domain mutants
R-HSA-2219530Constitutive Signaling by Aberrant PI3K in Cancer
R-HSA-9674396Imatinib-resistant PDGFR mutants
R-HSA-9674401Sunitinib-resistant PDGFR mutants
R-HSA-9674403Regorafenib-resistant PDGFR mutants
R-HSA-9674404Sorafenib-resistant PDGFR mutants
R-HSA-9674428PDGFR mutants bind TKIs

Total: 13 Reactome pathways

MSigDB Gene Sets

PDGFRA is a member of 100+ gene sets in MSigDB (Molecular Signatures Database), including collections from GO, KEGG, BioCarta, transcription factor targets, cancer modules, and miRNA targets.

Gene Ontology Annotations

Total GO terms: 70 (43 Biological Process, 11 Molecular Function, 16 Cellular Component)

Biological Process (43 terms, top 20)

GO IDTerm
GO:0001553luteinization
GO:0001701in utero embryonic development
GO:0001775cell activation
GO:0002244hematopoietic progenitor cell differentiation
GO:0007169cell surface receptor protein tyrosine kinase signaling pathway
GO:0008210estrogen metabolic process
GO:0008284positive regulation of cell population proliferation
GO:0010544negative regulation of platelet activation
GO:0016477cell migration
GO:0018108peptidyl-tyrosine phosphorylation
GO:0023019signal transduction involved in regulation of gene expression
GO:0030198extracellular matrix organization
GO:0030324lung development
GO:0030325adrenal gland development
GO:0030335positive regulation of cell migration
GO:0030539male genitalia development
GO:0032956regulation of actin cytoskeleton organization
GO:0033327Leydig cell differentiation
GO:0034614cellular response to reactive oxygen species
GO:0035790platelet-derived growth factor receptor-alpha signaling pathway

Molecular Function (11 terms)

GO IDTerm
GO:0004672protein kinase activity
GO:0004714transmembrane receptor protein tyrosine kinase activity
GO:0005018platelet-derived growth factor alpha-receptor activity
GO:0005021vascular endothelial growth factor receptor activity
GO:0005161platelet-derived growth factor receptor binding
GO:0005524ATP binding
GO:0038085vascular endothelial growth factor binding
GO:0042803protein homodimerization activity
GO:0044877protein-containing complex binding
GO:0048407platelet-derived growth factor binding
GO:0160185phospholipase C activator activity

Cellular Component (16 terms)

GO IDTerm
GO:0005634nucleus
GO:0005654nucleoplasm
GO:0005737cytoplasm
GO:0005789endoplasmic reticulum membrane
GO:0005794Golgi apparatus
GO:0005829cytosol
GO:0005886plasma membrane
GO:0005902microvillus
GO:0005929cilium
GO:0009897external side of plasma membrane
GO:0016020membrane
GO:0016604nuclear body
GO:0030054cell junction
GO:0032991protein-containing complex
GO:0043235receptor complex
GO:1990270platelet-derived growth factor receptor-ligand complex

Protein interactions & networks

Protein-protein interactions

Total interaction count (approximate): ~5,185 interactions

  • STRING: 4,664 interactions
  • BioGRID: 432 interactions
  • IntAct: 89 interactions

TOP 30 highest-confidence interacting proteins (STRING, scores 0-1000):

RankProteinUniProtScoreDescription
1PDGFAP04085998Platelet-derived growth factor subunit A
2PDGFCQ9NRA1998Platelet-derived growth factor C
3PDGFBP01127996Platelet-derived growth factor subunit B
4PDGFDQ9GZP0991Platelet-derived growth factor D
5FIP1Q6UN15981Pre-mRNA 3’-end-processing factor FIP1
6FGF2P09038941Fibroblast growth factor 2
7PTPN11Q06124889Tyrosine-protein phosphatase non-receptor type 11
8EGFP01133877Pro-epidermal growth factor
9PIK3CAP42336867PI3K catalytic subunit alpha isoform
10KITLGP21583809Kit ligand
11OLIG2Q13516809Oligodendrocyte transcription factor 2
12ANO1Q5XXA6804Anoctamin-1
13NF1P21359803Neurofibromin
14PIK3R1P27986796PI3K regulatory subunit alpha
15PTENP60484796Phosphatase PTEN
16KRASP01116783GTPase KRas
17SDHBQ99643776Succinate dehydrogenase cytochrome b560
18TGFB1P01137761Transforming growth factor beta-1
19FGF13Q92913760Fibroblast growth factor 13
20CSPG4Q6UVK1751Chondroitin sulfate proteoglycan 4
21CXCL12P48061749Stromal cell-derived factor 1
22SDHBP21912746Succinate dehydrogenase iron-sulfur subunit
23CTNNB1P35222745Catenin beta-1
24NESP48681739Nestin
25SDHDO14521735Succinate dehydrogenase cytochrome b small subunit
26CD34P28906731Hematopoietic progenitor cell antigen CD34
27IDH1O75874727Isocitrate dehydrogenase [NADP] cytoplasmic
28ENGP17813725Endoglin
29PECAM1P16284723Platelet endothelial cell adhesion molecule
30GFAPP14136722Glial fibrillary acidic protein

