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Items: 45

1.

The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models.

Zhang S, Anjum R, Squillace R, Nadworny S, Zhou T, Keats J, Ning Y, Wardwell SD, Miller D, Song Y, Eichinger L, Moran L, Huang WS, Liu S, Zou D, Wang Y, Mohemmad Q, Jang HG, Ye E, Narasimhan N, Wang F, Miret J, Zhu X, Clackson T, Dalgarno D, Shakespeare WC, Rivera VM.

Clin Cancer Res. 2016 Nov 15;22(22):5527-5538. doi: 10.1158/1078-0432.CCR-16-0569. Epub 2016 Oct 25.

2.

Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.

Huang WS, Liu S, Zou D, Thomas M, Wang Y, Zhou T, Romero J, Kohlmann A, Li F, Qi J, Cai L, Dwight TA, Xu Y, Xu R, Dodd R, Toms A, Parillon L, Lu X, Anjum R, Zhang S, Wang F, Keats J, Wardwell SD, Ning Y, Xu Q, Moran LE, Mohemmad QK, Jang HG, Clackson T, Narasimhan NI, Rivera VM, Zhu X, Dalgarno D, Shakespeare WC.

J Med Chem. 2016 May 26;59(10):4948-64. doi: 10.1021/acs.jmedchem.6b00306. Epub 2016 May 12.

PMID:
27144831
3.

Novel Small Molecule Inhibitors of Choline Kinase Identified by Fragment-Based Drug Discovery.

Zech SG, Kohlmann A, Zhou T, Li F, Squillace RM, Parillon LE, Greenfield MT, Miller DP, Qi J, Thomas RM, Wang Y, Xu Y, Miret JJ, Shakespeare WC, Zhu X, Dalgarno DC.

J Med Chem. 2016 Jan 28;59(2):671-86. doi: 10.1021/acs.jmedchem.5b01552. Epub 2016 Jan 13.

PMID:
26700752
4.

Fragment growing and linking lead to novel nanomolar lactate dehydrogenase inhibitors.

Kohlmann A, Zech SG, Li F, Zhou T, Squillace RM, Commodore L, Greenfield MT, Lu X, Miller DP, Huang WS, Qi J, Thomas RM, Wang Y, Zhang S, Dodd R, Liu S, Xu R, Xu Y, Miret JJ, Rivera V, Clackson T, Shakespeare WC, Zhu X, Dalgarno DC.

J Med Chem. 2013 Feb 14;56(3):1023-40. doi: 10.1021/jm3014844. Epub 2013 Jan 9.

PMID:
23302067
5.

Ponatinib (AP24534), a multitargeted pan-FGFR inhibitor with activity in multiple FGFR-amplified or mutated cancer models.

Gozgit JM, Wong MJ, Moran L, Wardwell S, Mohemmad QK, Narasimhan NI, Shakespeare WC, Wang F, Clackson T, Rivera VM.

Mol Cancer Ther. 2012 Mar;11(3):690-9. doi: 10.1158/1535-7163.MCT-11-0450. Epub 2012 Jan 11.

6.

Crizotinib-resistant mutants of EML4-ALK identified through an accelerated mutagenesis screen.

Zhang S, Wang F, Keats J, Zhu X, Ning Y, Wardwell SD, Moran L, Mohemmad QK, Anjum R, Wang Y, Narasimhan NI, Dalgarno D, Shakespeare WC, Miret JJ, Clackson T, Rivera VM.

Chem Biol Drug Des. 2011 Dec;78(6):999-1005. doi: 10.1111/j.1747-0285.2011.01239.x. Epub 2011 Oct 31.

7.

Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.

Thomas M, Huang WS, Wen D, Zhu X, Wang Y, Metcalf CA, Liu S, Chen I, Romero J, Zou D, Sundaramoorthi R, Li F, Qi J, Cai L, Zhou T, Commodore L, Xu Q, Keats J, Wang F, Wardwell S, Ning Y, Snodgrass JT, Broudy MI, Russian K, Iuliucci J, Rivera VM, Sawyer TK, Dalgarno DC, Clackson T, Shakespeare WC.

