1. Gribouval O, Gonzales M, Neuhaus T, Aziza J, Bieth E, Laurent N, Bouton JM, Feuillet F, Makni S, Ben Amar H et al.. (2005) Mutations in genes in the renin-angiotensin system are associated with autosomal recessive renal tubular dysgenesis.. Nat Genet, 37 (9): (964-8). [PMID:16116425] |
2. Hilpert H, Guba W, Woltering TJ, Wostl W, Pinard E, Mauser H, Mayweg AV, Rogers-Evans M, Humm R, Krummenacher D et al.. (2013) β-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease.. J Med Chem, 56 (10): (3980-95). [PMID:23590342] |
3. Kwan JC, Eksioglu EA, Liu C, Paul VJ, Luesch H. (2009) Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.. J Med Chem, 52 (18): (5732-47). [PMID:19715320] |
4. Pettus LH, Bourbeau MP, Bradley J, Bartberger MD, Chen K, Hickman D, Johnson M, Liu Q, Manning JR, Nanez A et al.. (2020) Discovery of AM-6494: A Potent and Orally Efficacious β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in Vivo Selectivity over BACE2.. J Med Chem, 63 (5): (2263-2281). [PMID:31589043] |
5. Ondetti MA, Cushman DW.. (1981) Inhibition of the renin-angiotensin system. A new approach to the therapy of hypertension.. J Med Chem, 24 (4): (355-361). [PMID:6267277] |
6. Hui KY, Holtzman EJ, Quinones MA, Hollenberg NK, Haber E.. (1988) Design of rat renin inhibitory peptides.. J Med Chem, 31 (9): (1679-1686). [PMID:3045320] |
7. Göschke R, Stutz S, Rasetti V, Cohen NC, Rahuel J, Rigollier P, Baum HP, Forgiarini P, Schnell CR, Wagner T, Gruetter MG, Fuhrer W, Schilling W, Cumin F, Wood JM, Maibaum J.. (2007) Novel 2,7-dialkyl-substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamide transition state peptidomimetics are potent and orally active inhibitors of human renin.. J Med Chem, 50 (20): (4818-4831). [PMID:17824679] |
8. Maibaum J, Stutz S, Göschke R, Rigollier P, Yamaguchi Y, Cumin F, Rahuel J, Baum HP, Cohen NC, Schnell CR, Fuhrer W, Gruetter MG, Schilling W, Wood JM.. (2007) Structural modification of the P2' position of 2,7-dialkyl-substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamides: the discovery of aliskiren, a potent nonpeptide human renin inhibitor active after once daily dosing in marmosets.. J Med Chem, 50 (20): (4832-4844). [PMID:17824680] |
9. Tice CM, Xu Z, Yuan J, Simpson RD, Cacatian ST, Flaherty PT, Zhao W, Guo J, Ishchenko A, Singh SB, Wu Z, Scott BB, Bukhtiyarov Y, Berbaum J, Mason J, Panemangalore R, Cappiello MG, Müller D, Harrison RK, McGeehan GM, Dillard LW, Baldwin JJ, Claremon DA.. (2009) Design and optimization of renin inhibitors: Orally bioavailable alkyl amines.. Bioorg Med Chem Lett, 19 (13): (3541-3545). [PMID:19457666] |
10. Malamas MS, Erdei J, Gunawan I, Barnes K, Johnson M, Hui Y, Turner J, Hu Y, Wagner E, Fan K, Olland A, Bard J, Robichaud AJ.. (2009) Aminoimidazoles as potent and selective human beta-secretase (BACE1) inhibitors.. J Med Chem, 52 (20): (6314-6323). [PMID:19757823] |
11. Malamas MS, Erdei J, Gunawan I, Turner J, Hu Y, Wagner E, Fan K, Chopra R, Olland A, Bard J, Jacobsen S, Magolda RL, Pangalos M, Robichaud AJ.. (2010) Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors.. J Med Chem, 53 (3): (1146-1158). [PMID:19968289] |
