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Items: 36

1.

Permeability of Cyclic Peptide Macrocycles and Cyclotides and Their Potential as Therapeutics.

Liras S, Mcclure KF.

ACS Med Chem Lett. 2019 Jun 14;10(7):1026-1032. doi: 10.1021/acsmedchemlett.9b00149. eCollection 2019 Jul 11.

PMID:
31312403
2.

Structural basis for selective stalling of human ribosome nascent chain complexes by a drug-like molecule.

Li W, Ward FR, McClure KF, Chang ST, Montabana E, Liras S, Dullea RG, Cate JHD.

Nat Struct Mol Biol. 2019 Jun;26(6):501-509. doi: 10.1038/s41594-019-0236-8. Epub 2019 Jun 3.

PMID:
31160784
3.

Discovery of N-(piperidin-3-yl)-N-(pyridin-2-yl)piperidine/piperazine-1-carboxamides as small molecule inhibitors of PCSK9.

Londregan AT, Aspnes G, Limberakis C, Loria PM, McClure KF, Petersen DN, Raymer B, Ruggeri RB, Wei L, Xiao J, Piotrowski DW.

Bioorg Med Chem Lett. 2018 Dec 15;28(23-24):3685-3688. doi: 10.1016/j.bmcl.2018.10.029. Epub 2018 Oct 22.

PMID:
30482620
4.

Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors: Hit to Lead Optimization of Systemic Agents.

Londregan AT, Wei L, Xiao J, Lintner NG, Petersen D, Dullea RG, McClure KF, Bolt MW, Warmus JS, Coffey SB, Limberakis C, Genovino J, Thuma BA, Hesp KD, Aspnes GE, Reidich B, Salatto CT, Chabot JR, Cate JHD, Liras S, Piotrowski DW.

J Med Chem. 2018 Jul 12;61(13):5704-5718. doi: 10.1021/acs.jmedchem.8b00650. Epub 2018 Jun 25.

PMID:
29878763
5.

Receptor-Mediated Delivery of CRISPR-Cas9 Endonuclease for Cell-Type-Specific Gene Editing.

Rouet R, Thuma BA, Roy MD, Lintner NG, Rubitski DM, Finley JE, Wisniewska HM, Mendonsa R, Hirsh A, de Oñate L, Compte Barrón J, McLellan TJ, Bellenger J, Feng X, Varghese A, Chrunyk BA, Borzilleri K, Hesp KD, Zhou K, Ma N, Tu M, Dullea R, McClure KF, Wilson RC, Liras S, Mascitti V, Doudna JA.

J Am Chem Soc. 2018 May 30;140(21):6596-6603. doi: 10.1021/jacs.8b01551. Epub 2018 May 18.

6.

Correction: Selective stalling of human translation through small-molecule engagement of the ribosome nascent chain.

Lintner NG, McClure KF, Petersen D, Londregan AT, Piotrowski DW, Wei L, Xiao J, Bolt M, Loria PM, Maguire B, Geoghegan KF, Huang A, Rolph T, Liras S, Doudna JA, Dullea RG, Cate JHD.

PLoS Biol. 2018 Apr 17;16(4):e1002628. doi: 10.1371/journal.pbio.1002628. eCollection 2018 Apr.

7.

Liver-Targeted Small-Molecule Inhibitors of Proprotein Convertase Subtilisin/Kexin Type 9 Synthesis.

McClure KF, Piotrowski DW, Petersen D, Wei L, Xiao J, Londregan AT, Kamlet AS, Dechert-Schmitt AM, Raymer B, Ruggeri RB, Canterbury D, Limberakis C, Liras S, DaSilva-Jardine P, Dullea RG, Loria PM, Reidich B, Salatto CT, Eng H, Kimoto E, Atkinson K, King-Ahmad A, Scott D, Beaumont K, Chabot JR, Bolt MW, Maresca K, Dahl K, Arakawa R, Takano A, Halldin C.

Angew Chem Int Ed Engl. 2017 Dec 18;56(51):16218-16222. doi: 10.1002/anie.201708744. Epub 2017 Nov 24.

PMID:
29073340
8.

Selective stalling of human translation through small-molecule engagement of the ribosome nascent chain.

Lintner NG, McClure KF, Petersen D, Londregan AT, Piotrowski DW, Wei L, Xiao J, Bolt M, Loria PM, Maguire B, Geoghegan KF, Huang A, Rolph T, Liras S, Doudna JA, Dullea RG, Cate JH.

PLoS Biol. 2017 Mar 21;15(3):e2001882. doi: 10.1371/journal.pbio.2001882. eCollection 2017 Mar. Erratum in: PLoS Biol. 2018 Apr 17;16(4):e1002628.

9.