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3743-8. doi: 10.1016/j.bmcl.2011.04.060. Epub 2011 Apr 22.

PMID:
21561767
8.

Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK.

Katayama R, Khan TM, Benes C, Lifshits E, Ebi H, Rivera VM, Shakespeare WC, Iafrate AJ, Engelman JA, Shaw AT.

Proc Natl Acad Sci U S A. 2011 May 3;108(18):7535-40. doi: 10.1073/pnas.1019559108. Epub 2011 Apr 18.

9.

Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies.

Gozgit JM, Wong MJ, Wardwell S, Tyner JW, Loriaux MM, Mohemmad QK, Narasimhan NI, Shakespeare WC, Wang F, Druker BJ, Clackson T, Rivera VM.

Mol Cancer Ther. 2011 Jun;10(6):1028-35. doi: 10.1158/1535-7163.MCT-10-1044. Epub 2011 Apr 11.

10.

Structural mechanism of the Pan-BCR-ABL inhibitor ponatinib (AP24534): lessons for overcoming kinase inhibitor resistance.

Zhou T, Commodore L, Huang WS, Wang Y, Thomas M, Keats J, Xu Q, Rivera VM, Shakespeare WC, Clackson T, Dalgarno DC, Zhu X.

Chem Biol Drug Des. 2011 Jan;77(1):1-11. doi: 10.1111/j.1747-0285.2010.01054.x. Epub 2010 Nov 30.

PMID:
21118377
11.

Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant.

Huang WS, Metcalf CA, Sundaramoorthi R, Wang Y, Zou D, Thomas RM, Zhu X, Cai L, Wen D, Liu S, Romero J, Qi J, Chen I, Banda G, Lentini SP, Das S, Xu Q, Keats J, Wang F, Wardwell S, Ning Y, Snodgrass JT, Broudy MI, Russian K, Zhou T, Commodore L, Narasimhan NI, Mohemmad QK, Iuliucci J, Rivera VM, Dalgarno DC, Sawyer TK, Clackson T, Shakespeare WC.

J Med Chem. 2010 Jun 24;53(12):4701-19. doi: 10.1021/jm100395q.

PMID:
20513156
12.

AP24163 inhibits the gatekeeper mutant of BCR-ABL and suppresses in vitro resistance.

Azam M, Powers JT, Einhorn W, Huang WS, Shakespeare WC, Zhu X, Dalgarno D, Clackson T, Sawyer TK, Daley GQ.

Chem Biol Drug Des. 2010 Feb;75(2):223-7. doi: 10.1111/j.1747-0285.2009.00911.x. Epub 2009 Dec 17.

PMID:
20028401
13.

Structural analysis of DFG-in and DFG-out dual Src-Abl inhibitors sharing a common vinyl purine template.

Zhou T, Commodore L, Huang WS, Wang Y, Sawyer TK, Shakespeare WC, Clackson T, Zhu X, Dalgarno DC.

Chem Biol Drug Des. 2010 Jan;75(1):18-28. doi: 10.1111/j.1747-0285.2009.00905.x. Epub 2009 Nov 5.

PMID:
19895503
14.

AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance.

O'Hare T, Shakespeare WC, Zhu X, Eide CA, Rivera VM, Wang F, Adrian LT, Zhou T, Huang WS, Xu Q, Metcalf CA 3rd, Tyner JW, Loriaux MM, Corbin AS, Wardwell S, Ning Y, Keats JA, Wang Y, Sundaramoorthi R, Thomas M, Zhou D, Snodgrass J, Commodore L, Sawyer TK, Dalgarno DC, Deininger MW, Druker BJ, Clackson T.

Cancer Cell. 2009 Nov 6;16(5):401-12. doi: 10.1016/j.ccr.2009.09.028.

15.

9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation.

Huang WS, Zhu X, Wang Y, Azam M, Wen D, Sundaramoorthi R, Thomas RM, Liu S, Banda G, Lentini SP, Das S, Xu Q, Keats J, Wang F, Wardwell S, Ning Y, Snodgrass JT, Broudy MI, Russian K, Daley GQ, Iuliucci J, Dalgarno DC, Clackson T, Sawyer TK, Shakespeare WC.

