Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTEPJL5)

• DTT Name: Parathyroid hormone receptor (PTH2R)
• Synonyms: PTHR2; PTH2R; PTH2 receptor
• Gene Name: PTH2R
• DTT Type: Clinical trial target; [1]
• BioChemical Class: GPCR secretin
• UniProt ID: PTH2R_HUMAN
• TTD ID: T22032
• Sequence:
  MAGLGASLHVWGWLMLGSCLLARAQLDSDGTITIEEQIVLVLKAKVQCELNITAQLQEGE
  GNCFPEWDGLICWPRGTVGKISAVPCPPYIYDFNHKGVAFRHCNPNGTWDFMHSLNKTWA
  NYSDCLRFLQPDISIGKQEFFERLYVMYTVGYSISFGSLAVAILIIGYFRRLHCTRNYIH
  MHLFVSFMLRATSIFVKDRVVHAHIGVKELESLIMQDDPQNSIEATSVDKSQYIGCKIAV
  VMFIYFLATNYYWILVEGLYLHNLIFVAFFSDTKYLWGFILIGWGFPAAFVAAWAVARAT
  LADARCWELSAGDIKWIYQAPILAAIGLNFILFLNTVRVLATKIWETNAVGHDTRKQYRK
  LAKSTLVLVLVFGVHYIVFVCLPHSFTGLGWEIRMHCELFFNSFQGFFVSIIYCYCNGEV
  QAEVKKMWSRWNLSVDWKRTPPCGSRRCGSVLTTVTHSTSSQSQVAASTRMVLISGKAAK
  IASRQPDSHITLPGYVWSNSEQDCLPHSFHEETKEDSGRQGDDILMEKPSRPMESNPDTE
  GCQGETEDVL
• Function: This is a specific receptor for parathyroid hormone. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase. PTH2R may be responsible for PTH effects in a number of physiological systems. It may play asignificant role in pancreatic function. PTH2R presence in neurons indicates that it may function as a neurotransmitter receptor.
• KEGG Pathway: Neuroactive ligand-receptor interaction (hsa04080)
• Reactome Pathway:
  G alpha (s) signalling events (R-HSA-418555)
  Class B/2 (Secretin family receptors) (R-HSA-373080)

Molecular Interaction Atlas (MIA) of This DTT

5 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BA-058	DMPV6B2	Osteoporosis	FB83.0	Phase 3	[1]
GSK768974	DMIEXUM	Osteoporosis	FB83.0	Phase 2	[2]
NPSP-795	DM3DQXG	Osteoporosis	FB83.0	Phase 2	[3]
UNI-PH (1-34)	DM8LBUK	Osteoporosis	FB83.0	Phase 2	[4]
PTH(7-34) liposomal cream	DMRQ5YT	Alopecia	ED70	Phase 1	[5]

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Semparatide	DMLK605	Osteoporosis	FB83.0	Discontinued in Phase 2	[6]

5 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BB-PTH 1-84	DM85AJ4	Osteoporosis	FB83.0	Investigative	[3]
Hemoparatide	DMF7X31	Discovery agent	N.A.	Investigative	[7]
PTHr pepducins	DM10KIW	Endocrine disease	5B3Z	Investigative	[3]
SDZ-PTS-893	DMBYSEM	Discovery agent	N.A.	Investigative	[8]
ZP-2307	DM8WRAU	Osteoporosis	FB83.0	Investigative	[3]

References

• [1] Emerging therapies for the treatment of osteoporosis. J Midlife Health. 2013 Jul-Sep; 4(3): 147-152.
• [2] Comparison of bone formation responses to parathyroid hormone(1-34), (1-31), and (2-34) in mice. Bone. 2000 Oct;27(4):471-8.
• [3] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 332).
• [4] Parathyroid hormone for the treatment of osteoporosis: a systematic review. CMAJ. 2006 July 4; 175(1): 52-59.
• [5] Differential effects of intermittent PTH(1-34) and PTH(7-34) on bone microarchitecture and aortic calcification in experimental renal failure. Bone. 2008 Dec;43(6):1022-30.
• [6] Quantitative cell membrane-based radioligand binding assays for parathyroid hormone receptors. J Pharmacol Toxicol Methods. 1999 Apr-Jun;41(2-3):83-90.
• [7] The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.
• [8] Long-term therapy of ovariectomy-induced osteopenia with parathyroid hormone analog SDZ PTS 893 and bone maintenance in retired breeder rats. Bone. 1999 Nov;25(5):561-9.