Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OT1Y8ARK)

DOT Name	Growth hormone secretagogue receptor type 1 (GHSR)
Synonyms	GHS-R; GH-releasing peptide receptor; GHRP; Ghrelin receptor
Gene Name	GHSR
Related Disease	Short stature due to GHSR deficiency ( )
UniProt ID	GHSR_HUMAN
3D Structure	Download 2D Sequence (FASTA) Download 3D Structure (PDB) Download
PDB ID	6KO5; 7F9Y; 7F9Z; 7NA7; 7NA8; 7W2Z
Pfam ID	PF00001
Sequence	MWNATPSEEPGFNLTLADLDWDASPGNDSLGDELLQLFPAPLLAGVTATCVALFVVGIAG NLLTMLVVSRFRELRTTTNLYLSSMAFSDLLIFLCMPLDLVRLWQYRPWNFGDLLCKLFQ FVSESCTYATVLTITALSVERYFAICFPLRAKVVVTKGRVKLVIFVIWAVAFCSAGPIFV LVGVEHENGTDPWDTNECRPTEFAVRSGLLTVMVWVSSIFFFLPVFCLTVLYSLIGRKLW RRRRGDAVVGASLRDQNHKQTVKMLAVVVFAFILCWLPFHVGRYLFSKSFEPGSLEIAQI SQYCNLVSFVLFYLSAAINPILYNIMSKKYRVAVFRLLGFEPFSQRKLSTLKDESSRAWT ESSINT
Function	Receptor for ghrelin, coupled to G-alpha-11 proteins. Stimulates growth hormone secretion. Binds also other growth hormone releasing peptides (GHRP) (e.g. Met-enkephalin and GHRP-6) as well as non-peptide, low molecular weight secretagogues (e.g. L-692,429, MK-0677, adenosine).
Tissue Specificity	Pituitary and hypothalamus.
KEGG Pathway	cAMP sig.ling pathway (hsa04024 ) Neuroactive ligand-receptor interaction (hsa04080 ) Growth hormone synthesis, secretion and action (hsa04935 )
Reactome Pathway	G alpha (q) signalling events (R-HSA-416476 ) Peptide ligand-binding receptors (R-HSA-375276 )

Molecular Interaction Atlas (MIA) of This DOT

1 Disease(s) Related to This DOT

Disease Name	Disease ID	Evidence Level	Mode of Inheritance		REF
Short stature due to GHSR deficiency	DISOSN3Q	Moderate	Semidominant	[1]
------------------------------------------------------------------------------------

Molecular Interaction Atlas (MIA)

Jump to Detail Molecular Interaction Atlas of This DOT

3 Drug(s) Affected the Gene/Protein Processing of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
DTI-015	DMXZRW0	Approved	DTI-015 decreases the expression of Growth hormone secretagogue receptor type 1 (GHSR).	[2]
Zithromax	DMN4H2O	Approved	Zithromax increases the expression of Growth hormone secretagogue receptor type 1 (GHSR).	[3]
AHPN	DM8G6O4	Investigative	AHPN decreases the expression of Growth hormone secretagogue receptor type 1 (GHSR).	[5]
------------------------------------------------------------------------------------

1 Drug(s) Affected the Post-Translational Modifications of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene increases the methylation of Growth hormone secretagogue receptor type 1 (GHSR).	[4]
------------------------------------------------------------------------------------

References

1	Classification of Genes: Standardized Clinical Validity Assessment of Gene-Disease Associations Aids Diagnostic Exome Analysis and Reclassifications. Hum Mutat. 2017 May;38(5):600-608. doi: 10.1002/humu.23183. Epub 2017 Feb 13.
2	Gene expression profile induced by BCNU in human glioma cell lines with differential MGMT expression. J Neurooncol. 2005 Jul;73(3):189-98.
3	The comparative analysis of gastrointestinal toxicity of azithromycin and 3'-decladinosyl azithromycin on zebrafish larvae. Toxicol Appl Pharmacol. 2023 Jun 15;469:116529. doi: 10.1016/j.taap.2023.116529. Epub 2023 Apr 24.
4	Air pollution and DNA methylation alterations in lung cancer: A systematic and comparative study. Oncotarget. 2017 Jan 3;8(1):1369-1391. doi: 10.18632/oncotarget.13622.
5	ST1926, a novel and orally active retinoid-related molecule inducing apoptosis in myeloid leukemia cells: modulation of intracellular calcium homeostasis. Blood. 2004 Jan 1;103(1):194-207.