Therapeutic Targets Database
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TTD Target ID: TTDS00451

Target Information
NameRenin, renal    
Type of targetSuccessful target    
SynonymsAngiotensinogenase    
Renin    
DiseaseCancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[1]
Hypertension
[ICD9: 401   ICD10: I10, I11, I12, I13, I15]
[2]
Drug(s)AliskirenApprovedHypertension[3]
RemikirenApprovedHypertension[4]
TAK-272Phase IHypertension
BioChemical ClassHydrolases acting on peptide bonds (Peptidases)    
EC NumberEC 3.4.23.15
PathwayRenin-angiotensin system
UniProt IDP00797
PDB Structure1BBS; 1BIL; 1BIM; 1HRN; 1RNE; 2BKS; 2BKT; 2FS4; 2G1N; 2G1O; 2G1R; 2G1S; 2G1Y; 2G20; 2G21; 2G22; 2G24; 2G26; 2G27; 2I4Q; 2IKO; 2IKU; 2IL2; 2REN; 2V0Z; 2V10; 2V11; 2V12; 2V13; 2V16; 2X0B; 3D91; 3G6Z; 3G70; 3G72; 3GW5; 3K1W; 3KM4; 3O9L; 3OAD; 3OAG; 3OOT; 3OQF; 3OQK; 3OWN; 3Q3T; 3Q4B; 3Q5H; 3SFC; 3VCM; 3VSW; 3VSX; 3VUC; 3VYD; 3VYE; 3VYF; 4AMT; 4GJ5; 4GJ6; 4GJ7; 4GJ8; 4GJ9; 4GJA; 4GJB; 4GJC; 4GJD.    
FunctionRenin is a highly specific endopeptidase, whose only known function 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.    
SequenceMDGWRRMPRWGLLLLLWGSCTFGLPTDTTTFKRIFLKRMPSIRESLKERGVDMARLGPEW SQPMKRLTLGNTTSSVILTNYMDTQYYGEIGIGTPPQTFKVVFDTGSSNVWVPSSKCSRL YTACVYHKLFDASDSSSYKHNGTELTLRYSTGTVSGFLSQDIITVGGITVTQMFGEVTEM PALPFMLAEFDGVVGMGFIEQAIGRVTPIFDNIISQGVLKEDVFSFYYNRDSENSQSLGG QIVLGGSDPQHYEGNFHYINLIKTGVWQIQMKGVSVGSSTLLCEDGCLALVDTGASYISG STSSIEKLMEALGAKKRLFDYVVKCNEGPTLPDISFHLGGKEYTLTSADYVFQESYSSKK LCTLAIHAMDIPPPTGPTWALGATFIRKFYTEFDRRNNRIGFALAR
Related US Patent6,376,672
6,673,931
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor (H-261)Boc-His-Pro-Phe-His-Leu[5]
1-Hydroxy-2-Amino-3-Cyclohexylpropane[6]
1-Hydroxy-3-Methylbutane[6]
1-Methyl-2-Oxy-5,5-Dimethyl Pyrrolidine[6]
2-Cyclopropylmethylenepropanal[6]
2-Methyl-3- (2-Aminothiazolo)Propanal[7]
3-Phenyl-1,2-Propandiol[6]
Aliskiren[3]
CP-305202[8]
CP-80794[9]
Dimethylformamide[10]
Enalkiren[11]
Enalkiren[12]
Glu-Trp-Pro-Arg-Pro-Gln-Ile-Pro-Pro[13]
Iva-His-Pro-Phe-His-ACHPA-Leu-Phe-NH2[14]
Iva-His-Pro-Phe-His-AHPPA-Leu-Phe-NH2[14]
Iva-His-Pro-Phe-His-Sta-Leu-Phe-NH2[14]
N-Methyl-N- (Methylbenzyl)Formamide[7]
PEPSTATIN A[15]
PP1-Pro-Phe-N-MeHis-LVA-Ile-Amp- (O)[16]
PP2-Pro-Phe-N-MeHis-LVA-Ile-Amp- (O)[16]
Pro-His-Pro-His-Leu-Phe-Val-Tyr[13]
Pro-His-Pro-His-Phe-Phe-Val-Tyr[13]
Pro-His-Pro-His-Phe-Phe-Val-Tyr-Lys[13]
Pro-His-Pro-Phe-His-Leu (CH2NH)Val-Ile-His-Lys[17]
Remikiren[4]
Ro-65-7219[8]
Ro-66-1168[18]
Ro-66-1168[8]
Sul-Pro-Phe-N-MeHis-LVA-Ile-Amp[16]
Sul-Pro-Phe-N-MeHis-LVA-Ile-Amp- (O)[16]
ZANKIREN[18]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Renin inhibition: a new approach to cardiovascular therapy. J Clin Pharmacol. 1994 Sep;34(9):873-80. To Reference