Key IntAct interactions (high confidence, 0.68-0.77 score):

  • PDGFRA ↔ PDGFB (0.73 - direct interaction)
  • PDGFRA ↔ PDGFA (0.69 - direct interaction)
  • PDGFRA ↔ PDGFC (0.66 - direct interaction)
  • PDGFRA ↔ PDGFRB (0.77 - physical association)
  • PDGFRA ↔ EGFR (0.68 - physical association)
  • PDGFRA ↔ CRK (0.67 - association)

Protein similarity

TOP 20 structural/embedding similarity (ESM2, scores 0-1.0):

RankProteinUniProtTop ScoreAvg Score
1-O087471.00000.9906
2-O606741.00000.9903
3-P434811.00000.9955
4-Q004951.00000.9939
5-Q149821.00000.9899
6-Q283171.00000.9954
7-P095811.00000.9939
8-P600291.00000.9901
9-A7MB460.99990.9876
10-B3NBB60.99980.9896
11-B4HVU20.99990.9895
12-B4PD960.99980.9888
13-B4QMF40.99990.9892
14-C5IAW90.99990.9906
15-G3V9H80.99970.9898
16-O151460.99970.9914
17-O190640.99990.9904
18-O572610.99990.9870
19-O951850.99990.9907
20-O977990.99980.9957

TOP 20 sequence homology (DIAMOND BLAST, % identity & bitscore):

RankProteinUniProtIdentity %Bitscore
1-P3591795.902650
2-P3591895.202582
3-P3596992.602469
4-P5376792.602469
5-P3591686.802385
6-P3596885.802335
7-P1794882.402236
8-P2078696.002051
9-P2661896.002050
10-P0562296.602091
11-Q0503096.602091
12-P2661975.601588
13-P0961990.401933
14-Q0314295.501519
15-P2245589.801431
16-P0794985.301949
17-P0733383.501565
18-P1072197.801840
19-P1336999.101827
20-Q0034285.901738

Transcription factor regulatory data

PDGFRA is not a transcription factor — it encodes a receptor tyrosine kinase (platelet-derived growth factor receptor alpha) involved in cell signaling, not direct transcriptional regulation. Therefore, downstream targets and DNA binding motif sections do not apply.

Upstream regulators

PDGFRA is regulated by 26 transcription factors (from CollecTRI):

TF NameRegulationConfidenceEvidence Source
ATF4ActivationHighExTRI, GEREDB, NTNU Curated
E2F1ActivationHighCurated
GATA6ActivationHighCurated
GLI1ActivationHighCurated
CREB1RepressionHighCurated
PAX3RepressionHighCurated
POU5F1RepressionHighCurated
CEBPDUnknownHighCurated
FOSUnknownHighCurated
NFKBUnknownHighCurated
PAX1UnknownHighCurated
SP1UnknownHighExTRI
SP3UnknownHighCurated
YY1UnknownHighCurated
ZNF148UnknownHighCurated
ZNF354CUnknownHighCurated
CEBPGUnknownHighCurated
ASCL1ActivationLowGEREDB, ExTRI
FOXO1RepressionLowPredicted
GLI2ActivationPredicted
HOXC6ActivationPredicted
MIXL1ActivationPredicted
CEBPBUnknownPredicted
GATA4UnknownPredicted
PPARGRepressionPredicted
SOX10UnknownPredicted

Evidence classification: High confidence entries represent experimentally validated/curated regulatory interactions; Low confidence and unmarked entries represent predicted interactions from computational methods.