12. Xu Z, Cacatian S, Yuan J, Simpson RD, Jia L, Zhao W, Tice CM, Flaherty PT, Guo J, Ishchenko A, Singh SB, Wu Z, McKeever BM, Scott BB, Bukhtiyarov Y, Berbaum J, Mason J, Panemangalore R, Cappiello MG, Bentley R, Doe CP, Harrison RK, McGeehan GM, Dillard LW, Baldwin JJ, Claremon DA.. (2010) Optimization of orally bioavailable alkyl amine renin inhibitors.. Bioorg Med Chem Lett, 20 (2): (694-699). [PMID:19959358] |
13. Chen A, Bayly C, Bezençon O, Richard-Bildstein S, Dubé D, Dubé L, Gagné S, Gallant M, Gaudreault M, Grimm E, Houle R, Lacombe P, Laliberté S, Lévesque JF, Liu S, MacDonald D, Mackay B, Martin D, McKay D, Powell D, Remen L, Soisson S, Toulmond S.. (2010) Design and optimization of a substituted amino propanamide series of renin inhibitors for the treatment of hypertension.. Bioorg Med Chem Lett, 20 (7): (2204-2209). [PMID:20206513] |
14. Al-Nadaf A, Abu Sheikha G, Taha MO.. (2010) Elaborate ligand-based pharmacophore exploration and QSAR analysis guide the synthesis of novel pyridinium-based potent beta-secretase inhibitory leads.. Bioorg Med Chem, 18 (9): (3088-3115). [PMID:20378363] |
15. Corminboeuf O, Bezençon O, Grisostomi C, Remeň L, Richard-Bildstein S, Bur D, Prade L, Hess P, Strickner P, Fischli W, Steiner B, Treiber A.. (2010) Design and optimization of new piperidines as renin inhibitors.. Bioorg Med Chem Lett, 20 (21): (6286-6290). [PMID:20843686] |
16. Scheiper B, Matter H, Steinhagen H, Stilz U, Böcskei Z, Fleury V, McCort G.. (2010) Discovery and optimization of a new class of potent and non-chiral indole-3-carboxamide-based renin inhibitors.. Bioorg Med Chem Lett, 20 (21): (6268-6272). [PMID:20850300] |
17. Webb RL, Schiering N, Sedrani R, Maibaum J.. (2010) Direct renin inhibitors as a new therapy for hypertension.. J Med Chem, 53 (21): (7490-7520). [PMID:20731374] |
18. Chen A, Campeau LC, Cauchon E, Chefson A, Ducharme Y, Dubé D, Falgueyret JP, Fournier PA, Gagné S, Grimm E, Han Y, Houle R, Huang JQ, Lacombe P, Laliberté S, Lévesque JF, Liu S, MacDonald D, Mackay B, McKay D, Percival MD, Regan C, Regan H, St-Jacques R, Toulmond S.. (2011) Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of pyridone-substituted piperidines.. Bioorg Med Chem Lett, 21 (13): (3970-3975). [PMID:21621998] |
19. Yuan J, Simpson RD, Zhao W, Tice CM, Xu Z, Cacatian S, Jia L, Flaherty PT, Guo J, Ishchenko A, Wu Z, McKeever BM, Scott BB, Bukhtiyarov Y, Berbaum J, Panemangalore R, Bentley R, Doe CP, Harrison RK, McGeehan GM, Singh SB, Dillard LW, Baldwin JJ, Claremon DA.. (2011) Biphenyl/diphenyl ether renin inhibitors: filling the S1 pocket of renin via the S3 pocket.. Bioorg Med Chem Lett, 21 (16): (4836-4843). [PMID:21741239] |
20. Matter H, Scheiper B, Steinhagen H, Böcskei Z, Fleury V, McCort G.. (2011) Structure-based design and optimization of potent renin inhibitors on 5- or 7-azaindole-scaffolds.. Bioorg Med Chem Lett, 21 (18): (5487-5492). [PMID:21840215] |
21. Scheiper B, Matter H, Steinhagen H, Böcskei Z, Fleury V, McCort G.. (2011) Structure-based optimization of potent 4- and 6-azaindole-3-carboxamides as renin inhibitors.. Bioorg Med Chem Lett, 21 (18): (5480-5486). [PMID:21840218] |
