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Items: 20

1.

Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.

Verma SK, Tian X, LaFrance LV, Duquenne C, Suarez DP, Newlander KA, Romeril SP, Burgess JL, Grant SW, Brackley JA, Graves AP, Scherzer DA, Shu A, Thompson C, Ott HM, Aller GS, Machutta CA, Diaz E, Jiang Y, Johnson NW, Knight SD, Kruger RG, McCabe MT, Dhanak D, Tummino PJ, Creasy CL, Miller WH.

ACS Med Chem Lett. 2012 Oct 19;3(12):1091-6. doi: 10.1021/ml3003346. eCollection 2012 Dec 13.

2.

Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.

Adams ND, Adams JL, Burgess JL, Chaudhari AM, Copeland RA, Donatelli CA, Drewry DH, Fisher KE, Hamajima T, Hardwicke MA, Huffman WF, Koretke-Brown KK, Lai ZV, McDonald OB, Nakamura H, Newlander KA, Oleykowski CA, Parrish CA, Patrick DR, Plant R, Sarpong MA, Sasaki K, Schmidt SJ, Silva DJ, Sutton D, Tang J, Thompson CS, Tummino PJ, Wang JC, Xiang H, Yang J, Dhanak D.

J Med Chem. 2010 May 27;53(10):3973-4001. doi: 10.1021/jm901870q.

PMID:
20420387
3.

Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin.

Knight SD, Adams ND, Burgess JL, Chaudhari AM, Darcy MG, Donatelli CA, Luengo JI, Newlander KA, Parrish CA, Ridgers LH, Sarpong MA, Schmidt SJ, Van Aller GS, Carson JD, Diamond MA, Elkins PA, Gardiner CM, Garver E, Gilbert SA, Gontarek RR, Jackson JR, Kershner KL, Luo L, Raha K, Sherk CS, Sung CM, Sutton D, Tummino PJ, Wegrzyn RJ, Auger KR, Dhanak D.

ACS Med Chem Lett. 2010 Jan 19;1(1):39-43. doi: 10.1021/ml900028r. eCollection 2010 Apr 8.

4.

Discovery of the First Potent and Selective Inhibitor of Centromere-Associated Protein E: GSK923295.

Qian X, McDonald A, Zhou HJ, Adams ND, Parrish CA, Duffy KJ, Fitch DM, Tedesco R, Ashcraft LW, Yao B, Jiang H, Huang JK, Marin MV, Aroyan CE, Wang J, Ahmed S, Burgess JL, Chaudhari AM, Donatelli CA, Darcy MG, Ridgers LH, Newlander KA, Schmidt SJ, Chai D, Colón M, Zimmerman MN, Lad L, Sakowicz R, Schauer S, Belmont L, Baliga R, Pierce DW, Finer JT, Wang Z, Morgan BP, Morgans DJ Jr, Auger KR, Sung CM, Carson JD, Luo L, Hugger ED, Copeland RA, Sutton D, Elliott JD, Jackson JR, Wood KW, Dhanak D, Bergnes G, Knight SD.

ACS Med Chem Lett. 2010 Jan 19;1(1):30-4. doi: 10.1021/ml900018m. eCollection 2010 Apr 8.

5.

Novel ATP-competitive kinesin spindle protein inhibitors.

Parrish CA, Adams ND, Auger KR, Burgess JL, Carson JD, Chaudhari AM, Copeland RA, Diamond MA, Donatelli CA, Duffy KJ, Faucette LF, Finer JT, Huffman WF, Hugger ED, Jackson JR, Knight SD, Luo L, Moore ML, Newlander KA, Ridgers LH, Sakowicz R, Shaw AN, Sung CM, Sutton D, Wood KW, Zhang SY, Zimmerman MN, Dhanak D.

J Med Chem. 2007 Oct 4;50(20):4939-52. Epub 2007 Aug 29.

PMID:
17725339
6.

Indole naphthyridinones as inhibitors of bacterial enoyl-ACP reductases FabI and FabK.

