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Items: 36

1.

Discovery of a Potent and Orally Bioavailable Cyclophilin Inhibitor Derived from the Sanglifehrin Macrocycle.

Mackman RL, Steadman VA, Dean DK, Jansa P, Poullennec KG, Appleby T, Austin C, Blakemore CA, Cai R, Cannizzaro C, Chin G, Chiva JC, Dunbar NA, Fliri H, Highton AJ, Hui H, Ji M, Jin H, Karki K, Keats AJ, Lazarides L, Lee YJ, Liclican A, Mish M, Murray B, Pettit SB, Pyun P, Sangi M, Santos R, Sanvoisin J, Schmitz U, Schrier A, Siegel D, Sperandio D, Stepan G, Tian Y, Watt GM, Yang H, Schultz BE.

J Med Chem. 2018 Nov 8;61(21):9473-9499. doi: 10.1021/acs.jmedchem.8b00802. Epub 2018 Aug 22.

PMID:
30074795
2.

Coronavirus Susceptibility to the Antiviral Remdesivir (GS-5734) Is Mediated by the Viral Polymerase and the Proofreading Exoribonuclease.

Agostini ML, Andres EL, Sims AC, Graham RL, Sheahan TP, Lu X, Smith EC, Case JB, Feng JY, Jordan R, Ray AS, Cihlar T, Siegel D, Mackman RL, Clarke MO, Baric RS, Denison MR.

MBio. 2018 Mar 6;9(2). pii: e00221-18. doi: 10.1128/mBio.00221-18.

3.

Broad-spectrum antiviral GS-5734 inhibits both epidemic and zoonotic coronaviruses.

Sheahan TP, Sims AC, Graham RL, Menachery VD, Gralinski LE, Case JB, Leist SR, Pyrc K, Feng JY, Trantcheva I, Bannister R, Park Y, Babusis D, Clarke MO, Mackman RL, Spahn JE, Palmiotti CA, Siegel D, Ray AS, Cihlar T, Jordan R, Denison MR, Baric RS.

Sci Transl Med. 2017 Jun 28;9(396). pii: eaal3653. doi: 10.1126/scitranslmed.aal3653.

4.

GS-5734 and its parent nucleoside analog inhibit Filo-, Pneumo-, and Paramyxoviruses.

Lo MK, Jordan R, Arvey A, Sudhamsu J, Shrivastava-Ranjan P, Hotard AL, Flint M, McMullan LK, Siegel D, Clarke MO, Mackman RL, Hui HC, Perron M, Ray AS, Cihlar T, Nichol ST, Spiropoulou CF.

Sci Rep. 2017 Mar 6;7:43395. doi: 10.1038/srep43395.

5.

Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses.

Siegel D, Hui HC, Doerffler E, Clarke MO, Chun K, Zhang L, Neville S, Carra E, Lew W, Ross B, Wang Q, Wolfe L, Jordan R, Soloveva V, Knox J, Perry J, Perron M, Stray KM, Barauskas O, Feng JY, Xu Y, Lee G, Rheingold AL, Ray AS, Bannister R, Strickley R, Swaminathan S, Lee WA, Bavari S, Cihlar T, Lo MK, Warren TK, Mackman RL.

J Med Chem. 2017 Mar 9;60(5):1648-1661. doi: 10.1021/acs.jmedchem.6b01594. Epub 2017 Feb 14.

PMID:
28124907
6.

Discovery of Potent Cyclophilin Inhibitors Based on the Structural Simplification of Sanglifehrin A.

Steadman VA, Pettit SB, Poullennec KG, Lazarides L, Keats AJ, Dean DK, Stanway SJ, Austin CA, Sanvoisin JA, Watt GM, Fliri HG, Liclican AC, Jin D, Wong MH, Leavitt SA, Lee YJ, Tian Y, Frey CR, Appleby TC, Schmitz U, Jansa P, Mackman RL, Schultz BE.

J Med Chem. 2017 Feb 9;60(3):1000-1017. doi: 10.1021/acs.jmedchem.6b01329. Epub 2017 Jan 31.

PMID:
28075591
7.

Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys.

Warren TK, Jordan R, Lo MK, Ray AS, Mackman RL, Soloveva V, Siegel D, Perron M, Bannister R, Hui HC, Larson N, Strickley R, Wells J, Stuthman KS, Van Tongeren SA, Garza NL, Donnelly G, Shurtleff AC, Retterer CJ, Gharaibeh D, Zamani R, Kenny T, Eaton BP, Grimes E, Welch LS, Gomba L, Wilhelmsen CL, Nichols DK, Nuss JE, Nagle ER, Kugelman JR, Palacios G, Doerffler E, Neville S, Carra E, Clarke MO, Zhang L, Lew W, Ross B, Wang Q, Chun K, Wolfe L, Babusis D, Park Y, Stray KM, Trancheva I, Feng JY, Barauskas O, Xu Y, Wong P, Braun MR, Flint M, McMullan LK, Chen SS, Fearns R, Swaminathan S, Mayers DL, Spiropoulou CF, Lee WA, Nichol ST, Cihlar T, Bavari S.