Pharmacological characterization of the first in class clinical candidate PF-05190457: a selective ghrelin receptor competitive antagonist with inverse agonism that increases vagal afferent firing and glucose-dependent insulin secretion ex vivo.

Kong J, Chuddy J, Stock IA, Loria PM, Straub SV, Vage C, Cameron KO, Bhattacharya SK, Lapham K, McClure KF, Zhang Y, Jackson VM.

Br J Pharmacol. 2016 May;173(9):1452-64. doi: 10.1111/bph.13439. Epub 2016 Mar 17.

10.

Evaluation and synthesis of polar aryl- and heteroaryl spiroazetidine-piperidine acetamides as ghrelin inverse agonists.

Orr ST, Beveridge R, Bhattacharya SK, Cameron KO, Coffey S, Fernando D, Hepworth D, Jackson MV, Khot V, Kosa R, Lapham K, Loria PM, McClure KF, Patel J, Rose C, Saenz J, Stock IA, Storer G, von Volkenburg M, Vrieze D, Wang G, Xiao J, Zhang Y.

ACS Med Chem Lett. 2014 Dec 14;6(2):156-61. doi: 10.1021/ml500414n. eCollection 2015 Feb 12.

11.

Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate.

Bhattacharya SK, Andrews K, Beveridge R, Cameron KO, Chen C, Dunn M, Fernando D, Gao H, Hepworth D, Jackson VM, Khot V, Kong J, Kosa RE, Lapham K, Loria PM, Londregan AT, McClure KF, Orr ST, Patel J, Rose C, Saenz J, Stock IA, Storer G, VanVolkenburg M, Vrieze D, Wang G, Xiao J, Zhang Y.

ACS Med Chem Lett. 2014 Feb 24;5(5):474-9. doi: 10.1021/ml400473x. eCollection 2014 May 8.

12.

Design and synthesis of truncated EGF-A peptides that restore LDL-R recycling in the presence of PCSK9 in vitro.

Schroeder CI, Swedberg JE, Withka JM, Rosengren KJ, Akcan M, Clayton DJ, Daly NL, Cheneval O, Borzilleri KA, Griffor M, Stock I, Colless B, Walsh P, Sunderland P, Reyes A, Dullea R, Ammirati M, Liu S, McClure KF, Tu M, Bhattacharya SK, Liras S, Price DA, Craik DJ.

Chem Biol. 2014 Feb 20;21(2):284-94. doi: 10.1016/j.chembiol.2013.11.014. Epub 2014 Jan 16.

13.

Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor.

McClure KF, Jackson M, Cameron KO, Kung DW, Perry DA, Orr ST, Zhang Y, Kohrt J, Tu M, Gao H, Fernando D, Jones R, Erasga N, Wang G, Polivkova J, Jiao W, Swartz R, Ueno H, Bhattacharya SK, Stock IA, Varma S, Bagdasarian V, Perez S, Kelly-Sullivan D, Wang R, Kong J, Cornelius P, Michael L, Lee E, Janssen A, Steyn SJ, Lapham K, Goosen T.

Bioorg Med Chem Lett. 2013 Oct 1;23(19):5410-4. doi: 10.1016/j.bmcl.2013.07.044. Epub 2013 Jul 30.

PMID:
23953189
14.

Enantioselective hydroarylation of bridged [3.2.1] heterocycles: an efficient entry into the homoepibatidine skeleton.

Brawn RA, Guimarães CR, McClure KF, Liras S.

Org Lett. 2013 Jul 5;15(13):3424-7. doi: 10.1021/ol401477r. Epub 2013 Jun 21.

PMID:
23790034
15.

Design and synthesis of diazatricyclodecane agonists of the G-protein-coupled receptor 119.

Darout E, Robinson RP, McClure KF, Corbett M, Li B, Shavnya A, Andrews MP, Jones CS, Li Q, Minich ML, Mascitti V, Guimarães CR, Munchhof MJ, Bahnck KB, Cai C, Price DA, Liras S, Bonin PD, Cornelius P, Wang R, Bagdasarian V, Sobota CP, Hornby S, Masterson VM, Joseph RM, Kalgutkar AS, Chen Y.

J Med Chem. 2013 Jan 10;56(1):301-19. doi: 10.1021/jm301626p. Epub 2012 Dec 31.

PMID:
23234271
16.

From partial to full agonism: identification of a novel 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole as a full agonist of the human GPR119 receptor.

Futatsugi K, Mascitti V, Guimarães CR, Morishita N, Cai C, DeNinno MP, Gao H, Hamilton MD, Hank R, Harris AR, Kung DW, Lavergne SY, Lefker BA, Lopaze MG, McClure KF, Munchhof MJ, Preville C, Robinson RP, Wright SW, Bonin PD, Cornelius P, Chen Y, Kalgutkar AS.