22. Chen A, Cauchon E, Chefson A, Dolman S, Ducharme Y, Dubé D, Falgueyret JP, Fournier PA, Gagné S, Gallant M, Grimm E, Han Y, Houle R, Huang JQ, Hughes G, Jûteau H, Lacombe P, Lauzon S, Lévesque JF, Liu S, Macdonald D, Mackay B, McKay D, Percival MD, St-Jacques R, Toulmond S.. (2011) Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of tertiary alcohol-bearing piperidines.. Bioorg Med Chem Lett, 21 (13): (3976-3981). [PMID:21641209] |
23. Chen A, Aspiotis R, Campeau LC, Cauchon E, Chefson A, Ducharme Y, Falgueyret JP, Gagné S, Han Y, Houle R, Laliberté S, Larouche G, Lévesque JF, McKay D, Percival D.. (2011) Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of spirocyclic piperidines.. Bioorg Med Chem Lett, 21 (24): (7399-7404). [PMID:22071301] |
24. Stachel SJ, Steele TG, Petrocchi A, Haugabook SJ, McGaughey G, Katharine Holloway M, Allison T, Munshi S, Zuck P, Colussi D, Tugasheva K, Wolfe A, Graham SL, Vacca JP.. (2012) Discovery of pyrrolidine-based β-secretase inhibitors: lead advancement through conformational design for maintenance of ligand binding efficiency.. Bioorg Med Chem Lett, 22 (1): (240-244). [PMID:22130130] |
25. Lacombe P, Arbour M, Aspiotis R, Cauchon E, Chen A, Dubé D, Falgueyret JP, Fournier PA, Gallant M, Grimm E, Han Y, Juteau H, Liu S, Mellon C, Ramtohul Y, Simard D, St-Jacques R, Tsui GC.. (2012) 3,4-Diarylpiperidines as potent renin inhibitors.. Bioorg Med Chem Lett, 22 (5): (1953-1957). [PMID:22325946] |
26. Jia L, Simpson RD, Yuan J, Xu Z, Zhao W, Cacatian S, Tice CM, Guo J, Ishchenko A, Singh SB, Wu Z, McKeever BM, Bukhtiyarov Y, Johnson JA, Doe CP, Harrison RK, McGeehan GM, Dillard LW, Baldwin JJ, Claremon DA.. (2011) Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility.. ACS Med Chem Lett, 2 (10): (747-751). [PMID:24900262] |
27. Tzoupis H, Leonis G, Megariotis G, Supuran CT, Mavromoustakos T, Papadopoulos MG.. (2012) Dual inhibitors for aspartic proteases HIV-1 PR and renin: advancements in AIDS-hypertension-diabetes linkage via molecular dynamics, inhibition assays, and binding free energy calculations.. J Med Chem, 55 (12): (5784-5796). [PMID:22621689] |
28. Ostermann N, Ruedisser S, Ehrhardt C, Breitenstein W, Marzinzik A, Jacoby E, Vangrevelinghe E, Ottl J, Klumpp M, Hartwieg JC, Cumin F, Hassiepen U, Trappe J, Sedrani R, Geisse S, Gerhartz B, Richert P, Francotte E, Wagner T, Krömer M, Kosaka T, Webb RL, Rigel DF, Maibaum J, Baeschlin DK.. (2013) A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore.. J Med Chem, 56 (6): (2196-2206). [PMID:23360239] |
29. Yuan J, Venkatraman S, Zheng Y, McKeever BM, Dillard LW, Singh SB.. (2013) Structure-based design of β-site APP cleaving enzyme 1 (BACE1) inhibitors for the treatment of Alzheimer's disease.. J Med Chem, 56 (11): (4156-4180). [PMID:23509904] |
30. Sellner H, Cottens S, Cumin F, Ehrhardt C, Kosaka T, Lorthiois E, Ostermann N, Webb RL, Rigel DF, Wagner T, Maibaum J.. (2015) trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker.. Bioorg Med Chem Lett, 25 (8): (1787-1791). [PMID:25754490] |
31. Sun X, Wen X, Chen YY, Shi C, Gao C, Wu Y, Wang LJ, Yang XH, Sun H.. (2015) Discovery of highly potent renin inhibitors potentially interacting with the S3' subsite of renin.. Eur J Med Chem, 103 (269-288). [PMID:26363506] |
