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Items: 34

1.

Crystallographic structure of a small molecule SIRT1 activator-enzyme complex.

Dai H, Case AW, Riera TV, Considine T, Lee JE, Hamuro Y, Zhao H, Jiang Y, Sweitzer SM, Pietrak B, Schwartz B, Blum CA, Disch JS, Caldwell R, Szczepankiewicz B, Oalmann C, Yee Ng P, White BH, Casaubon R, Narayan R, Koppetsch K, Bourbonais F, Wu B, Wang J, Qian D, Jiang F, Mao C, Wang M, Hu E, Wu JC, Perni RB, Vlasuk GP, Ellis JL.

Nat Commun. 2015 Jul 2;6:7645. doi: 10.1038/ncomms8645.

2.

Discovery of thieno[3,2-d]pyrimidine-6-carboxamides as potent inhibitors of SIRT1, SIRT2, and SIRT3.

Disch JS, Evindar G, Chiu CH, Blum CA, Dai H, Jin L, Schuman E, Lind KE, Belyanskaya SL, Deng J, Coppo F, Aquilani L, Graybill TL, Cuozzo JW, Lavu S, Mao C, Vlasuk GP, Perni RB.

J Med Chem. 2013 May 9;56(9):3666-79. doi: 10.1021/jm400204k. Epub 2013 Apr 29.

PMID:
23570514
3.

Evidence for a common mechanism of SIRT1 regulation by allosteric activators.

Hubbard BP, Gomes AP, Dai H, Li J, Case AW, Considine T, Riera TV, Lee JE, E SY, Lamming DW, Pentelute BL, Schuman ER, Stevens LA, Ling AJ, Armour SM, Michan S, Zhao H, Jiang Y, Sweitzer SM, Blum CA, Disch JS, Ng PY, Howitz KT, Rolo AP, Hamuro Y, Moss J, Perni RB, Ellis JL, Vlasuk GP, Sinclair DA.

Science. 2013 Mar 8;339(6124):1216-9. doi: 10.1126/science.1231097.

4.

Synthesis of carba-NAD and the structures of its ternary complexes with SIRT3 and SIRT5.

Szczepankiewicz BG, Dai H, Koppetsch KJ, Qian D, Jiang F, Mao C, Perni RB.

J Org Chem. 2012 Sep 7;77(17):7319-29. doi: 10.1021/jo301067e. Epub 2012 Aug 17.

PMID:
22849721
5.

One-step, nonenzymatic synthesis of O-acetyl-ADP-ribose and analogues from NAD and carboxylates.

Szczepankiewicz BG, Koppetsch KJ, Perni RB.

J Org Chem. 2011 Aug 19;76(16):6465-74. doi: 10.1021/jo2008466. Epub 2011 Jun 13.

PMID:
21639110
6.

SIRT1 modulation as a novel approach to the treatment of diseases of aging.

Blum CA, Ellis JL, Loh C, Ng PY, Perni RB, Stein RL.

J Med Chem. 2011 Jan 27;54(2):417-32. doi: 10.1021/jm100861p. Epub 2010 Nov 16. Review. No abstract available.

PMID:
21080630
7.

SIRT1 activation by small molecules: kinetic and biophysical evidence for direct interaction of enzyme and activator.

Dai H, Kustigian L, Carney D, Case A, Considine T, Hubbard BP, Perni RB, Riera TV, Szczepankiewicz B, Vlasuk GP, Stein RL.

J Biol Chem. 2010 Oct 22;285(43):32695-703. doi: 10.1074/jbc.M110.133892. Epub 2010 Aug 11.

8.

In vitro and in vivo isotope effects with hepatitis C protease inhibitors: enhanced plasma exposure of deuterated telaprevir versus telaprevir in rats.

Maltais F, Jung YC, Chen M, Tanoury J, Perni RB, Mani N, Laitinen L, Huang H, Liao S, Gao H, Tsao H, Block E, Ma C, Shawgo RS, Town C, Brummel CL, Howe D, Pazhanisamy S, Raybuck S, Namchuk M, Bennani YL.

J Med Chem. 2009 Dec 24;52(24):7993-8001. doi: 10.1021/jm901023f.

PMID:
19894743
9.

Crystal structures of human SIRT3 displaying substrate-induced conformational changes.

Jin L, Wei W, Jiang Y, Peng H, Cai J, Mao C, Dai H, Choy W, Bemis JE, Jirousek MR, Milne JC, Westphal CH, Perni RB.

J Biol Chem. 2009 Sep 4;284(36):24394-405. doi: 10.1074/jbc.M109.014928. Epub 2009 Jun 16.

10.

Discovery of oxazolo[4,5-b]pyridines and related heterocyclic analogs as novel SIRT1 activators.

Bemis JE, Vu CB, Xie R, Nunes JJ, Ng PY, Disch JS, Milne JC, Carney DP, Lynch AV, Jin L, Smith JJ, Lavu S, Iffland A, Jirousek MR, Perni RB.