Bioorg Med Chem Lett. 2013 Jan 1;23(1):194-7. doi: 10.1016/j.bmcl.2012.10.119. Epub 2012 Nov 5.

PMID:
23177788
17.

An efficient synthesis of bridged heterocycles from an Ir(I) bis-amination/ring-closing metathesis sequence.

Brawn RA, Guimarães CR, McClure KF, Liras S.

Org Lett. 2012 Sep 21;14(18):4802-5. Epub 2012 Sep 6.

PMID:
22953715
18.

Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor.

Kung DW, Coffey SB, Jones RM, Cabral S, Jiao W, Fichtner M, Carpino PA, Rose CR, Hank RF, Lopaze MG, Swartz R, Chen HT, Hendsch Z, Posner B, Wielis CF, Manning B, Dubins J, Stock IA, Varma S, Campbell M, DeBartola D, Kosa-Maines R, Steyn SJ, McClure KF.

Bioorg Med Chem Lett. 2012 Jul 1;22(13):4281-7. doi: 10.1016/j.bmcl.2012.05.024. Epub 2012 May 17.

PMID:
22677316
19.

Oxidative metabolism of a quinoxaline derivative by xanthine oxidase in rodent plasma.

Sharma R, Eng H, Walker GS, Barreiro G, Stepan AF, McClure KF, Wolford A, Bonin PD, Cornelius P, Kalgutkar AS.

Chem Res Toxicol. 2011 Dec 19;24(12):2207-16. doi: 10.1021/tx200329k. Epub 2011 Oct 4.

PMID:
21939274
20.

Activation of the G-protein-coupled receptor 119: a conformation-based hypothesis for understanding agonist response.

McClure KF, Darout E, Guimarães CR, DeNinno MP, Mascitti V, Munchhof MJ, Robinson RP, Kohrt J, Harris AR, Moore DE, Li B, Samp L, Lefker BA, Futatsugi K, Kung D, Bonin PD, Cornelius P, Wang R, Salter E, Hornby S, Kalgutkar AS, Chen Y.

J Med Chem. 2011 Mar 24;54(6):1948-52. doi: 10.1021/jm200003p. Epub 2011 Mar 1.

PMID:
21361292
21.

Design and evaluation of a 2-(2,3,6-trifluorophenyl)acetamide derivative as an agonist of the GPR119 receptor.

Mascitti V, Stevens BD, Choi C, McClure KF, Guimarães CR, Farley KA, Munchhof MJ, Robinson RP, Futatsugi K, Lavergne SY, Lefker BA, Cornelius P, Bonin PD, Kalgutkar AS, Sharma R, Chen Y.

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1306-9. doi: 10.1016/j.bmcl.2011.01.088. Epub 2011 Jan 25.

PMID:
21310611
22.

Intrinsic electrophilicity of a 4-substituted-5-cyano-6-(2-methylpyridin-3-yloxy)pyrimidine derivative: structural characterization of glutathione conjugates in vitro.

Kalgutkar AS, Mascitti V, Sharma R, Walker GW, Ryder T, McDonald TS, Chen Y, Preville C, Basak A, McClure KF, Kohrt JT, Robinson RP, Munchhof MJ, Cornelius P.

Chem Res Toxicol. 2011 Feb 18;24(2):269-78. doi: 10.1021/tx100429x. Epub 2011 Feb 3.

PMID:
21288051
23.

Continued exploration of the triazolopyridine scaffold as a platform for p38 MAP kinase inhibition.

Jerome KD, Rucker PV, Xing L, Shieh HS, Baldus JE, Selness SR, Letavic MA, Braganza JF, McClure KF.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):469-73. doi: 10.1016/j.bmcl.2009.11.114. Epub 2009 Nov 26.

PMID:
19969459
24.

Biochemical basis for differences in metabolism-dependent genotoxicity by two diazinylpiperazine-based 5-HT2C receptor agonists.

Kalgutkar AS, Bauman JN, McClure KF, Aubrecht J, Cortina SR, Paralkar J.

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1559-63. doi: 10.1016/j.bmcl.2009.02.032. Epub 2009 Feb 12.

PMID:
19246199
25.

Genotoxicity of 2-(3-chlorobenzyloxy)-6-(piperazinyl)pyrazine, a novel 5-hydroxytryptamine2c receptor agonist for the treatment of obesity: role of metabolic activation.

Kalgutkar AS, Dalvie DK, Aubrecht J, Smith EB, Coffing SL, Cheung JR, Vage C, Lame ME, Chiang P, McClure KF, Maurer TS, Coelho RV Jr, Soliman VF, Schildknegt K.