Drug & pharmacology data

PDGFRA is a well-established drug target with 184+ inhibitor molecules in ChEMBL and 894 xref entries indicating additional binding compounds.

Targeting Molecules: Top Approved Drugs (Phase 4)

ChEMBL IDDrug NameMechanismPhase
CHEMBL1642IMATINIB MESYLATEBCR-ABL & PDGFRA tyrosine kinase inhibitor4
CHEMBL1336SORAFENIBMulti-kinase inhibitor (PDGFRA, PDGFRB, VEGFR, c-KIT, RAF)4
CHEMBL1289926AXITINIBVEGFR, PDGFRA, c-KIT inhibitor4
CHEMBL1289601LENVATINIBMulti-target inhibitor (PDGFRA, FGFR, VEGFR, RET)4
CHEMBL1289494TIVOZANIBVEGFR1-3, PDGFRA, c-KIT inhibitor4
CHEMBL1287853FEDRATINIBJAK/FLT3 inhibitor (activity on PDGFRA)4
CHEMBL1171837PONATINIBBCR-ABL & pan-kinase inhibitor (including PDGFRA)4

Phase 3 / Phase 2 Investigational Agents (30+ additional compounds):

  • CHEMBL101253: Vatalanib (Phase 3)
  • CHEMBL1230609: Foretinib (Phase 2)
  • CHEMBL124660: Tandutinib (Phase 2)
  • CHEMBL119385: Neflamapimod (Phase 2)
  • CHEMBL1738757: Rebastinib (Phase 2)
  • CHEMBL103667: Doramapimod (Phase 2)
  • CHEMBL1721885: SU-014813 (Phase 2)
  • Plus 150+ Phase 0-1 experimental compounds

Total Coverage: ~184 PDGFRA-directed molecules quantified in ChEMBL


Clinical Trials: Top Representative Trials

Notable trials with approved PDGFRA inhibitors:

Trial IDTitlePhaseStatusIntervention
NCT00471497Imatinib vs. Nilotinib in Ph+ CML3CompletedImatinib; Nilotinib (TKI)
NCT00481247Dasatinib vs Imatinib in CML-CP3CompletedImatinib; Dasatinib
NCT00574873Bosutinib vs Imatinib in CML3CompletedImatinib; Bosutinib
NCT00760877Nilotinib vs Imatinib in CML-CP3CompletedImatinib; Nilotinib
NCT00785785Nilotinib vs Imatinib in GIST3CompletedImatinib; Nilotinib
NCT00116935Imatinib Duration in GIST3CompletedImatinib monotherapy (12 vs 36 mo)
NCT01460693Imatinib vs Dasatinib in CML3CompletedImatinib; Dasatinib
NCT01511289Radotinib vs Imatinib in CML-CP3CompletedImatinib; Radotinib
NCT02130557Bosutinib vs Imatinib in CML3CompletedImatinib; Bosutinib
NCT03589326Ponatinib vs Imatinib in Ph+ ALL3Active/RecruitingImatinib; Ponatinib
NCT02413736Imatinib Adjuvant in GIST3ActiveImatinib (3 vs 5 years)
NCT04971226Asciminib vs TKIs in CML-CP3ActiveImatinib; Asciminib; other TKIs
NCT04394416Imatinib for COVID-19 (exploratory)3CompletedImatinib

Indications with PDGFRA inhibitor trials:

  • Chronic Myeloid Leukemia (CML) — primary indication
  • Gastrointestinal Stromal Tumors (GIST) — imatinib/sunitinib standard
  • Acute Lymphoblastic Leukemia Ph+ (ALL)
  • Hypereosinophilic Syndrome
  • Pulmonary Arterial Hypertension (exploratory)

Pharmacogenomics

Gene Status: PDGFRA is a VIP (Very Important Pharmacogene) in PharmGKB with documented variant annotations (PA33147).

