Aliskiren displays long-lasting interactions with human renin

Naunyn-Schmiedeberg's Archives of Pharmacology

Volumn 385, Issue 2, 2012, Pages 219-224

  Gossas, Thomas ^a   Vrang, Lotta ^b   Henderson, Ian ^b   Sedig, Susanne ^b   Sahlberg, Christer ^b   Lindström, Erik ^b   Danielson, U Helena ^a  

^a UPPSALA UNIVERSITY   (Sweden)

^b MEDIVIR AB   (Sweden)

Author keywords

Aliskiren; Inhibitors; Interaction kinetics; Optical biosensor; Renin; Surface plasmon resonance (SPR)

Indexed keywords

ALISKIREN; ANGIOTENSIN I; REMIKIREN; RENIN;

ANTIHYPERTENSIVE ACTIVITY; ARTICLE; BINDING AFFINITY; BIOSENSOR; DRUG POTENCY; DRUG PROTEIN BINDING; ENZYME SUBSTRATE; FLUORESCENCE; IC 50; KINETICS; PLASMA RENIN ACTIVITY; PROTEIN CLEAVAGE; PROTEIN IMMOBILIZATION; SURFACE PLASMON RESONANCE;

AMIDES; ANTIHYPERTENSIVE AGENTS; BIOSENSING TECHNIQUES; FUMARATES; HUMANS; IMIDAZOLES; KINETICS; RECOMBINANT PROTEINS; RENIN;

EID: 84857032761     PISSN: 00281298     EISSN: 14321912     Source Type: Journal    
DOI: 10.1007/s00210-011-0718-7     Document Type: Article

References (29)