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2350-3. doi: 10.1016/j.bmcl.2008.11.106. Epub 2008 Dec 6.

PMID:
19303289
11.

Biochemical characterization, localization, and tissue distribution of the longer form of mouse SIRT3.

Jin L, Galonek H, Israelian K, Choy W, Morrison M, Xia Y, Wang X, Xu Y, Yang Y, Smith JJ, Hoffmann E, Carney DP, Perni RB, Jirousek MR, Bemis JE, Milne JC, Sinclair DA, Westphal CH.

Protein Sci. 2009 Mar;18(3):514-25. doi: 10.1002/pro.50.

12.

Discovery of imidazo[1,2-b]thiazole derivatives as novel SIRT1 activators.

Vu CB, Bemis JE, Disch JS, Ng PY, Nunes JJ, Milne JC, Carney DP, Lynch AV, Smith JJ, Lavu S, Lambert PD, Gagne DJ, Jirousek MR, Schenk S, Olefsky JM, Perni RB.

J Med Chem. 2009 Mar 12;52(5):1275-83. doi: 10.1021/jm8012954.

PMID:
19199480
13.

Discovery of benzothiazole derivatives as efficacious and enterocyte-specific MTP inhibitors.

Vu CB, Milne JC, Carney DP, Song J, Choy W, Lambert PD, Gagne DJ, Hirsch M, Cote A, Davis M, Lainez E, Meade N, Normington K, Jirousek MR, Perni RB.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1416-20. doi: 10.1016/j.bmcl.2009.01.044. Epub 2009 Jan 19.

PMID:
19181526
14.

Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes.

Milne JC, Lambert PD, Schenk S, Carney DP, Smith JJ, Gagne DJ, Jin L, Boss O, Perni RB, Vu CB, Bemis JE, Xie R, Disch JS, Ng PY, Nunes JJ, Lynch AV, Yang H, Galonek H, Israelian K, Choy W, Iffland A, Lavu S, Medvedik O, Sinclair DA, Olefsky JM, Jirousek MR, Elliott PJ, Westphal CH.

Nature. 2007 Nov 29;450(7170):712-6.

15.

Inhibitors of hepatitis C virus NS3.4A protease. Effect of P4 capping groups on inhibitory potency and pharmacokinetics.

Perni RB, Chandorkar G, Cottrell KM, Gates CA, Lin C, Lin K, Luong YP, Maxwell JP, Murcko MA, Pitlik J, Rao G, Schairer WC, Van Drie J, Wei Y.

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3406-11. Epub 2007 Apr 3.

PMID:
17482818
16.

Hepatitis C virus NS3-4A protease inhibitors: countering viral subversion in vitro and showing promise in the clinic.

Thomson JA, Perni RB.

Curr Opin Drug Discov Devel. 2006 Sep;9(5):606-17. Review.

PMID:
17002221
17.

Discovery and development of VX-950, a novel, covalent, and reversible inhibitor of hepatitis C virus NS3.4A serine protease.

Lin C, Kwong AD, Perni RB.

Infect Disord Drug Targets. 2006 Mar;6(1):3-16. Review.

PMID:
16787300
18.
19.

Preclinical profile of VX-950, a potent, selective, and orally bioavailable inhibitor of hepatitis C virus NS3-4A serine protease.

Perni RB, Almquist SJ, Byrn RA, Chandorkar G, Chaturvedi PR, Courtney LF, Decker CJ, Dinehart K, Gates CA, Harbeson SL, Heiser A, Kalkeri G, Kolaczkowski E, Lin K, Luong YP, Rao BG, Taylor WP, Thomson JA, Tung RD, Wei Y, Kwong AD, Lin C.

Antimicrob Agents Chemother. 2006 Mar;50(3):899-909.

20.

In vitro studies of cross-resistance mutations against two hepatitis C virus serine protease inhibitors, VX-950 and BILN 2061.

Lin C, Gates CA, Rao BG, Brennan DL, Fulghum JR, Luong YP, Frantz JD, Lin K, Ma S, Wei YY, Perni RB, Kwong AD.

J Biol Chem. 2005 Nov 4;280(44):36784-91. Epub 2005 Aug 8.

21.

Inhibitors of hepatitis C virus NS3.4A protease. Part 3: P2 proline variants.

Perni RB, Farmer LJ, Cottrell KM, Court JJ, Courtney LF, Deininger DD, Gates CA, Harbeson SL, Kim JL, Lin C, Lin K, Luong YP, Maxwell JP, Murcko MA, Pitlik J, Rao BG, Schairer WC, Tung RD, Van Drie JH, Wilson K, Thomson JA.

Bioorg Med Chem Lett. 2004 Apr 19;14(8):1939-42.

PMID:
15050632
22.

Inhibitors of hepatitis C virus NS3.4A protease 2. Warhead SAR and optimization.