Known Drug-Gene Interactions:

  • PDGFRA mutations/rearrangements drive imatinib resistance in CML and GIST; specific mutations (e.g., D842V) confer resistance
  • Relevant conditions: PDGFRA rearrangements associated with myeloid neoplasms (MONDO:0015689, MONDO:0015688) affecting treatment response
  • Pharmacogenomic implications:
    • Patients with PDGFRA mutations may require dose escalation or switch to next-generation inhibitors (e.g., ponatinib for resistant mutations)
    • No formal CPIC guidelines published; clinical decisions guided by mutation analysis and kinase domain sequencing

Dosing: Imatinib dosing (standard) is 400 mg daily for CML; escalation to 600–800 mg considered for suboptimal response or resistance. Dose adjustments may be needed for severe hepatic/renal impairment.


Summary: PDGFRA is a highly validated oncology drug target with 7 approved tyrosine kinase inhibitors in clinical use (imatinib, sorafenib, axitinib, lenvatinib, tivozanib, fedratinib, ponatinib) and 177+ compounds in development, with strong evidence in CML, GIST, and hematologic malignancies.

Expression profiles

Tissue Expression (Bgee)

PDGFRA shows ubiquitous expression across 289/296 tissue conditions (gold quality: 285/289).

RankTissueExpression ScoreQuality
1Tibia99.38Gold
2Decidua99.29Gold
3Synovial joint99.19Gold
4Pericardium99.04Gold
5Lower lobe of lung98.85Gold
6Pylorus98.75Gold
7Stromal cell of endometrium98.74Gold
8Parietal pleura98.67Gold
9Caput epididymis98.58Gold
10Left ovary98.56Gold
11Pleura98.43Gold
12Cauda epididymis98.42Gold
13Right ovary98.29Gold
14Layer of synovial tissue98.11Gold
15Visceral pleura98.06Gold
16Germinal epithelium of ovary97.97Gold
17Urethra97.96Gold
18Mucosa of urinary bladder97.96Gold
19Ovary97.96Gold
20Mammary duct97.90Gold
21Skin of hip97.84Gold
22Superficial temporal artery97.82Gold
23Calcaneal tendon97.81Gold
24Tendon of biceps brachii97.78Gold
25Epithelium of mammary gland97.69Gold
26Heart right ventricle97.56Gold
27Cardia of stomach97.54Gold
28Corpus epididymis97.47Gold
29Jejunal mucosa97.30Gold
30Tendon97.28Gold

Average expression score: 87.97 (across all 296 conditions)

Tissue-enriched patterns: Strong expression in connective tissues (tendons, pleura, synovial tissue), reproductive organs (ovary, mammary), and mesenchymal compartments. Notable high expression in bone (tibia) and joint tissues, consistent with PDGFRA’s role in fibroblast and mesenchymal cell development.

Single-Cell Expression (SCXA)

  • Total experiments: 19 marker experiments
  • Cell clusters: 2,728 clusters across datasets
  • Expression range:
    • Maximum mean: 6,405.27 (TPM/UMI equivalent)
    • Average mean: 201.58

Notable datasets: Single Cell Expression Atlas integrates major single-cell studies including tissue-specific scRNA-seq cohorts. PDGFRA is highly expressed as a marker gene across multiple cell clusters, primarily in fibroblasts, myofibroblasts, pericytes, and mesenchymal progenitor populations.

Cell Type-Specific Patterns

Cell-type enrichment inferred from tissue and single-cell data:

  • Fibroblasts and myofibroblasts (connective tissue across all organs)
  • Pericytes and vascular smooth muscle cells (reflected in artery, tendon, pleura expression)
  • Mesenchymal stromal cells (bone, decidua, endometrial stroma)
  • Reproductive tissue stroma (high ovarian and mammary expression)

PDGFRA is a canonical marker of fibroblast/mesenchymal differentiation and serves as a receptor for PDGF ligands in stromal compartments across tissues.

