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Items: 39

1.

MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology.

Boga SB, Deng Y, Zhu L, Nan Y, Cooper AB, Shipps GW Jr, Doll R, Shih NY, Zhu H, Sun R, Wang T, Paliwal S, Tsui HC, Gao X, Yao X, Desai J, Wang J, Alhassan AB, Kelly J, Patel M, Muppalla K, Gudipati S, Zhang LK, Buevich A, Hesk D, Carr D, Dayananth P, Black S, Mei H, Cox K, Sherborne B, Hruza AW, Xiao L, Jin W, Long B, Liu G, Taylor SA, Kirschmeier P, Windsor WT, Bishop R, Samatar AA.

ACS Med Chem Lett. 2018 Jun 14;9(7):761-767. doi: 10.1021/acsmedchemlett.8b00220. eCollection 2018 Jul 12.

2.

Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology.

Boga SB, Alhassan AB, Cooper AB, Doll R, Shih NY, Shipps G, Deng Y, Zhu H, Nan Y, Sun R, Zhu L, Desai J, Patel M, Muppalla K, Gao X, Wang J, Yao X, Kelly J, Gudipati S, Paliwal S, Tsui HC, Wang T, Sherborne B, Xiao L, Hruza A, Buevich A, Zhang LK, Hesk D, Samatar AA, Carr D, Long B, Black S, Dayananth P, Windsor W, Kirschmeier P, Bishop R.

Bioorg Med Chem Lett. 2018 Jun 15;28(11):2029-2034. doi: 10.1016/j.bmcl.2018.04.063. Epub 2018 Apr 26.

PMID:
29748051
3.

Development of MK-8353, an orally administered ERK1/2 inhibitor, in patients with advanced solid tumors.

Moschos SJ, Sullivan RJ, Hwu WJ, Ramanathan RK, Adjei AA, Fong PC, Shapira-Frommer R, Tawbi HA, Rubino J, Rush TS 3rd, Zhang D, Miselis NR, Samatar AA, Chun P, Rubin EH, Schiller J, Long BJ, Dayananth P, Carr D, Kirschmeier P, Bishop WR, Deng Y, Cooper A, Shipps GW, Moreno BH, Robert L, Ribas A, Flaherty KT.

JCI Insight. 2018 Feb 22;3(4). pii: 92352. doi: 10.1172/jci.insight.92352. eCollection 2018 Feb 22.

4.

Corrigendum to "1-Thiazol-2-yl-N-3-methyl-1H-pyrozole-5-carboxylic acid derivatives as antitumor agents" [Bioorg. Med. Chem. Lett. 27 (2017) 4471-4477].

Cooper AB, Ciblat S, Shipps G, Levine J, Kostura M, Oza V, Constantineau-Forget L, Dery M, Grand-Maitre C, Bruneau-Latour N, Bellavance E, Patane M, Siddiqui A, Luther M.

Bioorg Med Chem Lett. 2018 Mar 1;28(5):985. doi: 10.1016/j.bmcl.2018.01.046. Epub 2018 Feb 9. No abstract available.

PMID:
29433931
5.

1-Thiazol-2-yl-N-3-methyl-1H-pyrozole-5-carboxylic acid derivatives as antitumor agents.

Cooper AB, Ciblat S, Shipps G, Levine J, Kostura M, Oza V, Constantineau-Forget L, Dery M, Grand-Maitre C, Bruneau-Latour N, Bellavance E, Patane M, Siddiqui A, Luther M.

Bioorg Med Chem Lett. 2017 Sep 15;27(18):4471-4477. doi: 10.1016/j.bmcl.2017.08.003. Epub 2017 Aug 2. Erratum in: Bioorg Med Chem Lett. 2018 Feb 9;:.

PMID:
28844391
6.

Structure-activity relationship study of 4-substituted piperidines at Leu26 moiety of novel p53-hDM2 inhibitors.

Tian Y, Ma Y, Gibeau CR, Lahue BR, Shipps GW Jr, Strickland C, Bogen SL.