Ref 2New therapeutic agents in the management of hypertension: angiotensin II-receptor antagonists and renin inhibitors. Ann Pharmacother. 1993 Dec;27(12):1495-503. To Reference
Ref 3Comparative effects of aliskiren-based and ramipril-based therapy on the renin system during long-term (6 months) treatment and withdrawal in patients with hypertension. J Renin Angiotensin Aldosterone Syst. 2009 Jul 17. [Epub ahead of print] To Reference
Ref 4Functional expression of the renin-angiotensin system in human podocytes. Am J Physiol Renal Physiol. 2006 Mar;290(3):F710-9. Epub 2005 Sep 27. To Reference
Ref 5J Med Chem. 1987 Oct;30(10):1729-37.Renin inhibitors. Dipeptide analogues of angiotensinogen incorporating transition-state, nonpeptidic replacements at the scissile bond. To Reference
Ref 6Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 7Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 8J Med Chem. 2010 Nov 11;53(21):7490-520.Direct renin inhibitors as a new therapy for hypertension. To Reference
Ref 9Synergistic effect on reduction in blood pressure with coadministration of the renin inhibitor, CP-80,794, and the angiotensin converting enzyme inhibitor, captopril. J Cardiovasc Pharmacol. 1992 Jul;20(1):75-82. To Reference
Ref 10Redlich CA, Beckett WS, Sparer J, Barwick KW, Riely CA, Miller H, Sigal SL, Shalat SL, Cullen MR: Liver disease associated with occupational exposure to the solvent dimethylformamide. Ann Intern Med. 1988 May;108(5):680-6. To Reference
Ref 11Comparative effects of three different potent renin inhibitors in primates. Hypertension. 1993 Jul;22(1):9-17. To Reference
Ref 12Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. To Reference
Ref 13J Med Chem. 1981 Apr;24(4):355-61.Inhibition of the renin-angiotensin system. A new approach to the therapy of hypertension. To Reference
Ref 14J Med Chem. 1985 Dec;28(12):1779-90.Renin inhibitors. Syntheses of subnanomolar, competitive, transition-state analogue inhibitors containing a novel analogue of statine. To Reference
Ref 15J Med Chem. 1986 Oct;29(10):2080-7.Design and synthesis of potent and specific renin inhibitors containing difluorostatine, difluorostatone, and related analogues. To Reference
Ref 16J Med Chem. 1991 Feb;34(2):633-42.Renin inhibitory peptides. Incorporation of polar, hydrophilic end groups into an active renin inhibitory peptide template and their evaluation in a human renin infused rat model and in conscious sodium-depleted monkeys. To Reference
Ref 17J Med Chem. 1988 Sep;31(9):1839-46.Synthesis and biological activity of some transition-state inhibitors of human renin. To Reference
Ref 18J Med Chem. 2009 Jun 25;52(12):3689-702.Design and preparation of potent, nonpeptidic, bioavailable renin inhibitors. To Reference



 

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