Perni RB, Pitlik J, Britt SD, Court JJ, Courtney LF, Deininger DD, Farmer LJ, Gates CA, Harbeson SL, Levin RB, Lin C, Lin K, Moon YC, Luong YP, O'Malley ET, Rao BG, Thomson JA, Tung RD, Van Drie JH, Wei Y.

Bioorg Med Chem Lett. 2004 Mar 22;14(6):1441-6.

PMID:
15006379
23.

In vitro resistance studies of hepatitis C virus serine protease inhibitors, VX-950 and BILN 2061: structural analysis indicates different resistance mechanisms.

Lin C, Lin K, Luong YP, Rao BG, Wei YY, Brennan DL, Fulghum JR, Hsiao HM, Ma S, Maxwell JP, Cottrell KM, Perni RB, Gates CA, Kwong AD.

J Biol Chem. 2004 Apr 23;279(17):17508-14. Epub 2004 Feb 6.

24.

Inhibitors of hepatitis C virus NS3.4A protease 1. Non-charged tetrapeptide variants.

Perni RB, Britt SD, Court JC, Courtney LF, Deininger DD, Farmer LJ, Gates CA, Harbeson SL, Kim JL, Landro JA, Levin RB, Luong YP, O'Malley ET, Pitlik J, Rao BG, Schairer WC, Thomson JA, Tung RD, Van Drie JH, Wei Y.

Bioorg Med Chem Lett. 2003 Nov 17;13(22):4059-63.

PMID:
14592508
25.

NS3.4A protease as a target for interfering with hepatitis C virus replication.

Perni RB.

Drug News Perspect. 2000 Mar;13(2):69-77.

PMID:
12937632
26.

Inhibitors of hepatitis C virus NS3.4A protease: an overdue line of therapy.

Perni RB, Kwong AD.

Prog Med Chem. 2002;39:215-55. Review. No abstract available.

PMID:
12536674
27.

Phenylpropenamide derivatives as inhibitors of hepatitis B virus replication.

Perni RB, Conway SC, Ladner SK, Zaifert K, Otto MJ, King RW.

Bioorg Med Chem Lett. 2000 Dec 4;10(23):2687-90.

PMID:
11128652
28.

Inhibition of human hepatitis B virus replication by AT-61, a phenylpropenamide derivative, alone and in combination with (-)beta-L-2',3'-dideoxy-3'-thiacytidine.

King RW, Ladner SK, Miller TJ, Zaifert K, Perni RB, Conway SC, Otto MJ.

Antimicrob Agents Chemother. 1998 Dec;42(12):3179-86. Erratum in: Antimicrob Agents Chemother 1999 Mar;43(3):726.

29.

Synthesis and antitumor activity of 4-aminomethylthioxanthenone and 5-aminomethylbenzothiopyranoindazole derivatives.

Perni RB, Wentland MP, Huang JI, Powles RG, Aldous S, Klingbeil KM, Peverly AD, Robinson RG, Corbett TH, Jones JL, Mattes KC, Rake JB, Coughlin SA.

J Med Chem. 1998 Sep 10;41(19):3645-54.

PMID:
9733489
30.

Antiviral properties of 3-quinolinecarboxamides: a series of novel non-nucleoside antiherpetic agents.

Wentland MP, Perni RB, Dorff PH, Brundage RP, Castaldi MJ, Carlson JA, Bailey TR, Aldous SC, Carabateas PM, Bacon ER, Kullnig RK, Young DC, Woods MG, Kingsley SD, Ryan KA, Rosi D, Drozd ML, Dutko FJ.

Drug Des Discov. 1997 May;15(1):25-38. Review.

PMID:
9332829
31.

Cyclic variations of 3-quinolinecarboxamides and effects on antiherpetic activity.

Wentland MP, Carlson JA, Dorff PH, Aldous SC, Perni RB, Young DC, Woods MG, Kingsley SD, Ryan KA, Rosi D, et al.

J Med Chem. 1995 Jul 7;38(14):2541-5.

PMID:
7629793
32.

Synthesis and antibacterial activity of some novel 1-substituted 1,4-dihydro-4-oxo-7-pyridinyl-3-quinolinecarboxylic acids. Potent antistaphylococcal agents.

Reuman M, Daum SJ, Singh B, Wentland MP, Perni RB, Pennock P, Carabateas PM, Gruett MD, Saindane MT, Dorff PH, et al.

J Med Chem. 1995 Jul 7;38(14):2531-40.

PMID:
7629792
33.

3-Quinolinecarboxamides. A series of novel orally-active antiherpetic agents.

Wentland MP, Perni RB, Dorff PH, Brundage RP, Castaldi MJ, Bailey TR, Carabateas PM, Bacon ER, Young DC, Woods MG, et al.

J Med Chem. 1993 May 28;36(11):1580-96.

PMID:
8388470
34.

Synthesis and bacterial DNA gyrase inhibitory properties of a spirocyclopropylquinolone derivative.

Wentland MP, Perni RB, Dorff PH, Rake JB.

J Med Chem. 1988 Sep;31(9):1694-7.

PMID:
2842501

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