Nature. 2016 Mar 17;531(7594):381-5. doi: 10.1038/nature17180. Epub 2016 Mar 2. Erratum in: ACS Chem Biol. 2016 May 20;11(5):1463.

8.

Antiviral Efficacy of a Respiratory Syncytial Virus (RSV) Fusion Inhibitor in a Bovine Model of RSV Infection.

Jordan R, Shao M, Mackman RL, Perron M, Cihlar T, Lewis SA, Eisenberg EJ, Carey A, Strickley RG, Chien JW, Anderson ML, McEligot HA, Behrens NE, Gershwin LJ.

Antimicrob Agents Chemother. 2015 Aug;59(8):4889-900. doi: 10.1128/AAC.00487-15. Epub 2015 Jun 8.

9.

Anti-HIV Nucleoside Phosphonate GS-9148 and Its Prodrug GS-9131: Scale Up of a 2'-F Modified Cyclic Nucleoside Phosphonate and Synthesis of Selected Amidate Prodrugs.

Mackman RL.

Curr Protoc Nucleic Acid Chem. 2014 Mar 26;56:14.10.1-21. doi: 10.1002/0471142700.nc1410s56. Review.

PMID:
25606977
10.

Discovery of an oral respiratory syncytial virus (RSV) fusion inhibitor (GS-5806) and clinical proof of concept in a human RSV challenge study.

Mackman RL, Sangi M, Sperandio D, Parrish JP, Eisenberg E, Perron M, Hui H, Zhang L, Siegel D, Yang H, Saunders O, Boojamra C, Lee G, Samuel D, Babaoglu K, Carey A, Gilbert BE, Piedra PA, Strickley R, Iwata Q, Hayes J, Stray K, Kinkade A, Theodore D, Jordan R, Desai M, Cihlar T.

J Med Chem. 2015 Feb 26;58(4):1630-43. doi: 10.1021/jm5017768. Epub 2015 Jan 27.

PMID:
25574686
11.

Oral GS-5806 activity in a respiratory syncytial virus challenge study.

DeVincenzo JP, Whitley RJ, Mackman RL, Scaglioni-Weinlich C, Harrison L, Farrell E, McBride S, Lambkin-Williams R, Jordan R, Xin Y, Ramanathan S, O'Riordan T, Lewis SA, Li X, Toback SL, Lin SL, Chien JW.

N Engl J Med. 2014 Aug 21;371(8):711-22. doi: 10.1056/NEJMoa1401184.

12.

Evaluation of 2'-α-fluorine modified nucleoside phosphonates as potential inhibitors of HCV polymerase.

Parrish JP, Lee SK, Boojamra CG, Hui H, Babusis D, Brown B, Shih IH, Feng JY, Ray AS, Mackman RL.

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3354-7. doi: 10.1016/j.bmcl.2013.03.095. Epub 2013 Apr 2.

PMID:
23639543
13.

Discovery of GS-9131: Design, synthesis and optimization of amidate prodrugs of the novel nucleoside phosphonate HIV reverse transcriptase (RT) inhibitor GS-9148.

Mackman RL, Ray AS, Hui HC, Zhang L, Birkus G, Boojamra CG, Desai MC, Douglas JL, Gao Y, Grant D, Laflamme G, Lin KY, Markevitch DY, Mishra R, McDermott M, Pakdaman R, Petrakovsky OV, Vela JE, Cihlar T.

Bioorg Med Chem. 2010 May 15;18(10):3606-17. doi: 10.1016/j.bmc.2010.03.041. Epub 2010 Mar 27.

PMID:
20409721
14.

Visualizing the molecular interactions of a nucleotide analog, GS-9148, with HIV-1 reverse transcriptase-DNA complex.

Lansdon EB, Samuel D, Lagpacan L, Brendza KM, White KL, Hung M, Liu X, Boojamra CG, Mackman RL, Cihlar T, Ray AS, McGrath ME, Swaminathan S.

J Mol Biol. 2010 Apr 9;397(4):967-78. doi: 10.1016/j.jmb.2010.02.019. Epub 2010 Feb 13.

PMID:
20156454
15.