32. Imaeda Y, Tokuhara H, Fukase Y, Kanagawa R, Kajimoto Y, Kusumoto K, Kondo M, Snell G, Behnke CA, Kuroita T.. (2016) Discovery of TAK-272: A Novel, Potent, and Orally Active Renin Inhibitor.. ACS Med Chem Lett, 7 (10): (933-938). [PMID:27774132] |
33. Johansson P, Kaspersson K, Gurrell IK, Bäck E, Eketjäll S, Scott CW, Cebers G, Thorne P, McKenzie MJ, Beaton H, Davey P, Kolmodin K, Holenz J, Duggan ME, Budd Haeberlein S, Bürli RW.. (2018) Toward β-Secretase-1 Inhibitors with Improved Isoform Selectivity.. J Med Chem, 61 (8): (3491-3502). [PMID:29617572] |
34. Cloudsdale IS, Dickson JK, Barta TE, Grella BS, Smith ED, Kulp JL, Guarnieri F, Kulp JL.. (2017) Design, synthesis and biological evaluation of renin inhibitors guided by simulated annealing of chemical potential simulations.. Bioorg Med Chem, 25 (15): (3947-3963). [PMID:28601508] |
35. Ramya K, Suresh R, Kumar HY, Kumar BRP, Murthy NBS.. (2020) Decades-old renin inhibitors are still struggling to find a niche in antihypertensive therapy. A fleeting look at the old and the promising new molecules.. Bioorg Med Chem, 28 (10): (115466-115466). [PMID:32247750] |
36. and Werning, C C.. (1976) The effect of minoxidil on blood pressure and plasma renin activity in patients with essential and renal hypertension.. Klinische Wochenschrift, (1): [PMID:790007] |
37. Dhanaraj, V V and 9 more authors.. (1992) X-ray analyses of peptide-inhibitor complexes define the structural basis of specificity for human and mouse renins.. Nature, (11): [PMID:1608447] |
38. Glassman, H N HN and 5 more authors.. (1990) Clinical pharmacology of enalkiren, a novel, dipeptide renin inhibitor.. Journal of cardiovascular pharmacology, [PMID:1705633] |
39. Ishizuka, Y Y and 5 more authors.. (1991) Isolation and characterization of recombinant human prorenin in Chinese hamster ovary cells.. Journal of biochemistry, [PMID:2016271] |
40. Sielecki, A R AR and 9 more authors.. (1989) Structure of recombinant human renin, a target for cardiovascular-active drugs, at 2.5 A resolution.. Science (New York, N.Y.), (10): [PMID:2493678] |
41. Burt, D W DW, Nakamura, N N, Kelley, P P and Dzau, V J VJ.. (1989) Identification of negative and positive regulatory elements in the human renin gene.. The Journal of biological chemistry, (5): [PMID:2540188] |
42. Fukamizu, A A and 5 more authors.. (1986) Human renin gene of renin-secreting tumor.. Gene, [PMID:3032746] |
43. Soubrier, F F, Panthier, J J JJ, Houot, A M AM, Rougeon, F F and Corvol, P P.. (1986) Segmental homology between the promoter region of the human renin gene and the mouse ren1 and ren2 promoter regions.. Gene, [PMID:3516796] |
44. and Morris, B J BJ.. (1986) New possibilities for intracellular renin and inactive renin now that the structure of the human renin gene has been elucidated.. Clinical science (London, England : 1979), [PMID:3530608] |
45. Soubrier, F F, Panthier, J J JJ, Corvol, P P and Rougeon, F F.. (1983) Molecular cloning and nucleotide sequence of a human renin cDNA fragment.. Nucleic acids research, (25): [PMID:6138751] |
46. Imai, T T and 8 more authors.. (1983) Cloning and sequence analysis of cDNA for human renin precursor.. Proceedings of the National Academy of Sciences of the United States of America, [PMID:6324167] |
