Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTB2MXP)

• DTT Name: Angiotensinogenase renin (REN)
• Synonyms: Renin; Angiotensinogenase
• Gene Name: REN
• DTT Type: Successful target; [1]
• Related Disease: Hypertension [ICD-11: BA00-BA04]
• BioChemical Class: Peptidase
• UniProt ID: RENI_HUMAN
• TTD ID: T61622
• EC Number: EC 3.4.23.15
• Sequence:
  MDGWRRMPRWGLLLLLWGSCTFGLPTDTTTFKRIFLKRMPSIRESLKERGVDMARLGPEW
  SQPMKRLTLGNTTSSVILTNYMDTQYYGEIGIGTPPQTFKVVFDTGSSNVWVPSSKCSRL
  YTACVYHKLFDASDSSSYKHNGTELTLRYSTGTVSGFLSQDIITVGGITVTQMFGEVTEM
  PALPFMLAEFDGVVGMGFIEQAIGRVTPIFDNIISQGVLKEDVFSFYYNRDSENSQSLGG
  QIVLGGSDPQHYEGNFHYINLIKTGVWQIQMKGVSVGSSTLLCEDGCLALVDTGASYISG
  STSSIEKLMEALGAKKRLFDYVVKCNEGPTLPDISFHLGGKEYTLTSADYVFQESYSSKK
  LCTLAIHAMDIPPPTGPTWALGATFIRKFYTEFDRRNNRIGFALAR
• Function: Renin is a highly specific endopeptidase, whose only knownfunction is to generate angiotensin I from angiotensinogen in the plasma, initiating a cascade of reactions that produce an elevation of blood pressure and increased sodium retention by the kidney.
• Reactome Pathway: Metabolism of Angiotensinogen to Angiotensins (R-HSA-2022377)

Molecular Interaction Atlas (MIA) of This DTT

2 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Aliskiren	DM1BV7W	Hypertension	BA00-BA04	Approved	[1]
Remikiren	DMNAKLY	Hypertension	BA00-BA04	Approved	[2]

7 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CP-80794	DMT3ORQ	Hypertension	BA00-BA04	Phase 2	[3]
SPP-600	DMOVQP8	Hypertension	BA00-BA04	Phase 2	[4]
SR-43845	DMTOCIV	Glaucoma/ocular hypertension	9C61	Phase 2	[5], [6]
TAK-272	DM81UAZ	Type-2 diabetes	5A11	Phase 2	[7]
ACT-178882	DMOZ3AT	Cardiovascular disease	BA00-BE2Z	Phase 1	[8]
CARD-024	DM4SNK8	Cardiovascular disease	BA00-BE2Z	Phase 1	[9]
VTP-27999	DMQEOD6	Hypertension	BA00-BA04	Phase 1	[10]

15 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Enalkiren	DMDAS5B	Glaucoma/ocular hypertension	9C61	Discontinued in Phase 2	[11]
FK-906	DMTEW80	Hypertension	BA00-BA04	Discontinued in Phase 2	[12]
ZANKIREN	DM9F650	Hypertension	BA00-BA04	Discontinued in Phase 2	[13]
RS-8891	DM4P5WO	Hypertension	BA00-BA04	Discontinued in Phase 1	[14]
SPP-1148	DMWQKEN	Hypertension	BA00-BA04	Discontinued in Phase 1	[10]
SPP-676	DMKEHGT	Hypertension	BA00-BA04	Discontinued in Phase 1	[10]
A-74273	DMBEIFL	Hypertension	BA00-BA04	Terminated	[15]
BILA-2157BS	DMRV4UL	Hypertension	BA00-BA04	Terminated	[16]
Ciprokiren	DM0NJMG	Hypertension	BA00-BA04	Terminated	[17]
ES-1005	DMRP7BX	Hypertension	BA00-BA04	Terminated	[18]
JTP-2724	DMG7B61	Hypertension	BA00-BA04	Terminated	[19]
JTP-4761	DM6TXKR	Hypertension	BA00-BA04	Terminated	[20]
KRI-1314	DM4QHNG	Hypertension	BA00-BA04	Terminated	[21]
SC-56525	DM25MUA	Hypertension	BA00-BA04	Terminated	[22]
SQ-33800	DMMRWKP	Hypertension	BA00-BA04	Terminated	[23]