Design, synthesis, and anti-HIV activity of 4'-modified carbocyclic nucleoside phosphonate reverse transcriptase inhibitors.

Boojamra CG, Parrish JP, Sperandio D, Gao Y, Petrakovsky OV, Lee SK, Markevitch DY, Vela JE, Laflamme G, Chen JM, Ray AS, Barron AC, Sparacino ML, Desai MC, Kim CU, Cihlar T, Mackman RL.

Bioorg Med Chem. 2009 Feb 15;17(4):1739-46. doi: 10.1016/j.bmc.2008.12.028. Epub 2008 Dec 24.

PMID:
19179082
16.

Synthesis of ethyl (1S,2R,3S,4S,5S)-2,3-O-(isopropylidene)-4-hydroxy-bicyclo[3.1.0]hexane-carboxylate from L-ribose: a versatile chiral synthon for preparation of adenosine and P2 receptor ligands.

Joshi BV, Melman A, Mackman RL, Jacobson KA.

Nucleosides Nucleotides Nucleic Acids. 2008 Mar;27(3):279-91. doi: 10.1080/15257770701845253.

PMID:
18260011
17.

Synthesis and anti-HIV activity of GS-9148 (2'-Fd4AP), a novel nucleoside phosphonate HIV reverse transcriptase inhibitor.

Boojamra CG, Mackman RL, Markevitch DY, Prasad V, Ray AS, Douglas J, Grant D, Kim CU, Cihlar T.

Bioorg Med Chem Lett. 2008 Feb 1;18(3):1120-3. doi: 10.1016/j.bmcl.2007.11.125. Epub 2007 Dec 5.

PMID:
18164198
18.

Synthesis and anti-HIV activity of 2'-fluorine modified nucleoside phosphonates: analogs of GS-9148.

Mackman RL, Lin KY, Boojamra CG, Hui H, Douglas J, Grant D, Petrakovsky O, Prasad V, Ray AS, Cihlar T.

Bioorg Med Chem Lett. 2008 Feb 1;18(3):1116-9. Epub 2007 Dec 5.

PMID:
18082402
19.

Synthesis and anti-HIV activity of cyclic pyrimidine phosphonomethoxy nucleosides and their prodrugs: a comparison of phosphonates and corresponding nucleosides.

Mackman RL, Zhang L, Prasad V, Boojamra CG, Chen J, Douglas J, Grant D, Laflamme G, Hui H, Kim CU, Parrish J, Stoycheva AD, Swaminathan S, Wang K, Cihlar T.

Nucleosides Nucleotides Nucleic Acids. 2007;26(6-7):573-7.

PMID:
18066858
20.

Design and profiling of GS-9148, a novel nucleotide analog active against nucleoside-resistant variants of human immunodeficiency virus type 1, and its orally bioavailable phosphonoamidate prodrug, GS-9131.

Cihlar T, Ray AS, Boojamra CG, Zhang L, Hui H, Laflamme G, Vela JE, Grant D, Chen J, Myrick F, White KL, Gao Y, Lin KY, Douglas JL, Parkin NT, Carey A, Pakdaman R, Mackman RL.

Antimicrob Agents Chemother. 2008 Feb;52(2):655-65. Epub 2007 Dec 3.

21.

Intracellular metabolism of the nucleotide prodrug GS-9131, a potent anti-human immunodeficiency virus agent.

Ray AS, Vela JE, Boojamra CG, Zhang L, Hui H, Callebaut C, Stray K, Lin KY, Gao Y, Mackman RL, Cihlar T.

Antimicrob Agents Chemother. 2008 Feb;52(2):648-54. Epub 2007 Dec 3.

22.

Synthesis, anti-HIV activity, and resistance profiles of ribose modified nucleoside phosphonates.

Mackman RL, Boojamra CG, Prasad V, Zhang L, Lin KY, Petrakovsky O, Babusis D, Chen J, Douglas J, Grant D, Hui HC, Kim CU, Markevitch DY, Vela J, Ray A, Cihlar T.

Bioorg Med Chem Lett. 2007 Dec 15;17(24):6785-9. Epub 2007 Oct 17.

PMID:
18029175
23.

Synthesis, anti-HIV activity, and resistance profile of thymidine phosphonomethoxy nucleosides and their bis-isopropyloxymethylcarbonyl (bisPOC) prodrugs.

Mackman RL, Zhang L, Prasad V, Boojamra CG, Douglas J, Grant D, Hui H, Kim CU, Laflamme G, Parrish J, Stoycheva AD, Swaminathan S, Wang K, Cihlar T.

Bioorg Med Chem. 2007 Aug 15;15(16):5519-28. Epub 2007 May 25.