1. K Andersen MH Weinberger B Egan CM Constance MA Ali J Jin DL Keefe 2008 Comparative efficacy and safety of aliskiren, an oral direct renin inhibitor, and ramipril in hypertension: a 6-month, randomized, double-blind trial J Hypertens 26 589 599 18300872 10.1097/HJH.0b013e3282f3ad9a 1:CAS:528: DC%2BD1cXisVWhur0%3D (Pubitemid 351317270)
2. Baldwin JJ, Claremon DA, Tice C, Cacatian S, Dillard LW, Ishchenko AV, Yuan J, Xu Z, McGeehan G, Zhao W, Simpson RD, Singh SB, Flaherty PT, Wery J-P (2006) WO2006/042150, Apr. 20, 2006; CAN 144:432692.
3. KB Biswas AH Nabi Y Arai T Nakagawa A Ebihara A Ichihara T Watanabe T Inagami F Suzuki 2010 Aliskiren binds to renin and prorenin bound to (pro)renin receptor in vitro Hypertens Res 33 1053 1059 20664543 10.1038/hr.2010.136 1:CAS:528:DC%2BC3cXht1ers7%2FN
4. CT Carilli JL Vigne LC Wallace LM Smith MA Wong JA Lewicki JD Baxter 1988 Characterization of recombinant human prorenin and renin Hypertension 11 713 716 3292415 1:STN:280:DyaL1c3nt1CmsQ%3D%3D
5. RA Copeland DL Pompliano TD Meek 2006 Drug-target residence time and its implications for lead optimization Nat Rev Drug Discov 5 730 739 16888652 10.1038/nrd2082 1:CAS:528:DC%2BD28XptVCltro%3D (Pubitemid 44323700)
6. I Dierynck M De Wit E Gustin I Keuleers J Vandersmissen S Hallenberger K Hertogs 2007 Binding kinetics of darunavir to human immunodeficiency virus type 1 protease explain the potent antiviral activity and high genetic barrier J Virol 81 13845 13851 17928344 10.1128/JVI.01184-07 1:CAS:528:DC%2BD2sXhsValsbbF (Pubitemid 350247878)
7. H Dong Z-L Zhang J-H Huang R Ma S-H Chen G Li 2005 Practical synthesis of an orally active renin inhibitor aliskiren Tetrahedron Lett 46 6337 6340 10.1016/j.tetlet.2005.07.028 1:CAS:528:DC%2BD2MXns1SgsL8%3D (Pubitemid 41140192)
8. DL Feldman L Jin H Xuan A Contrepas Y Zhou RL Webb DN Mueller S Feldt F Cumin W Maniara E Persohn H Schuetz AH Jan Danser G Nguyen 2008 Effects of aliskiren on blood pressure, albuminuria, and (pro)renin receptor expression in diabetic TG(mRen-2)27 rats Hypertension 52 130 136 18490518 10.1161/ HYPERTENSIONAHA.107.108845 1:CAS:528:DC%2BD1cXntVaisL0%3D
9. W Fischli JP Clozel K el Amrani W Wostl W Neidhart H Stadler Q Branca 1991 Ro 42-5892 is a potent orally active renin inhibitor in primates Hypertension 18 22 31 1830563 1:CAS:528:DyaK3MXlt1Kltbc%3D
10. ND Fisher NK Hollenberg 2001 Is there a future for renin inhibitors? Expert Opin Investig Drugs 10 417 426 11227042 10.1517/13543784.10.3.417 1:CAS:528:DC%2BD3MXhs1Kjs7o%3D (Pubitemid 32186140)
11. I Kobrin RJ Viskoper A Laszt J Bock C Weber V Charlon 1993 Effects of an orally active renin inhibitor, Ro 42-5892, in patients with essential hypertension Am J Hypertens 6 349 356 8512659 1:STN:280:DyaK3s3ptVyjsg%3D%3D (Pubitemid 23161685)
12. M Krop IM Garrelds RJ de Bruin JM van Gool ND Fisher NK Hollenberg AH Jan Danser 2008 Aliskiren accumulates in Renin secretory granules and binds plasma prorenin Hypertension 52 1076 1083 18981317 10.1161/HYPERTENSIONAHA.108.123042 1:CAS:528:DC%2BD1cXhsVWrt7jI
13. G Levy 1994 Pharmacologic target-mediated drug disposition Clin Pharmacol Ther 56 248 252 7924119 10.1038/clpt.1994.134 1:STN:280:DyaK2M%2FgvVGqsw%3D%3D (Pubitemid 24323915)
14. E Lindström B von Mentzer I Pahlman I Ahlstedt A Uvebrant E Kristensson R Martinsson A Noven J de Verdier G Vauquelin 2007 Neurokinin 1 receptor antagonists: correlation between in vitro receptor interaction and in vivo efficacy J Pharmacol Exp Ther 322 1286 1293 17575073 10.1124/jpet.107. 124958 (Pubitemid 47295789)
15. JF Morrison 1969 Kinetics of the reversible inhibition of enzyme-catalysed reactions by tight-binding inhibitors Biochim Biophys Acta 185 269 286 4980133 1:CAS:528:DyaF1MXkvVOqsbo%3D