27 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(H-261)Boc-His-Pro-Phe-His-Leu(OH)-Val-Ile-His-OH	DMVKJ0H	Discovery agent	N.A.	Investigative	[24]
1-Hydroxy-2-Amino-3-Cyclohexylpropane	DM9EWN8	Discovery agent	N.A.	Investigative	[25]
1-Hydroxy-3-Methylbutane	DMZ8IL9	Discovery agent	N.A.	Investigative	[25]
1-Methyl-2-Oxy-5,5-Dimethyl Pyrrolidine	DM5GELS	Discovery agent	N.A.	Investigative	[25]
2-Cyclopropylmethylenepropanal	DM0W2QB	Discovery agent	N.A.	Investigative	[25]
2-Methyl-3-(2-Aminothiazolo)Propanal	DM3DNFQ	Discovery agent	N.A.	Investigative	[26]
3-Phenyl-1,2-Propandiol	DMU9WGT	Discovery agent	N.A.	Investigative	[25]
CP-305202	DMME6K2	Discovery agent	N.A.	Investigative	[27]
Dimethylformamide	DML6O4N	Discovery agent	N.A.	Investigative	[28]
ES-6864	DMSNM5O	Hypertension	BA00-BA04	Investigative	[29], [6]
Glu-Trp-Pro-Arg-Pro-Gln-Ile-Pro-Pro	DM1Q83B	Discovery agent	N.A.	Investigative	[30]
Iva-His-Pro-Phe-His-ACHPA-Leu-Phe-NH2	DMFMYIH	Discovery agent	N.A.	Investigative	[31]
Iva-His-Pro-Phe-His-AHPPA-Leu-Phe-NH2	DMZTIU3	Discovery agent	N.A.	Investigative	[31]
Iva-His-Pro-Phe-His-Sta-Leu-Phe-NH2	DM92QIW	Discovery agent	N.A.	Investigative	[31]
JT-2724	DMD9W0B	Discovery agent	N.A.	Investigative	[32]
N-Methyl-N-(Methylbenzyl)Formamide	DMYPEX3	Discovery agent	N.A.	Investigative	[26]
PP1-Pro-Phe-N-MeHis-LVA-Ile-Amp-(O)	DMYA5CB	Discovery agent	N.A.	Investigative	[33]
PP2-Pro-Phe-N-MeHis-LVA-Ile-Amp-(O)	DM3NUKX	Discovery agent	N.A.	Investigative	[33]
Pro-His-Pro-His-Leu-Phe-Val-Tyr	DMZH0KY	Discovery agent	N.A.	Investigative	[30]
Pro-His-Pro-His-Phe-Phe-Val-Tyr	DMD3WVO	Discovery agent	N.A.	Investigative	[30]
Pro-His-Pro-His-Phe-Phe-Val-Tyr-Lys	DMNDUI3	Discovery agent	N.A.	Investigative	[30]
Pro-His-Pro-Phe-His-Leu(CH2NH)Val-Ile-His-Lys	DM26VFX	Discovery agent	N.A.	Investigative	[34]
Ro-65-7219	DM6S742	Discovery agent	N.A.	Investigative	[27]
Ro-66-1168	DMPT01J	Discovery agent	N.A.	Investigative	[13]
SPP-800	DMP5VN2	Hypertension	BA00-BA04	Investigative	[9]
Sul-Pro-Phe-N-MeHis-LVA-Ile-Amp	DMTEU0L	Discovery agent	N.A.	Investigative	[33]
Sul-Pro-Phe-N-MeHis-LVA-Ile-Amp-(O)	DMQB2CN	Discovery agent	N.A.	Investigative	[33]

References

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