PMID:
17562366
24.

Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA).

Katz BA, Luong C, Ho JD, Somoza JR, Gjerstad E, Tang J, Williams SR, Verner E, Mackman RL, Young WB, Sprengeler PA, Chan H, Mortara K, Janc JW, McGrath ME.

J Mol Biol. 2004 Nov 19;344(2):527-47.

PMID:
15522303
25.

Design and synthesis of beta-amino-alpha-hydroxy amide derivatives as inhibitors of MetAP2 and HUVEC growth.

Sendzik M, Janc JW, Cabuslay R, Honigberg L, Mackman RL, Magill C, Squires N, Waldeck N.

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3181-4.

PMID:
15149671
26.

Elaborate manifold of short hydrogen bond arrays mediating binding of active site-directed serine protease inhibitors.

Katz BA, Elrod K, Verner E, Mackman RL, Luong C, Shrader WD, Sendzik M, Spencer JR, Sprengeler PA, Kolesnikov A, Tai VW, Hui HC, Breitenbucher JG, Allen D, Janc JW.

J Mol Biol. 2003 May 23;329(1):93-120.

PMID:
12742021
27.

Contribution of multicentered short hydrogen bond arrays to potency of active site-directed serine protease inhibitors.

Katz BA, Spencer JR, Elrod K, Luong C, Mackman RL, Rice M, Sprengeler PA, Allen D, Janc J.

J Am Chem Soc. 2002 Oct 2;124(39):11657-68.

PMID:
12296731
28.

4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.

Spencer JR, McGee D, Allen D, Katz BA, Luong C, Sendzik M, Squires N, Mackman RL.

Bioorg Med Chem Lett. 2002 Aug 5;12(15):2023-6.

PMID:
12113833
29.

2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.

Mackman RL, Hui HC, Breitenbucher JG, Katz BA, Luong C, Martelli A, McGee D, Radika K, Sendzik M, Spencer JR, Sprengeler PA, Tario J, Verner E, Wang J.

Bioorg Med Chem Lett. 2002 Aug 5;12(15):2019-22.

PMID:
12113832
30.

Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets.

Katz BA, Sprengeler PA, Luong C, Verner E, Elrod K, Kirtley M, Janc J, Spencer JR, Breitenbucher JG, Hui H, McGee D, Allen D, Martelli A, Mackman RL.

Chem Biol. 2001 Nov;8(11):1107-21.

31.

Exploiting subsite S1 of trypsin-like serine proteases for selectivity: potent and selective inhibitors of urokinase-type plasminogen activator.

Mackman RL, Katz BA, Breitenbucher JG, Hui HC, Verner E, Luong C, Liu L, Sprengeler PA.

J Med Chem. 2001 Nov 8;44(23):3856-71.

PMID:
11689072
32.

Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasminogen activator and factor Xa.

Verner E, Katz BA, Spencer JR, Allen D, Hataye J, Hruzewicz W, Hui HC, Kolesnikov A, Li Y, Luong C, Martelli A, Radika K, Rai R, She M, Shrader W, Sprengeler PA, Trapp S, Wang J, Young WB, Mackman RL.

J Med Chem. 2001 Aug 16;44(17):2753-71.

PMID:
11495587
33.

A novel serine protease inhibition motif involving a multi-centered short hydrogen bonding network at the active site.

Katz BA, Elrod K, Luong C, Rice MJ, Mackman RL, Sprengeler PA, Spencer J, Hataye J, Janc J, Link J, Litvak J, Rai R, Rice K, Sideris S, Verner E, Young W.

J Mol Biol. 2001 Apr 13;307(5):1451-86.

PMID:
11292354
34.

CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation.

Brooks EE, Gray NS, Joly A, Kerwar SS, Lum R, Mackman RL, Norman TC, Rosete J, Rowe M, Schow SR, Schultz PG, Wang X, Wick MM, Shiffman D.

J Biol Chem. 1997 Nov 14;272(46):29207-11.

35.

Active-site topology of bovine cholesterol side-chain cleavage cytochrome P450 (P450scc) and evidence for interaction of tyrosine 94 with the side chain of cholesterol.

Pikuleva IA, Mackman RL, Kagawa N, Waterman MR, Ortiz de Montellano PR.

Arch Biochem Biophys. 1995 Sep 10;322(1):189-97.

PMID:
7574674
36.

Relationship of active site topology to substrate specificity for cytochrome P450terp (CYP108).

Fruetel JA, Mackman RL, Peterson JA, Ortiz de Montellano PR.

J Biol Chem. 1994 Nov 18;269(46):28815-21.

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