Drug Metab Dispos. 2007 Jun;35(6):848-58. Epub 2007 Mar 7.

PMID:
17344339
26.
27.

Structure-activity relationships of triazolopyridine oxazole p38 inhibitors: identification of candidates for clinical development.

McClure KF, Letavic MA, Kalgutkar AS, Gabel CA, Audoly L, Barberia JT, Braganza JF, Carter D, Carty TJ, Cortina SR, Dombroski MA, Donahue KM, Elliott NC, Gibbons CP, Jordan CK, Kuperman AV, Labasi JM, Laliberte RE, McCoy JM, Naiman BM, Nelson KL, Nguyen HT, Peese KM, Sweeney FJ, Taylor TJ, Trebino CE, Abramov YA, Laird ER, Volberg WA, Zhou J, Bach J, Lombardo F.

Bioorg Med Chem Lett. 2006 Aug 15;16(16):4339-44. Epub 2006 Jun 12.

PMID:
16759861
28.

Theoretical and experimental design of atypical kinase inhibitors: application to p38 MAP kinase.

McClure KF, Abramov YA, Laird ER, Barberia JT, Cai W, Carty TJ, Cortina SR, Danley DE, Dipesa AJ, Donahue KM, Dombroski MA, Elliott NC, Gabel CA, Han S, Hynes TR, Lemotte PK, Mansour MN, Marr ES, Letavic MA, Pandit J, Ripin DB, Sweeney FJ, Tan D, Tao Y.

J Med Chem. 2005 Sep 8;48(18):5728-37.

PMID:
16134941
29.

Pyran-containing sulfonamide hydroxamic acids: potent MMP inhibitors that spare MMP-1.

Reiter LA, Robinson RP, McClure KF, Jones CS, Reese MR, Mitchell PG, Otterness IG, Bliven ML, Liras J, Cortina SR, Donahue KM, Eskra JD, Griffiths RJ, Lame ME, Lopez-Anaya A, Martinelli GJ, McGahee SM, Yocum SA, Lopresti-Morrow LL, Tobiassen LM, Vaughn-Bowser ML.

Bioorg Med Chem Lett. 2004 Jul 5;14(13):3389-95.

PMID:
15177439
30.

Benzimidazolone p38 inhibitors.

Dombroski MA, Letavic MA, McClure KF, Barberia JT, Carty TJ, Cortina SR, Csiki C, Dipesa AJ, Elliott NC, Gabel CA, Jordan CK, Labasi JM, Martin WH, Peese KM, Stock IA, Svensson L, Sweeney FJ, Yu CH.

Bioorg Med Chem Lett. 2004 Feb 23;14(4):919-23.

PMID:
15012994
31.

Synthesis and biological activity of selective pipecolic acid-based TNF-alpha converting enzyme (TACE) inhibitors.

Letavic MA, Axt MZ, Barberia JT, Carty TJ, Danley DE, Geoghegan KF, Halim NS, Hoth LR, Kamath AV, Laird ER, Lopresti-Morrow LL, McClure KF, Mitchell PG, Natarajan V, Noe MC, Pandit J, Reeves L, Schulte GK, Snow SL, Sweeney FJ, Tan DH, Yu CH.

Bioorg Med Chem Lett. 2002 May 20;12(10):1387-90.

PMID:
11992783
32.

New Insights into Disintegrin Metalloproteases.

Carty TJ, LoPresti-Morrow LL, Mitchell PG, McNiff PA, McClure KF.

Inflamm Res. 1999 May;48(5):229-31. No abstract available.

PMID:
10391108
33.

Matrix metalloproteinase inhibition attenuates early left ventricular enlargement after experimental myocardial infarction in mice.

Rohde LE, Ducharme A, Arroyo LH, Aikawa M, Sukhova GH, Lopez-Anaya A, McClure KF, Mitchell PG, Libby P, Lee RT.

Circulation. 1999 Jun 15;99(23):3063-70.

PMID:
10368126
34.

Alkylation of succinates: synthesis of Ro 32-3555.

McClure KF, Axt MZ.

Bioorg Med Chem Lett. 1998 Jan 20;8(2):143-6.

PMID:
9871642
35.

Template-nucleated alanine-lysine helices are stabilized by position-dependent interactions between the lysine side chain and the helix barrel.

Groebke K, Renold P, Tsang KY, Allen TJ, McClure KF, Kemp DS.

Proc Natl Acad Sci U S A. 1996 Apr 30;93(9):4025-9.

36.

A strategy for the solid-phase synthesis of oligosaccharides.

Danishefsky SJ, McClure KF, Randolph JT, Ruggeri RB.

Science. 1993 May 28;260(5112):1307-9.

PMID:
8493573

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