Seefeld MA, Miller WH, Newlander KA, Burgess WJ, DeWolf WE Jr, Elkins PA, Head MS, Jakas DR, Janson CA, Keller PM, Manley PJ, Moore TD, Payne DJ, Pearson S, Polizzi BJ, Qiu X, Rittenhouse SF, Uzinskas IN, Wallis NG, Huffman WF.

J Med Chem. 2003 Apr 24;46(9):1627-35.

PMID:
12699381
7.

Defining and combating the mechanisms of triclosan resistance in clinical isolates of Staphylococcus aureus.

Fan F, Yan K, Wallis NG, Reed S, Moore TD, Rittenhouse SF, DeWolf WE Jr, Huang J, McDevitt D, Miller WH, Seefeld MA, Newlander KA, Jakas DR, Head MS, Payne DJ.

Antimicrob Agents Chemother. 2002 Nov;46(11):3343-7.

8.

Discovery of a novel and potent class of FabI-directed antibacterial agents.

Payne DJ, Miller WH, Berry V, Brosky J, Burgess WJ, Chen E, DeWolf WE Jr, Fosberry AP, Greenwood R, Head MS, Heerding DA, Janson CA, Jaworski DD, Keller PM, Manley PJ, Moore TD, Newlander KA, Pearson S, Polizzi BJ, Qiu X, Rittenhouse SF, Slater-Radosti C, Salyers KL, Seefeld MA, Smyth MG, Takata DT, Uzinskas IN, Vaidya K, Wallis NG, Winram SB, Yuan CC, Huffman WF.

Antimicrob Agents Chemother. 2002 Oct;46(10):3118-24.

9.

Discovery of aminopyridine-based inhibitors of bacterial enoyl-ACP reductase (FabI).

Miller WH, Seefeld MA, Newlander KA, Uzinskas IN, Burgess WJ, Heerding DA, Yuan CC, Head MS, Payne DJ, Rittenhouse SF, Moore TD, Pearson SC, Berry V, DeWolf WE Jr, Keller PM, Polizzi BJ, Qiu X, Janson CA, Huffman WF.

J Med Chem. 2002 Jul 18;45(15):3246-56.

PMID:
12109908
10.

Inhibitors of bacterial enoyl acyl carrier protein reductase (FabI): 2,9-disubstituted 1,2,3,4-tetrahydropyrido[3,4-b]indoles as potential antibacterial agents.

Seefeld MA, Miller WH, Newlander KA, Burgess WJ, Payne DJ, Rittenhouse SF, Moore TD, DeWolf WE Jr, Keller PM, Qiu X, Janson CA, Vaidya K, Fosberry AP, Smyth MG, Jaworski DD, Slater-Radosti C, Huffman WF.

Bioorg Med Chem Lett. 2001 Sep 3;11(17):2241-4.

PMID:
11527706
11.

Discovery of orally active nonpeptide vitronectin receptor antagonists based on a 2-benzazepine Gly-Asp mimetic.

Miller WH, Alberts DP, Bhatnagar PK, Bondinell WE, Callahan JF, Calvo RR, Cousins RD, Erhard KF, Heerding DA, Keenan RM, Kwon C, Manley PJ, Newlander KA, Ross ST, Samanen JM, Uzinskas IN, Venslavsky JW, Yuan CC, Haltiwanger RC, Gowen M, Hwang SM, James IE, Lark MW, Rieman DJ, Stroup GB, Azzarano LM, Salyers KL, Smith BR, Ward KW, Johanson KO, Huffman WF.

J Med Chem. 2000 Jan 13;43(1):22-6. No abstract available.

PMID:
10633035
12.

Preclinical pharmacokinetics and interspecies scaling of a novel vitronectin receptor antagonist.

Ward KW, Azzarano LM, Bondinell WE, Cousins RD, Huffman WF, Jakas DR, Keenan RM, Ku TW, Lundberg D, Miller WH, Mumaw JA, Newlander KA, Pirhalla JL, Roethke TJ, Salyers KL, Souder PR, Stelman GJ, Smith BR.

Drug Metab Dispos. 1999 Nov;27(11):1232-41.

PMID:
10534306
13.

Design and characterization of orally active Arg-Gly-Asp peptidomimetic vitronectin receptor antagonist SB 265123 for prevention of bone loss in osteoporosis.

Lark MW, Stroup GB, Hwang SM, James IE, Rieman DJ, Drake FH, Bradbeer JN, Mathur A, Erhard KF, Newlander KA, Ross ST, Salyers KL, Smith BR, Miller WH, Huffman WF, Gowen M.

J Pharmacol Exp Ther. 1999 Nov;291(2):612-7.

PMID:
10525079
14.

Orally bioavailable nonpeptide vitronectin receptor antagonists with efficacy in an osteoporosis model.

Miller WH, Bondinell WE, Cousins RD, Erhard KF, Jakas DR, Keenan RM, Ku TW, Newlander KA, Ross ST, Haltiwanger RC, Bradbeer J, Drake FH, Gowen M, Hoffman SJ, Hwang SM, James IE, Lark MW, Lechowska B, Rieman DJ, Stroup GB, Vasko-Moser JA, Zembryki DL, Azzarano LM, Adams PC, Huffman WF, et al.

Bioorg Med Chem Lett. 1999 Jul 5;9(13):1807-12.

PMID:
10406646
15.

Conformational preferences in a benzodiazepine series of potent nonpeptide fibrinogen receptor antagonists.

Keenan RM, Callahan JF, Samanen JM, Bondinell WE, Calvo RR, Chen L, DeBrosse C, Eggleston DS, Haltiwanger RC, Hwang SM, Jakas DR, Ku TW, Miller WH, Newlander KA, Nichols A, Parker MF, Southhall LS, Uzinskas I, Vasko-Moser JA, Venslavsky JW, Wong AS, Huffman WF.

J Med Chem. 1999 Feb 25;42(4):545-59.

PMID:
10052962
16.

Potent, selective, orally active 3-oxo-1,4-benzodiazepine GPIIb/IIIa integrin antagonists.

Samanen JM, Ali FE, Barton LS, Bondinell WE, Burgess JL, Callahan JF, Calvo RR, Chen W, Chen L, Erhard K, Feuerstein G, Heys R, Hwang SM, Jakas DR, Keenan RM, Ku TW, Kwon C, Lee CP, Miller WH, Newlander KA, Nichols A, Parker M, Peishoff CE, Rhodes G, Ross S, Shu A, Simpson R, Takata D, Yellin TO, Uzsinskas I, Venslavsky JW, Yuan CK, Huffman WF.

J Med Chem. 1996 Dec 6;39(25):4867-70. No abstract available.

PMID:
8960544
17.

A check on rational drug design: crystal structure of a complex of human immunodeficiency virus type 1 protease with a novel gamma-turn mimetic inhibitor.

Hoog SS, Zhao B, Winborne E, Fisher S, Green DW, DesJarlais RL, Newlander KA, Callahan JF, Moore ML, Huffman WF, et al.

J Med Chem. 1995 Aug 18;38(17):3246-52.

PMID:
7650677
18.

A novel constrained reduced-amide inhibitor of HIV-1 protease derived from the sequential incorporation of gamma-turn mimetics into a model substrate.

Newlander KA, Callahan JF, Moore ML, Tomaszek TA Jr, Huffman WF.

J Med Chem. 1993 Aug 6;36(16):2321-31.

PMID:
8360876
19.

A minor modification of residue 1 in potent vasopressin antagonists dramatically reduces agonist activity.

Huffman WF, Albrightson-Winslow C, Brickson B, Bryan HG, Caldwell N, Dytko G, Eggleston DS, Kinter LB, Moore ML, Newlander KA, et al.

J Med Chem. 1989 Apr;32(4):880-4.

PMID:
2522994
20.

Dicarbavasopressin antagonist analogues exhibit reduced in vivo agonist activity.

Moore ML, Albrightson C, Brickson B, Bryan HG, Caldwell N, Callahan JF, Foster J, Kinter LB, Newlander KA, Schmidt DB, et al.

J Med Chem. 1988 Aug;31(8):1487-9. No abstract available.

PMID:
3397986

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