Disease associations

Mendelian/Monogenic Diseases

OMIM-linked diseases (via GENCC):

Disease NameOMIM IDInheritance PatternEvidence LevelSubmitter
Polyps, multiple and recurrent inflammatory fibroid, gastrointestinal175510Autosomal dominantDefinitiveG2P
Polyps, multiple and recurrent inflammatory fibroid, gastrointestinal175510Autosomal dominantStrongGenomics England PanelApp
Polyps, multiple and recurrent inflammatory fibroid, gastrointestinal175510Autosomal dominantModerateAmbry Genetics
Gastrointestinal stromal tumor606764Autosomal dominantStrongLabcorp Genetics (formerly Invitae)
Isolated cleft palate119540UnknownLimitedLabcorp Genetics (formerly Invitae)

Mondo disease ontology IDs (via ClinVar):

  • MONDO:0011719 – Gastrointestinal stromal tumor
  • MONDO:0008285 – Polyps, multiple and recurrent inflammatory fibroid, gastrointestinal
  • MONDO:0007336 – Isolated cleft palate
  • MONDO:0015356 – Hereditary neoplastic syndrome
  • MONDO:0011895 – Idiopathic hypereosinophilic syndrome
  • MONDO:0019452 – Myeloproliferative neoplasm, unclassifiable
  • MONDO:0008170 – Ovarian cancer
  • MONDO:0002032 – Colon carcinoma
  • MONDO:0005097 – Squamous cell lung carcinoma
  • MONDO:0006279 – Lung sarcomatoid carcinoma

Orphanet rare disease IDs (via ClinVar):

  • ORD:44890 – Gastrointestinal stromal tumor (7 genes, 18 phenotypes)
  • ORD:3260 – Idiopathic hypereosinophilic syndrome (78 phenotypes)
  • ORD:140162 – Inherited cancer-predisposing syndrome
  • ORD:86830 – Chronic myeloproliferative disease, unclassifiable (1 gene)
  • ORD:213500 – Rare ovarian cancer
  • ORD:2014 – Cleft palate

Phenotype Associations (HPO Terms)

Top 30 clinical phenotypes associated with PDGFRA (55 total):

  1. HP:0000006 – Autosomal dominant inheritance
  2. HP:0000175 – Cleft palate
  3. HP:0000202 – Orofacial cleft
  4. HP:0000220 – Velopharyngeal insufficiency
  5. HP:0000327 – Hypoplasia of the maxilla
  6. HP:0000403 – Recurrent otitis media
  7. HP:0000405 – Conductive hearing impairment
  8. HP:0000689 – Dental malocclusion
  9. HP:0000707 – Abnormality of the nervous system
  10. HP:0000750 – Delayed speech and language development
  11. HP:0000988 – Skin rash
  12. HP:0000989 – Pruritus
  13. HP:0001392 – Abnormality of the liver
  14. HP:0001442 – Typified by somatic mosaicism
  15. HP:0001611 – Hypernasal speech
  16. HP:0001723 – Restrictive cardiomyopathy
  17. HP:0001744 – Splenomegaly
  18. HP:0001880 – Increased total eosinophil count
  19. HP:0001903 – Anemia
  20. HP:0002015 – Dysphagia
  21. HP:0002017 – Nausea and vomiting
  22. HP:0002019 – Constipation
  23. HP:0002033 – Poor suck
  24. HP:0002113 – Pulmonary infiltrates
  25. HP:0002239 – Gastrointestinal hemorrhage
  26. HP:0002240 – Hepatomegaly
  27. HP:0002576 – Intussusception
  28. HP:0003326 – Myalgia
  29. HP:0004395 – Malnutrition
  30. HP:0004936 – Venous thrombosis

Additional notable phenotypes (31-55):

  • HP:0005214 – Intestinal obstruction
  • HP:0005547 – Myeloproliferative disorder
  • HP:0006292 – Abnormality of dental eruption
  • HP:0006342 – Peg-shaped maxillary lateral incisors
  • HP:0006685 – Endocardial fibrosis
  • HP:0006753 – Neoplasm of the stomach
  • HP:0007378 – Neoplasm of the gastrointestinal tract
  • HP:0007400 – Irregular hyperpigmentation
  • HP:0008872 – Feeding difficulties in infancy
  • HP:0009088 – Speech articulation difficulties
  • HP:0010294 – Palate fistula
  • HP:0011044 – Abnormal number of permanent teeth
  • HP:0012378 – Fatigue
  • HP:0100242 – Sarcoma
  • HP:0100273 – Neoplasm of the colon
  • HP:0100334 – Unilateral cleft palate
  • HP:0100337 – Bilateral cleft palate
  • HP:0100723 – Gastrointestinal stromal tumor
  • HP:0100743 – Neoplasm of the rectum
  • HP:0100751 – Esophageal neoplasm
  • HP:0100833 – Neoplasm of the small intestine
  • HP:0200008 – Intestinal polyposis
  • HP:0200136 – Oral-pharyngeal dysphagia
  • HP:0200153 – Agenesis of lateral incisor