Bioorg Med Chem Lett. 2016 Jun 1;26(11):2735-8. doi: 10.1016/j.bmcl.2016.03.078. Epub 2016 Mar 23.

PMID:
27080185
7.

Discovery of Novel 3,3-Disubstituted Piperidines as Orally Bioavailable, Potent, and Efficacious HDM2-p53 Inhibitors.

Bogen SL, Pan W, Gibeau CR, Lahue BR, Ma Y, Nair LG, Seigel E, Shipps GW Jr, Tian Y, Wang Y, Lin Y, Liu M, Liu S, Mirza A, Wang X, Lipari P, Seidel-Dugan C, Hicklin DJ, Bishop WR, Rindgen D, Nomeir A, Prosise W, Reichert P, Scapin G, Strickland C, Doll RJ.

ACS Med Chem Lett. 2016 Jan 20;7(3):324-9. doi: 10.1021/acsmedchemlett.5b00472. eCollection 2016 Mar 10.

8.

Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.

Deng Y, Shipps GW Jr, Cooper A, English JM, Annis DA, Carr D, Nan Y, Wang T, Zhu HY, Chuang CC, Dayananth P, Hruza AW, Xiao L, Jin W, Kirschmeier P, Windsor WT, Samatar AA.

J Med Chem. 2014 Nov 13;57(21):8817-26. doi: 10.1021/jm500847m. Epub 2014 Oct 22.

PMID:
25313996
9.

Pivotal Role of an Aliphatic Side Chain in the Development of an HDM2 Inhibitor.

Ma Y, Lahue BR, Gibeau CR, Shipps GW Jr, Bogen SL, Wang Y, Guo Z, Guzi TJ.

ACS Med Chem Lett. 2014 Feb 24;5(5):572-5. doi: 10.1021/ml500019s. eCollection 2014 May 8.

10.

Core modification of substituted piperidines as novel inhibitors of HDM2-p53 protein-protein interaction.

Pan W, Lahue BR, Ma Y, Nair LG, Shipps GW Jr, Wang Y, Doll R, Bogen SL.

Bioorg Med Chem Lett. 2014 Apr 15;24(8):1983-6. doi: 10.1016/j.bmcl.2014.02.055. Epub 2014 Feb 28.

PMID:
24656661
11.

Substituted piperidines as HDM2 inhibitors.

Ma Y, Lahue BR, Shipps GW Jr, Brookes J, Wang Y.

Bioorg Med Chem Lett. 2014 Feb 15;24(4):1026-30. doi: 10.1016/j.bmcl.2014.01.026. Epub 2014 Jan 17.

PMID:
24486134
12.

Modulating the interaction between CDK2 and cyclin A with a quinoline-based inhibitor.

Deng Y, Shipps GW Jr, Zhao L, Siddiqui MA, Popovici-Muller J, Curran PJ, Duca JS, Hruza AW, Fischmann TO, Madison VS, Zhang R, McNemar CW, Mayhood TW, Syto R, Annis A, Kirschmeier P, Lees EM, Parry DA, Windsor WT.

Bioorg Med Chem Lett. 2014 Jan 1;24(1):199-203. doi: 10.1016/j.bmcl.2013.11.041. Epub 2013 Nov 23.

PMID:
24332088
13.

Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors.

Morris EJ, Jha S, Restaino CR, Dayananth P, Zhu H, Cooper A, Carr D, Deng Y, Jin W, Black S, Long B, Liu J, Dinunzio E, Windsor W, Zhang R, Zhao S, Angagaw MH, Pinheiro EM, Desai J, Xiao L, Shipps G, Hruza A, Wang J, Kelly J, Paliwal S, Gao X, Babu BS, Zhu L, Daublain P, Zhang L, Lutterbach BA, Pelletier MR, Philippar U, Siliphaivanh P, Witter D, Kirschmeier P, Bishop WR, Hicklin D, Gilliland DG, Jayaraman L, Zawel L, Fawell S, Samatar AA.