16. BH Oh J Mitchell JR Herron J Chung M Khan DL Keefe 2007 Aliskiren, an oral renin inhibitor, provides dose-dependent efficacy and sustained 24-hour blood pressure control in patients with hypertension J Am Coll Cardiol 49 1157 1163 17367658 10.1016/j.jacc.2006.11.032 1:CAS:528:DC%2BD2sXjtVagurk%3D (Pubitemid 46400330)
17. S Oparil SA Yarows S Patel H Fang J Zhang A Satlin 2007 Efficacy and safety of combined use of aliskiren and valsartan in patients with hypertension: a randomised, double-blind trial Lancet 370 221 229 17658393 10.1016/S0140-6736(07)61124-6 1:CAS:528:DC%2BD2sXnvF2gsrc%3D (Pubitemid 47069535)
18. F Portaluppi B Bagni E degli Uberti L Montanari R Cavallini G Trasforini A Margutti M Ferlini M Zanella M Parti 1990 Circadian rhythms of atrial natriuretic peptide, renin, aldosterone, cortisol, blood pressure and heart rate in normal and hypertensive subjects J Hypertens 8 85 95 2157761 10.1097/00004872-199001000-00013 1:STN:280:DyaK3c3hslCrtg%3D%3D (Pubitemid 20186318)
19. AR Sielecki K Hayakawa M Fujinaga ME Murphy M Fraser AK Muir CT Carilli JA Lewicki JD Baxter MN James 1989 Structure of recombinant human renin, a target for cardiovascular-active drugs, at 2.5 A resolution Science 243 1346 1351 2493678 10.1126/science.2493678 1:CAS:528:DyaL1MXhs12htbo%3D (Pubitemid 19085370)
20. LT Skeggs Jr JR Kahn K Lentz NP Shumway 1957 The preparation, purification, and amino acid sequence of a polypeptide renin substrate J Exp Med 106 439 453 13463253 10.1084/jem.106.3.439 1:CAS:528:DyaG2sXpvFGgtg%3D%3D
21. PJ Tummino RA Copeland 2008 Residence time of receptor-ligand complexes and its effect on biological function Biochemistry 47 5481 5492 18412369 10.1021/bi8002023 1:CAS:528:DC%2BD1cXks1Ont7s%3D (Pubitemid 351711169)
22. F Waldmeier U Glaenzel B Wirz L Oberer D Schmid M Seiberling J Valencia GJ Riviere P End S Vaidyanathan 2007 Absorption, distribution, metabolism, and elimination of the direct renin inhibitor aliskiren in healthy volunteers Drug Metab Dispos 35 1418 1428 17510248 10.1124/dmd.106.013797 1:CAS:528: DC%2BD2sXosVKqurg%3D (Pubitemid 47121784)
23. AH van den Meiracker PJ Admiraal AJ Man in 't Veld FH Derkx HJ Ritsema van Eck P Mulder P van Brummelen MA Schalekamp 1990 Prolonged blood pressure reduction by orally active renin inhibitor RO 42-5892 in essential hypertension BMJ 301 205 210 2203486 10.1136/bmj.301.6745.205 (Pubitemid 20238009)
24. G Vauquelin I Van Liefde 2006 Slow antagonist dissociation and long-lasting in vivo receptor protection Trends Pharmacol Sci 27 356 359 16766051 10.1016/j.tips.2006.05.001 (Pubitemid 43963183)
25. MA Weber 2002 The 24-hour blood pressure pattern: does it have implications for morbidity and mortality? Am J Cardiol 89 27A 33A 11835909 10.1016/S0002-9149(01)02324-4 (Pubitemid 34143243)
26. MR Weir 2007 Effects of renin-angiotensin system inhibition on end-organ protection: can we do better? Clin Ther 29 1803 1824 18035185 10.1016/j.clinthera.2007.09.019 1:CAS:528:DC%2BD2sXhtlakt7rL (Pubitemid 350214460)
27. WB White 2007 Importance of blood pressure control over a 24-hour period J Manag Care Pharm 13 34 39 17970615
28. RJ Viskoper V Charlon A Laszt C Yosefy J Bock M Landau I Kobrin 1994 Time dependency of the antihypertensive efficacy of the new renin inhibitor Ro 42-5892 J Hum Hypertens 8 133 136 8207739 1:STN:280:DyaK2c3mslyiug%3D%3D (Pubitemid 24065901)
29. JM Wood J Maibaum J Rahuel MG Grutter NC Cohen V Rasetti H Ruger R Goschke S Stutz W Fuhrer W Schilling P Rigollier Y Yamaguchi F Cumin HP Baum CR Schnell P Herold R Mah C Jensen E O'Brien A Stanton MP Bedigian 2003 Structure-based design of aliskiren, a novel orally effective renin inhibitor Biochem Biophys Res Commun 308 698 705 12927775 10.1016/S0006-291X(03)01451-7 1:CAS:528:DC%2BD3sXmsVGkt7k%3D (Pubitemid 36976519)