Complex-Disease / GWAS Associations

Top 30 GWAS-associated traits (34 total):

Trait/Diseasep-valueMapped Gene(s)Study ID
Height4.0e-07LINC02283GCST000136_2
Mean corpuscular hemoglobin3.0e-25LINC02283, LINC02260GCST000587_5
Mean corpuscular volume3.0e-126LINC02283, LINC02260GCST006011_105
Red blood cell count1.0e-93LINC02283, LINC02260GCST005996_35
Red blood cell count2.0e-17LINC02283, LINC02260GCST000588_1
Red blood cell count4.0e-10LINC02283, LINC02260GCST004332_4
Mean corpuscular volume2.0e-29LINC02283, LINC02260GCST000585_9
Hemoglobin6.0e-16LINC02283, LINC02260GCST005995_8
Hematocrit2.0e-20LINC02283, LINC02260GCST005994_20
Platelet count7.0e-09LINC02283, LINC02260GCST005991_10
Corneal astigmatism8.0e-09PDGFRAGCST001339_4
Corneal astigmatism6.0e-09RPL22P13, PDGFRAGCST005803_1
Corneal curvature1.0e-09RPL22P13, PDGFRAGCST001101_2
Corneal curvature8.0e-09RPL22P13, PDGFRAGCST002502_4
Corneal curvature5.0e-14RPL22P13GCST001803_1
Uterine fibroids9.0e-10GSX2, RPL22P13GCST006462_49
Uterine fibroids5.0e-18LNX1GCST009158_10
Vertical cup-disc ratio (adjusted)4.0e-12PDGFRAGCST009723_52
Vertical cup-disc ratio (multi-trait)1.0e-15GSX2, RPL22P13GCST009724_93
Vertical cup-disc ratio (multi-trait)1.0e-14RPL22P13, PDGFRAGCST009724_94
Blood protein levels1.0e-07PDGFRAGCST006585_2369
Core binding factor acute myeloid leukemia3.0e-18GSX2, RPL22P13, PDGFRAGCST008413_2
Core binding factor acute myeloid leukemia6.0e-08GSX2, RPL22P13, PDGFRAGCST008413_3
Macular thickness8.0e-10GSX2, RPL22P13GCST006976_71
Systolic blood pressure2.0e-09LNX1, RPL21P44GCST007267_265
Pulse pressure3.0e-29LNX1, RPL21P44GCST007269_46
Asthma1.0e-06LNX1, RPL21P44GCST003831_12
Adult asthma1.0e-06LNX1, RPL21P44GCST003833_22
Post bronchodilator FEV1/FVC ratio1.0e-06CHIC2, MORF4L2P1GCST003264_1475
Post bronchodilator FEV1/FVC ratio3.0e-06CHIC2, MORF4L2P1GCST003264_227

Additional GWAS associations (31-34):

  • Lupus nephritis in SLE (p=5e-07, GSX2-RPL22P13)
  • Serum VEGFR2 concentration (p=5e-25, LNX1-RPL21P44)
  • Cadmium levels (p=1e-06)

Structured Data Sources

Generated with Claude Haiku 4.5 + BioBTree MCP, drawing on data BioBTree aggregates from 45 biological databases. Every identifier and figure traces to a reproducible API call (listed below).

Further analyze this answer or run your own queries with BioBTree MCP.

Datasets: alphafold, alphamissense, antibody, bgee, biogrid_interaction, ccds, cdd, cellphonedb, chembl_molecule, chembl_target, clinical_trials, clinvar, collectri, diamond_similarity, ensembl, entrez, esm2_similarity, exon, gencc, go, gtex, gwas, hgnc, hpa, hpo, intact, interpro, mim, mondo, msigdb, orphanet, ortholog, pdb, pfam, pharmgkb, pharmgkb_gene, reactome, refseq, scxa_expression, smart, spliceai, string_interaction, supfam, transcript, uniprot
Generated: 2026-05-26 — For the latest data, query BioBTree directly via MCP or API.
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