Cancer Discov. 2013 Jul;3(7):742-50. doi: 10.1158/2159-8290.CD-13-0070. Epub 2013 Apr 24.

14.

Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors.

Huang X, Cheng CC, Fischmann TO, Duca JS, Richards M, Tadikonda PK, Reddy PA, Zhao L, Siddiqui MA, Parry D, Davis N, Seghezzi W, Wiswell D, Shipps GW Jr.

Bioorg Med Chem Lett. 2013 May 1;23(9):2590-4. doi: 10.1016/j.bmcl.2013.02.108. Epub 2013 Mar 7.

PMID:
23535330
15.

Discovery of liver-targeted inhibitors of stearoyl-CoA desaturase (SCD1).

Deng Y, Yang Z, Shipps GW Jr, Lo SM, West R, Hwa J, Zheng S, Farley C, Lachowicz J, van Heek M, Bass AS, Sinha DP, Mahon CR, Cartwright ME.

Bioorg Med Chem Lett. 2013 Feb 1;23(3):791-6. doi: 10.1016/j.bmcl.2012.11.075. Epub 2012 Dec 5.

PMID:
23265904
16.

Application of affinity selection-mass spectrometry assays to purification and affinity-based screening of the chemokine receptor CXCR4.

Whitehurst CE, Yao Z, Murphy D, Zhang M, Taremi S, Wojcik L, Strizki JM, Bracken JD, Cheng CC, Yang X, Shipps GW Jr, Ziebell M, Nickbarg E.

Comb Chem High Throughput Screen. 2012 Jul;15(6):473-85.

PMID:
22651846
17.

Discovery of a Novel Series of CHK1 Kinase Inhibitors with a Distinctive Hinge Binding Mode.

Huang X, Cheng CC, Fischmann TO, Duca JS, Yang X, Richards M, Shipps GW Jr.

ACS Med Chem Lett. 2012 Jan 20;3(2):123-8. doi: 10.1021/ml200249h. eCollection 2012 Feb 9.

18.

Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors.

Zeng H, Belanger DB, Curran PJ, Shipps GW Jr, Miao H, Bracken JB, Arshad Siddiqui M, Malkowski M, Wang Y.

Bioorg Med Chem Lett. 2011 Oct 1;21(19):5870-5. doi: 10.1016/j.bmcl.2011.07.101. Epub 2011 Aug 3.

PMID:
21855335
19.

Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors.

Huang X, Shipps GW Jr, Cheng CC, Spacciapoli P, Zhang X, McCoy MA, Wyss DF, Yang X, Achab A, Soucy K, Montavon DK, Murphy DM, Whitehurst CE.

ACS Med Chem Lett. 2011 Jun 24;2(8):632-7. doi: 10.1021/ml200113y. eCollection 2011 Aug 11.

20.

Small molecule inhibition of the TNF family cytokine CD40 ligand through a subunit fracture mechanism.

Silvian LF, Friedman JE, Strauch K, Cachero TG, Day ES, Qian F, Cunningham B, Fung A, Sun L, Shipps GW, Su L, Zheng Z, Kumaravel G, Whitty A.

ACS Chem Biol. 2011 Jun 17;6(6):636-47. doi: 10.1021/cb2000346. Epub 2011 Apr 20. Erratum in: ACS Chem Biol. 2011 Jul 15;6(7):761. Shipps, Gerald W [added].

21.

Small-molecule inhibitors of FABP4/5 ameliorate dyslipidemia but not insulin resistance in mice with diet-induced obesity.

Lan H, Cheng CC, Kowalski TJ, Pang L, Shan L, Chuang CC, Jackson J, Rojas-Triana A, Bober L, Liu L, Voigt J, Orth P, Yang X, Shipps GW Jr, Hedrick JA.

J Lipid Res. 2011 Apr;52(4):646-56. doi: 10.1194/jlr.M012757. Epub 2011 Feb 4.

22.