J Med Chem. 2009 Aug 13;52(15):4743-56. doi: 10.1021/jm900166t.

PMID:
19572547
16.

Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors.

Wang Y, Shakespeare WC, Huang WS, Sundaramoorthi R, Lentini S, Das S, Liu S, Banda G, Wen D, Zhu X, Xu Q, Keats J, Wang F, Wardwell S, Ning Y, Snodgrass JT, Broudy MI, Russian K, Dalgarno D, Clackson T, Sawyer TK.

Bioorg Med Chem Lett. 2008 Sep 1;18(17):4907-12. doi: 10.1016/j.bmcl.2008.06.042. Epub 2008 Jun 18.

PMID:
18691885
17.

SAR of carbon-linked, 2-substituted purines: synthesis and characterization of AP23451 as a novel bone-targeted inhibitor of Src tyrosine kinase with in vivo anti-resorptive activity.

Shakespeare WC, Wang Y, Bohacek R, Keenan T, Sundaramoorthi R, Metcalf C 3rd, Dilauro A, Roeloffzen S, Liu S, Saltmarsh J, Paramanathan G, Dalgarno D, Narula S, Pradeepan S, van Schravendijk MR, Keats J, Ram M, Liou S, Adams S, Wardwell S, Bogus J, Iuliucci J, Weigele M, Xing L, Boyce B, Sawyer TK.

Chem Biol Drug Des. 2008 Feb;71(2):97-105. doi: 10.1111/j.1747-0285.2007.00615.x. Epub 2008 Jan 3.

PMID:
18179464
18.

SRC inhibitors in metastatic bone disease.

Boyce BF, Xing L, Yao Z, Yamashita T, Shakespeare WC, Wang Y, Metcalf CA 3rd, Sundaramoorthi R, Dalgarno DC, Iuliucci JD, Sawyer TK.

Clin Cancer Res. 2006 Oct 15;12(20 Pt 2):6291s-6295s. Review.

19.

Antiangiogenic and antitumor effects of SRC inhibition in ovarian carcinoma.

Han LY, Landen CN, Trevino JG, Halder J, Lin YG, Kamat AA, Kim TJ, Merritt WM, Coleman RL, Gershenson DM, Shakespeare WC, Wang Y, Sundaramoorth R, Metcalf CA 3rd, Dalgarno DC, Sawyer TK, Gallick GE, Sood AK.

Cancer Res. 2006 Sep 1;66(17):8633-9.

20.

Src activation of Stat3 is an independent requirement from NF-kappaB activation for constitutive IL-8 expression in human pancreatic adenocarcinoma cells.

Trevino JG, Gray MJ, Nawrocki ST, Summy JM, Lesslie DP, Evans DB, Sawyer TK, Shakespeare WC, Watowich SS, Chiao PJ, McConkey DJ, Gallick GE.

Angiogenesis. 2006;9(2):101-10. Epub 2006 Jul 27.

PMID:
16871430
21.

Future anti-catabolic therapeutic targets in bone disease.

Boyce BF, Xing L, Yao Z, Shakespeare WC, Wang Y, Metcalf CA 3rd, Sundaramoorthi R, Dalgarno DC, Iuliucci JD, Sawyer TK.

Ann N Y Acad Sci. 2006 Apr;1068:447-57. Review.

PMID:
16831942
22.

Protein phosphorylation and signal transduction modulation: chemistry perspectives for small-molecule drug discovery.

Sawyer TK, Shakespeare WC, Wang Y, Sundaramoorthi R, Huang WS, Metcalf CA 3rd, Thomas M, Lawrence BM, Rozamus L, Noehre J, Zhu X, Narula S, Bohacek RS, Weigele M, Dalgarno DC.

Med Chem. 2005 May;1(3):293-319. Review.

PMID:
16787325
23.

Activity of dual SRC-ABL inhibitors highlights the role of BCR/ABL kinase dynamics in drug resistance.

Azam M, Nardi V, Shakespeare WC, Metcalf CA 3rd, