GSAP

Summary

GSAP (gamma-secretase activating protein, HGNC:28042) is a protein-coding gene on chromosome 7q11.23, encoding Gamma-secretase-activating protein (A4D1B5). Regulator of gamma-secretase activity, which specifically activates the production of amyloid-beta protein (amyloid-beta protein 40 and amyloid-beta protein 42), without affecting the cleavage of other gamma-secretase targets such has Notch.

Accumulation of neurotoxic amyloid-beta is a major hallmark of Alzheimer disease (AD; MIM 104300). Formation of amyloid-beta is catalyzed by gamma-secretase (see PSEN1; MIM 104311), a protease with numerous substrates. PION, or GSAP, selectively increases amyloid-beta production through a mechanism involving its interaction with both gamma-secretase and its substrate, the amyloid-beta precursor protein (APP; MIM 104760) C-terminal fragment (APP-CTF) (He et al., 2010 [PubMed 20811458]).

Source: NCBI Gene 54103 — RefSeq curated summary.

At a glance

• GWAS associations: 7
• Clinical variants (ClinVar): 149 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_017439

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:28042
Approved symbol	GSAP
Name	gamma-secretase activating protein
Location	7q11.23
Locus type	gene with protein product
Status	Approved
Aliases	LOC54103
Ensembl gene	ENSG00000186088
Ensembl biotype	protein_coding
OMIM	613552
Entrez	54103

Gene structure

Transcript identifiers

Ensembl transcripts: 15 — 6 retained_intron, 5 protein_coding, 4 protein_coding_CDS_not_defined

ENST00000257626, ENST00000334003, ENST00000415112, ENST00000426477, ENST00000430584, ENST00000434084, ENST00000440473, ENST00000441833, ENST00000449779, ENST00000474686, ENST00000482866, ENST00000489920, ENST00000491796, ENST00000880888, ENST00000943097

RefSeq mRNA: 7 — MANE Select: NM_017439 NM_001350896, NM_001350897, NM_001350898, NM_001350899, NM_001350900, NM_001350901, NM_017439

CCDS: CCDS34672

Canonical transcript exons

ENST00000257626 — 31 exons

Exon	Start	End
ENSE00001519751	77416213	77416349
ENSE00002146379	77330239	77330367
ENSE00003463013	77352944	77353026
ENSE00003464758	77353572	77353641
ENSE00003466933	77375058	77375101
ENSE00003473646	77360824	77360901
ENSE00003484003	77404559	77404615
ENSE00003485822	77387360	77387448
ENSE00003489812	77329333	77329391
ENSE00003495531	77396982	77397035
ENSE00003498848	77355555	77355647
ENSE00003499003	77320725	77320819
ENSE00003508758	77362583	77362660
ENSE00003525963	77349351	77349404
ENSE00003535668	77355213	77355430
ENSE00003539354	77374070	77374155
ENSE00003540359	77381305	77381354
ENSE00003550934	77326212	77326273
ENSE00003551131	77314370	77314489
ENSE00003573352	77376848	77376907
ENSE00003589443	77328606	77328637
ENSE00003590382	77311841	77311940
ENSE00003600572	77397346	77397415
ENSE00003604774	77382574	77382643
ENSE00003609174	77310751	77311449
ENSE00003629541	77313488	77313549
ENSE00003629595	77377286	77377390
ENSE00003645845	77321333	77321403
ENSE00003664100	77406029	77406105
ENSE00003670885	77323647	77323742
ENSE00003680988	77312101	77312202

Expression profiles

Bgee: expression breadth ubiquitous, 279 present calls, max score 96.09.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 8.3214 / max 237.7892, expressed in 1010 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
84462	8.2472	1007
84454	0.0579	20
84453	0.0162	8

Top tissues by expression

297 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
granulocyte	CL:0000094	96.09	gold quality
right uterine tube	UBERON:0001302	95.99	gold quality
monocyte	CL:0000576	95.45	gold quality
mononuclear cell	CL:0000842	95.45	gold quality
leukocyte	CL:0000738	95.08	gold quality
spleen	UBERON:0002106	94.20	gold quality
right lung	UBERON:0002167	93.16	gold quality
epithelium of nasopharynx	UBERON:0001951	92.80	gold quality
visceral pleura	UBERON:0002401	92.71	gold quality
right lobe of thyroid gland	UBERON:0001119	91.89	gold quality
secondary oocyte	CL:0000655	91.87	gold quality
upper lobe of left lung	UBERON:0008952	91.74	gold quality
left lobe of thyroid gland	UBERON:0001120	91.71	gold quality
upper lobe of lung	UBERON:0008948	91.54	gold quality
thyroid gland	UBERON:0002046	91.28	gold quality
lung	UBERON:0002048	91.05	gold quality
upper leg skin	UBERON:0004262	90.95	gold quality
pleura	UBERON:0000977	90.72	gold quality
pituitary gland	UBERON:0000007	90.22	gold quality
vermiform appendix	UBERON:0001154	90.22	gold quality
right lobe of liver	UBERON:0001114	89.99	gold quality
germinal epithelium of ovary	UBERON:0001304	89.96	gold quality
gall bladder	UBERON:0002110	89.93	gold quality
adenohypophysis	UBERON:0002196	89.84	gold quality
parietal pleura	UBERON:0002400	89.63	gold quality
small intestine Peyer’s patch	UBERON:0003454	89.63	gold quality
mucosa of stomach	UBERON:0001199	89.62	gold quality
lower lobe of lung	UBERON:0008949	89.59	gold quality
lymph node	UBERON:0000029	89.28	gold quality
bronchial epithelial cell	CL:0002328	88.90	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

39 targeting GSAP, 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-3120-5P	100.00	65.56	965
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-205-3P	99.92	69.92	3165
HSA-MIR-6885-3P	99.75	70.36	3187
HSA-MIR-8084	99.73	69.57	1760
HSA-MIR-6505-5P	99.73	69.25	1595
HSA-MIR-4422	99.72	72.07	2908
HSA-MIR-4255	99.72	67.70	1541
HSA-MIR-4677-5P	99.70	70.09	1940
HSA-MIR-379-3P	99.69	69.60	1524
HSA-MIR-411-3P	99.69	69.63	1524
HSA-MIR-10393-5P	99.65	68.01	1368
HSA-MIR-4328	99.57	71.06	4094
HSA-MIR-7844-5P	99.55	68.56	1428
HSA-MIR-5571-5P	99.49	66.99	1764
HSA-MIR-29A-5P	99.08	68.59	1813
HSA-MIR-4717-3P	99.06	66.34	1072
HSA-MIR-452-3P	99.01	66.25	1241
HSA-MIR-942-3P	98.81	69.04	876
HSA-MIR-519A-2-5P	98.78	71.74	1401
HSA-MIR-520B-5P	98.78	71.74	1401
HSA-MIR-1178-3P	98.57	67.09	890
HSA-MIR-3136-5P	98.53	67.68	793
HSA-MIR-4439	98.53	67.53	793
HSA-MIR-532-5P	98.43	67.53	760
HSA-MIR-4684-5P	98.29	67.99	1650
HSA-MIR-892B	98.00	67.11	821
HSA-MIR-4778-5P	97.96	68.06	1634
HSA-MIR-15A-3P	97.47	65.08	527

Literature-anchored findings (GeneRIF, showing 8)

• A gamma-secretase activating protein (GSAP) that selectively increases amyloid-beta production via interactions with both gamma-secretase and its substrate, the amyloid precursor protein carboxy-terminal fragment. (PMID:20811458)
• Aberrant regulation of gamma-secretase activating protein expression plays a key role in acceleration of gamma-cleavage of beta-secretase-cleaved C-terminal fragment of amyloid precursor protein and accumulation of Abeta in AD brains (PMID:21718343)
• Protocols for recombinant bacterial expression and purification of potentially important protein GSAP are not successful in generating soluble forms of GSAP that contain well-ordered and homogeneous tertiary structure. (PMID:22681044)
• gamma-secretase activating protein (GSAP) and imatinib have roles in the regulation of gamma-secretase activity and amyloid-beta generation (PMID:23209290)
• Its promoter variant contributes to Alzheimer’s disease liability. (PMID:25037285)
• GSAP cleavage via caspase-3 is regulated and depend upon the availability of 5-Lipoxygenase in Alzheimer’s disease. (PMID:26076991)
• These data demonstrate that GSAP proteins are differentially dysregulated in severe Alzheimer Disease, but only the full-length form was associated with cognitive test scores in Alzheimer Disease. (PMID:28743126)
• GSAP regulates lipid homeostasis and mitochondrial function associated with Alzheimer’s disease. (PMID:34156424)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	gsap	ENSDARG00000045481
mus_musculus	Gsap	ENSMUSG00000039934
rattus_norvegicus	Gsap	ENSRNOG00000028801
drosophila_melanogaster	pigeon	FBGN0010309

Protein

Protein identifiers

Gamma-secretase-activating protein — A4D1B5 (reviewed: A4D1B5)

Alternative names: Protein pigeon homolog

All UniProt accessions (3): A4D1B5, B7ZL33, H7C0Q7

UniProt curated annotations — full annotation on UniProt →

Function. Regulator of gamma-secretase activity, which specifically activates the production of amyloid-beta protein (amyloid-beta protein 40 and amyloid-beta protein 42), without affecting the cleavage of other gamma-secretase targets such has Notch. The gamma-secretase complex is an endoprotease complex that catalyzes the intramembrane cleavage of integral membrane proteins such as Notch receptors and APP (amyloid-beta precursor protein). Specifically promotes the gamma-cleavage of APP CTF-alpha (also named APP-CTF) by the gamma-secretase complex to generate amyloid-beta, while it reduces the epsilon-cleavage of APP CTF-alpha, leading to a low production of AICD.

Subunit / interactions. Interacts with APP; specifically interacts with the CTF-alpha product of APP. Interacts with the gamma-secretase complex.

Subcellular location. Golgi apparatus. trans-Golgi network.

Tissue specificity. Widely expressed.

Post-translational modifications. The protein is first synthesized as a holoprotein form of 98 kDa and rapidly processed into the gamma-secretase-activating protein 16 kDa C-terminal form, which constitutes the predominant form.

Miscellaneous. The gamma-secretase regulator activity is specifically inhibited by imatinib (also known as STI571 or Gleevec), an anticancer drug that selectively decreases amyloid-beta protein production. Imatinib binds PION/GSAP and acts by preventing PION/GSAP interaction with the gamma-secretase substrate, CTF-alpha. Its role as an activator of amyloid-beta protein production makes it a promising therapeutic target for the treatment of Alzheimer disease.

Similarity. Belongs to the GSAP family.

Isoforms (4)

UniProt ID	Names	Canonical?
A4D1B5-1	1	yes
A4D1B5-2	2
A4D1B5-3	3
A4D1B5-4	4

RefSeq proteins (7): NP_001337825, NP_001337826, NP_001337827, NP_001337828, NP_001337829, NP_001337830, NP_059135* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR026172	GSAP_fam	Family
IPR028010	GSAP_C_dom	Domain

Pfam: PF14959

UniProt features (10 total): splice variant 4, sequence variant 4, chain 2

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-A4D1B5-F1	80.78	0.28

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 261 (showing top): BROWNE_HCMV_INFECTION_30MIN_DN, BROWNE_HCMV_INFECTION_6HR_DN, BASSO_B_LYMPHOCYTE_NETWORK, GOBP_POSITIVE_REGULATION_OF_AMIDE_METABOLIC_PROCESS, GOBP_REGULATION_OF_AMYLOID_PRECURSOR_PROTEIN_CATABOLIC_PROCESS, GOCC_TRANS_GOLGI_NETWORK, DEURIG_T_CELL_PROLYMPHOCYTIC_LEUKEMIA_DN, GOBP_AMIDE_METABOLIC_PROCESS, RIGGI_EWING_SARCOMA_PROGENITOR_DN, VANHARANTA_UTERINE_FIBROID_DN, GOBP_REGULATION_OF_AMIDE_METABOLIC_PROCESS, GOBP_AMYLOID_PRECURSOR_PROTEIN_METABOLIC_PROCESS, chr7q11, GNF2_PTPRC, HAN_SATB1_TARGETS_DN

GO Biological Process (2): regulation of proteolysis (GO:0030162), positive regulation of amyloid-beta formation (GO:1902004)

GO Molecular Function (2): amyloid-beta binding (GO:0001540), protein binding (GO:0005515)

GO Cellular Component (2): trans-Golgi network (GO:0005802), Golgi apparatus (GO:0005794)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
proteolysis	1
regulation of protein metabolic process	1
amyloid-beta formation	1
regulation of amyloid-beta formation	1
positive regulation of amyloid precursor protein catabolic process	1
peptide binding	1
binding	1
Golgi apparatus subcompartment	1
cytoplasm	1
endomembrane system	1
intracellular membrane-bounded organelle	1

Protein interactions and networks

STRING

579 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
GSAP	PSEN1	P49768	845
GSAP	APP	P05067	827
GSAP	PSENEN	Q9NZ42	770
GSAP	NCSTN	Q92542	762
GSAP	APH1A	Q96BI3	757
GSAP	BSG	P35613	638
GSAP	TMED10	P49755	630
GSAP	APBB1	O00213	518
GSAP	TPPP	O94811	490
GSAP	RHBDL2	Q9NX52	455
GSAP	MRPL15	Q9P015	455
GSAP	UPK1B	O75841	450
GSAP	BACE1	P56817	439
GSAP	APH1B	Q8WW43	425
GSAP	A0A0J9YYB4	A0A0J9YYB4	417

IntAct

4 interactions, top by confidence:

A	B	Type	Score
GSAP	APP	psi-mi:“MI:0915”(physical association)	0.400

BioGRID (9): PSEN1 (Affinity Capture-Western), PSENEN (Affinity Capture-Western), NCSTN (Affinity Capture-Western), APP (Affinity Capture-Western), GSAP (Affinity Capture-Western), APP (Biochemical Activity), APP (PCA), HSP90B1 (Proximity Label-MS), GSAP (Cross-Linking-MS (XL-MS))

ESM2 similar proteins: A2RRP1, A4D1B5, E1BGH8, O43149, O88480, P53995, Q12769, Q13129, Q13315, Q3MHH2, Q3TCV3, Q3TUL7, Q3UHA3, Q3UPC7, Q3URV1, Q402B2, Q4R7B1, Q4R9E9, Q5H9S7, Q5RB52, Q5SSH7, Q5ZL79, Q5ZLS8, Q62388, Q63517, Q6P2C0, Q6TNU3, Q86VV8, Q8BJW5, Q8CE72, Q8IV33, Q8K1K4, Q8K2A7, Q8NB91, Q8NG48, Q8R4Y8, Q8TEL6, Q91VB4, Q920I9, Q92674

Diamond homologs: A4D1B5, Q3TCV3

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

149 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	98
Likely benign	14
Benign	2

Top pathogenic / likely-pathogenic (0)

SpliceAI

4936 predictions. Top by Δscore:

Variant	Effect	Δscore
7:77311445:CAGGG:C	acceptor_gain	1.0000
7:77312199:TAAG:T	acceptor_gain	1.0000
7:77312208:A:C	acceptor_gain	1.0000
7:77320720:CTTA:C	donor_loss	1.0000
7:77320722:TACCA:T	donor_loss	1.0000
7:77320723:ACCAG:A	donor_loss	1.0000
7:77320815:TATTG:T	acceptor_gain	1.0000
7:77320817:TTG:T	acceptor_gain	1.0000
7:77320820:C:CC	acceptor_gain	1.0000
7:77320824:G:C	acceptor_gain	1.0000
7:77320824:G:GC	acceptor_gain	1.0000
7:77326204:CCA:C	donor_gain	1.0000
7:77326207:CTTA:C	donor_loss	1.0000
7:77326209:TACCA:T	donor_loss	1.0000
7:77326210:A:AC	donor_gain	1.0000
7:77326210:A:C	donor_loss	1.0000
7:77326210:ACCAG:A	donor_gain	1.0000
7:77326211:C:CC	donor_gain	1.0000
7:77326211:CCAG:C	donor_gain	1.0000
7:77326211:CCAGC:C	donor_gain	1.0000
7:77326271:GCC:G	acceptor_gain	1.0000
7:77326272:CC:C	acceptor_gain	1.0000
7:77326272:CCC:C	acceptor_gain	1.0000
7:77326272:CCCTG:C	acceptor_loss	1.0000
7:77326273:CC:C	acceptor_gain	1.0000
7:77326274:C:CC	acceptor_gain	1.0000
7:77329331:A:AC	donor_gain	1.0000
7:77329332:C:CC	donor_gain	1.0000
7:77353042:T:C	acceptor_gain	1.0000
7:77353042:T:TC	acceptor_gain	1.0000

AlphaMissense

5654 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
7:77377327:A:G	W214R	0.995
7:77377327:A:T	W214R	0.995
7:77397028:A:C	S107R	0.994
7:77397028:A:T	S107R	0.994
7:77397030:T:G	S107R	0.994
7:77377336:A:G	W211R	0.991
7:77377336:A:T	W211R	0.991
7:77397348:A:G	L104P	0.991
7:77382641:A:C	F153L	0.990
7:77382641:A:T	F153L	0.990
7:77382643:A:G	F153L	0.990
7:77397035:G:T	A105D	0.988
7:77382597:A:G	L168P	0.987
7:77382642:A:G	F153S	0.986
7:77312175:A:G	W767R	0.985
7:77312175:A:T	W767R	0.985
7:77314485:A:C	F698L	0.985
7:77314485:A:T	F698L	0.985
7:77314487:A:G	F698L	0.985
7:77397377:A:C	S94R	0.985
7:77397377:A:T	S94R	0.985
7:77397379:T:G	S94R	0.985
7:77330346:A:G	W523R	0.984
7:77330346:A:T	W523R	0.984
7:77323729:A:G	L614P	0.982
7:77377325:C:A	W214C	0.982
7:77377325:C:G	W214C	0.982
7:77397365:G:C	N98K	0.982
7:77397365:G:T	N98K	0.982
7:77387427:A:G	L130S	0.981

dbSNP variants (sampled 300 via entrez): RS1000009606 (7:77381365 AAAACAAAG>A), RS1000015116 (7:77353170 T>G), RS1000037356 (7:77414613 C>A), RS1000046717 (7:77394411 T>C), RS1000149616 (7:77386712 G>C,T), RS1000176532 (7:77413179 A>C), RS1000185040 (7:77371340 G>C), RS1000189226 (7:77403232 G>A), RS1000191115 (7:77339197 A>C), RS1000224701 (7:77312357 T>C,G), RS1000236424 (7:77359097 G>A), RS1000269765 (7:77391660 CA>C,CAA), RS1000285995 (7:77346862 G>A), RS1000345259 (7:77383293 C>G,T), RS1000364891 (7:77397196 T>C)

Disease associations

OMIM: gene MIM:613552 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

7 associations (top):

Study	Trait	p-value
GCST003628_4	Clozapine-induced agranulocytosis/granulocytopenia in treatment-resistant schizophrenia	2.000000e-06
GCST005024_97	Pursuit maintenance gain	4.000000e-06
GCST005038_116	Allergic disease (asthma, hay fever or eczema)	2.000000e-13
GCST007216_9	Crohn’s disease	7.000000e-06
GCST010042_86	Asthma	3.000000e-08
GCST010043_157	Asthma	1.000000e-08
GCST010577_18	Crohn’s disease	3.000000e-06

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0008433	pursuit maintenance gain measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL3638343 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 756 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1770916	NIROGACESTAT	4	756

PharmGKB: 1 entry (VIP=true, CPIC=false)

Binding affinities (BindingDB)

2 measured of 2 human assays (2 total across all organisms); most potent 2 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
N-[13-[(5-chlorothiophen-2-yl)sulfonylamino]-5-tricyclo[8.2.1.03,8]trideca-3(8),4,6-trienyl]-2-(4-fluorophenoxy)acetamide	IC50	1 nM	US-9023767: γ-Secretase substrates and methods of use
2-[[2-(3,5-difluorophenyl)acetyl]amino]-N-(1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl)propanamide	IC50	1.2 nM	US-9023767: γ-Secretase substrates and methods of use

ChEMBL bioactivities

3 potent at pChembl≥5 of 3 total, top 3 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.00	IC50	1	nM	CHEMBL3703681
8.92	IC50	1.2	nM	CHEMBL3703680
8.21	IC50	6.2	nM	NIROGACESTAT

PubChem BioAssay actives

1 with measured affinity, of 1 total; 1 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
Nirogacestat	1924179: Inhibition of human gamma secretase by western blot assay	ic50	0.0062	uM

CTD chemical–gene interactions

43 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects cotreatment, decreases expression, affects expression, decreases methylation, increases expression	6
(+)-JQ1 compound	decreases expression, increases expression	3
bisphenol A	affects cotreatment, decreases methylation, affects expression	2
Vorinostat	affects cotreatment, decreases expression	2
Cisplatin	affects cotreatment, increases expression	2
Estradiol	affects cotreatment, decreases expression	2
Tetrachlorodibenzodioxin	decreases expression	2
Tretinoin	decreases expression, increases expression	2
Cyclosporine	increases expression, decreases expression	2
aristolochic acid I	decreases expression	1
dicrotophos	decreases expression	1
methylmercuric chloride	decreases expression	1
triphenyl phosphate	affects expression	1
trichostatin A	decreases expression, increases expression	1
tris(1,3-dichloro-2-propyl)phosphate	increases expression	1
cobaltous chloride	decreases expression	1
butyraldehyde	decreases expression	1
potassium chromate(VI)	affects cotreatment, decreases expression	1
diallyl trisulfide	increases expression	1
epigallocatechin gallate	affects cotreatment, decreases expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, decreases expression	1
dorsomorphin	affects cotreatment, decreases expression	1
MRK 003	decreases expression	1
jinfukang	affects cotreatment, increases expression	1
Resveratrol	affects cotreatment, increases expression	1
Sunitinib	decreases expression	1
Fulvestrant	decreases methylation, affects cotreatment	1
Leflunomide	decreases expression	1
Acetaminophen	decreases expression	1
Air Pollutants	increases abundance, increases expression	1

ChEMBL screening assays

2 unique, capped per target: 2 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL3705978	Binding	HTRF Biochemical Assay: Among the advantages of this Abeta 42 HTRF gamma-secretase assay is the construction of the biotinylated, recombinant CT6-I45F substrate, which has provided a highly active substrate allowing for increased sensitivit	Œ=-Secretase substrates and methods of use

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.