Pyridine Carboxamides: Potent Palm Site Inhibitors of HCV NS5B Polymerase.

Cheng CC, Huang X, Shipps GW Jr, Wang YS, Wyss DF, Soucy KA, Jiang CK, Agrawal S, Ferrari E, He Z, Huang HC.

ACS Med Chem Lett. 2010 Aug 17;1(9):466-71. doi: 10.1021/ml100128h. eCollection 2010 Dec 9.

23.

Novel benzimidazole inhibitors bind to a unique site in the kinesin spindle protein motor domain.

Sheth PR, Shipps GW Jr, Seghezzi W, Smith CK, Chuang CC, Sanden D, Basso AD, Vilenchik L, Gray K, Annis DA, Nickbarg E, Ma Y, Lahue B, Herbst R, Le HV.

Biochemistry. 2010 Sep 28;49(38):8350-8. doi: 10.1021/bi1005283.

PMID:
20718440
24.

Structure and activity relationships of tartrate-based TACE inhibitors.

Li D, Popovici-Muller J, Belanger DB, Caldwell J, Dai C, David M, Girijavallabhan VM, Lavey BJ, Lee JF, Liu Z, Mazzola R, Rizvi R, Rosner KE, Shankar B, Spitler J, Ting PC, Vaccaro H, Yu W, Zhou G, Zhu Z, Niu X, Sun J, Guo Z, Orth P, Chen S, Kozlowski JA, Lundell DJ, Madison V, McKittrick B, Piwinski JJ, Shih NY, Shipps GW Jr, Siddiqui MA, Strickland CO.

Bioorg Med Chem Lett. 2010 Aug 15;20(16):4812-5. doi: 10.1016/j.bmcl.2010.06.104. Epub 2010 Jun 25.

PMID:
20638281
25.

Inhibitors of hepatitis C virus polymerase: synthesis and characterization of novel 2-oxy-6-fluoro-N-((S)-1-hydroxy-3-phenylpropan-2-yl)-benzamides.

Cheng CC, Shipps GW Jr, Yang Z, Kawahata N, Lesburg CA, Duca JS, Bandouveres J, Bracken JD, Jiang CK, Agrawal S, Ferrari E, Huang HC.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2119-24. doi: 10.1016/j.bmcl.2010.02.054. Epub 2010 Feb 18.

PMID:
20219368
26.

The discovery of novel tartrate-based TNF-alpha converting enzyme (TACE) inhibitors.

Rosner KE, Guo Z, Orth P, Shipps GW Jr, Belanger DB, Chan TY, Curran PJ, Dai C, Deng Y, Girijavallabhan VM, Hong L, Lavey BJ, Lee JF, Li D, Liu Z, Popovici-Muller J, Ting PC, Vaccaro H, Wang L, Wang T, Yu W, Zhou G, Niu X, Sun J, Kozlowski JA, Lundell DJ, Madison V, McKittrick B, Piwinski JJ, Shih NY, Arshad Siddiqui M, Strickland CO.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1189-93. doi: 10.1016/j.bmcl.2009.12.004. Epub 2009 Dec 5.

PMID:
20022498
27.

Discovery and optimization of antibacterial AccC inhibitors.

Cheng CC, Shipps GW Jr, Yang Z, Sun B, Kawahata N, Soucy KA, Soriano A, Orth P, Xiao L, Mann P, Black T.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6507-14. doi: 10.1016/j.bmcl.2009.10.057. Epub 2009 Oct 28.

PMID:
19875284
28.

Pyrazolo[1,5-a]pyrimidine-based inhibitors of HCV polymerase.

Popovici-Muller J, Shipps GW Jr, Rosner KE, Deng Y, Wang T, Curran PJ, Brown MA, Siddiqui MA, Cooper AB, Duca J, Cable M, Girijavallabhan V.

Bioorg Med Chem Lett. 2009 Nov 15;19(22):6331-6. doi: 10.1016/j.bmcl.2009.09.087. Epub 2009 Sep 25.

PMID:
19819138
29.

Discovery of 4H-pyrazolo[1,5-a]pyrimidin-7-ones as potent inhibitors of hepatitis C virus polymerase.

Deng Y, Shipps GW Jr, Wang T, Popovici-Muller J, Rosner KE, Siddiqui MA, Duca J, Cooper AB, Cable M.

Bioorg Med Chem Lett. 2009 Sep 15;19(18):5363-7. doi: 10.1016/j.bmcl.2009.07.124. Epub 2009 Aug 6.

PMID:
19682898
30.

Inhibitors of the lipid phosphatase SHIP2 discovered by high-throughput affinity selection-mass spectrometry screening of combinatorial libraries.

Annis DA, Cheng CC, Chuang CC, McCarter JD, Nash HM, Nazef N, Rowe T, Kurzeja RJ, Shipps GW Jr.

Comb Chem High Throughput Screen. 2009 Sep;12(8):760-71. Epub 2009 Sep 1.

PMID:
19531013
31.

Substituted benzimidazoles: A novel chemotype for small molecule hKSP inhibitors.

Lahue BR, Ma Y, Shipps GW Jr, Seghezzi W, Herbst R.

Bioorg Med Chem Lett. 2009 Jul 1;19(13):3405-9. doi: 10.1016/j.bmcl.2009.05.040. Epub 2009 May 18.

PMID:
19481450
32.

Method for quantitative protein-ligand affinity measurements in compound mixtures.

Annis DA, Shipps GW Jr, Deng Y, Popovici-Müller J, Siddiqui MA, Curran PJ, Gowen M, Windsor WT.

Anal Chem. 2007 Jun 15;79(12):4538-42. Epub 2007 May 15.

PMID:
17500537
33.

Discovery and characterization of orthosteric and allosteric muscarinic M2 acetylcholine receptor ligands by affinity selection-mass spectrometry.

Whitehurst CE, Nazef N, Annis DA, Hou Y, Murphy DM, Spacciapoli P, Yao Z, Ziebell MR, Cheng CC, Shipps GW Jr, Felsch JS, Lau D, Nash HM.

J Biomol Screen. 2006 Mar;11(2):194-207. Epub 2006 Feb 20.

PMID:
16490772
34.

Aminothiazole inhibitors of HCV RNA polymerase.

Shipps GW Jr, Deng Y, Wang T, Popovici-Muller J, Curran PJ, Rosner KE, Cooper AB, Girijavallabhan V, Butkiewicz N, Cable M.

Bioorg Med Chem Lett. 2005 Jan 3;15(1):115-9.

PMID:
15582422
35.

Bocdene and mocdene derivatives of catechols and catecholamines.

Ariza X, Pineda O, Vilarrasa J, Shipps GW Jr, Ma Y, Dai X.

Org Lett. 2001 May 3;3(9):1399-401.

PMID:
11348244
36.

Synthesis and screening of small molecule libraries active in binding to DNA.

Shipps GW Jr, Pryor KE, Xian J, Skyler DA, Davidson EH, Rebek J Jr.

Proc Natl Acad Sci U S A. 1997 Oct 28;94(22):11833-8.

37.

Application of capillary electrophoresis-electrospray ionization mass spectometry in the determination of molecular diversity.

Dunayevskiy YM, Vouros P, Wintner EA, Shipps GW, Carell T, Rebek J Jr.

Proc Natl Acad Sci U S A. 1996 Jun 11;93(12):6152-7.

38.

Solution-phase generation of tetraurea libraries.

Shipps GW Jr, Spitz UP, Rebek J Jr.

Bioorg Med Chem. 1996 May;4(5):655-7.

PMID:
8804529
39.

Human bubonic plague transmitted by a domestic cat scratch.

Weniger BG, Warren AJ, Forseth V, Shipps GW, Creelman T, Gorton J, Barnes AM.

JAMA. 1984 Feb 17;251(7):927-8.

PMID:
6694293

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