Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTG4R8V)

• DTT Name: Growth hormone-releasing hormone receptor (GHRHR)
• Synonyms: GRFR; GRF receptor; GHRHR; GHRH receptor
• Gene Name: GHRHR
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR secretin
• UniProt ID: GHRHR_HUMAN
• TTD ID: T70449
• Sequence:
  MDRRMWGAHVFCVLSPLPTVLGHMHPECDFITQLREDESACLQAAEEMPNTTLGCPATWD
  GLLCWPTAGSGEWVTLPCPDFFSHFSSESGAVKRDCTITGWSEPFPPYPVACPVPLELLA
  EEESYFSTVKIIYTVGHSISIVALFVAITILVALRRLHCPRNYVHTQLFTTFILKAGAVF
  LKDAALFHSDDTDHCSFSTVLCKVSVAASHFATMTNFSWLLAEAVYLNCLLASTSPSSRR
  AFWWLVLAGWGLPVLFTGTWVSCKLAFEDIACWDLDDTSPYWWIIKGPIVLSVGVNFGLF
  LNIIRILVRKLEPAQGSLHTQSQYWRLSKSTLFLIPLFGIHYIIFNFLPDNAGLGIRLPL
  ELGLGSFQGFIVAILYCFLNQEVRTEISRKWHGHDPELLPAWRTRAKWTTPSRSAAKVLT
  SMC
• Function: Receptor for GRF,coupled to G proteins which activate adenylyl cyclase. Stimulates somatotroph cell growth, growth hormone gene transcription and growth hormone secretion.
• KEGG Pathway: Neuroactive ligand-receptor interaction (hsa04080)
• Reactome Pathway:
  Glucagon-type ligand receptors (R-HSA-420092)
  G alpha (s) signalling events (R-HSA-418555)

Molecular Interaction Atlas (MIA) of This DTT

2 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sermorelin	DM25HP1	Pediatric growth disorder	FB86	Approved	[2]
Tesamorelin	DM9GP85	HIV-associated lipodystrophy	1C62.1	Approved	[1]

4 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AKL-0707	DME6OXB	Lipodystrophy	EF01	Discontinued in Phase 2	[3]
Examorelin	DMGJMQH	Growth hormone deficiency	5A61.3	Discontinued in Phase 2	[4]
L-692429	DMLHE5A	Growth hormone deficiency	5A61.3	Discontinued in Phase 1	[5]
NNC-26-0762	DMLTYFI	Growth hormone deficiency	5A61.3	Terminated	[6]

1 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Mutated growth hormone	DMAY50R	Acromegaly	5A60.0	Investigative	[7]

References

• [1] Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
• [2] Sermorelin: a better approach to management of adult-onset growth hormone insufficiency Clin Interv Aging. 2006;1(4):307-8.
• [3] A super-agonist of growth hormone-releasing hormone causes rapid improvement of nutritional status in patients with chronic kidney disease. Kidney Int. 2010 Mar;77(5):450-8.
• [4] Hexarelin is a stronger GH-releasing peptide than GHRH in normal cycling women but not in anorexia nervosa. J Endocrinol Invest. 1997 May;20(5):257-63.
• [5] Nonpeptide and peptide growth hormone secretagogues act both as ghrelin receptor agonist and as positive or negative allosteric modulators of ghrel... Mol Endocrinol. 2005 Sep;19(9):2400-11.
• [6] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010046)
• [7] Treatment strategies for acromegaly. Expert Opin Emerg Drugs. 2005 Nov;10(4):875-90.