47. Hardman, J A JA and 6 more authors.. (1984) Primary structure of the human renin gene.. DNA (Mary Ann Liebert, Inc.), [PMID:6391881] |
48. Kiowski, W W and 6 more authors.. (1994) Angiotensinergic versus nonangiotensinergic hemodynamic effects of converting enzyme inhibition in patients with chronic heart failure. Assessment by acute renin and converting enzyme inhibition.. Circulation, [PMID:7994817] |
49. van Paassen, P P, Navis, G J GJ, De Jong, P E PE and De Zeeuw, D D.. (1999) Pretreatment renal vascular tone predicts the effect of specific renin inhibition on natriuresis in essential hypertension.. European journal of clinical investigation, [PMID:10583449] |
50. Rahuel, J J and 10 more authors.. (2000) Structure-based drug design: the discovery of novel nonpeptide orally active inhibitors of human renin.. Chemistry & biology, [PMID:10903938] |
51. Chen, X X, Ji, Z L ZL and Chen, Y Z YZ.. (2002) TTD: Therapeutic Target Database.. Nucleic acids research, (1): [PMID:11752352] |
52. Nussberger, Juerg J, Wuerzner, Grégoire G, Jensen, Chris C and Brunner, Hans R HR.. (2002) Angiotensin II suppression in humans by the orally active renin inhibitor Aliskiren (SPP100): comparison with enalapril.. Hypertension (Dallas, Tex. : 1979), [PMID:11799102] |
53. Nguyen, Genevieve G and 5 more authors.. (2002) Pivotal role of the renin/prorenin receptor in angiotensin II production and cellular responses to renin.. The Journal of clinical investigation, [PMID:12045255] |
54. Wood, Jeanette M JM and 21 more authors.. (2003) Structure-based design of aliskiren, a novel orally effective renin inhibitor.. Biochemical and biophysical research communications, (5): [PMID:12927775] |
55. Cody, Wayne L WL and 10 more authors.. (2005) The discovery and preparation of disubstituted novel amino-aryl-piperidine-based renin inhibitors.. Bioorganic & medicinal chemistry, (3): [PMID:15582452] |
56. Gregory, S G SG and 178 more authors.. (2006) The DNA sequence and biological annotation of human chromosome 1.. Nature, (18): [PMID:16710414] |
57. Gradman, Alan H AH and Vivas, Yoel Y.. (2006) New drugs for hypertension: what do they offer?. Current hypertension reports, [PMID:16965731] |
58. Sarver, Ronald W RW and 16 more authors.. (2007) Binding thermodynamics of substituted diaminopyrimidine renin inhibitors.. Analytical biochemistry, (1): [PMID:17113558] |
59. Zivná, Martina M and 28 more authors.. (2009) Dominant renin gene mutations associated with early-onset hyperuricemia, anemia, and chronic kidney failure.. American journal of human genetics, [PMID:19664745] |
60. Zhou, Aiwu A and 8 more authors.. (2010) A redox switch in angiotensinogen modulates angiotensin release.. Nature, (4): [PMID:20927107] |
61. Wal, Pranay P, Wal, Ankita A, Rai, Awani K AK and Dixit, Anuj A.. (2011) Aliskiren: An orally active renin inhibitor.. Journal of pharmacy & bioallied sciences, [PMID:21687346] |
62. Te Riet, Luuk L, van Esch, Joep H M JH, Roks, Anton J M AJ, van den Meiracker, Anton H AH and Danser, A H Jan AH.. (2015) Hypertension: renin-angiotensin-aldosterone system alterations.. Circulation research, (13): [PMID:25767283] |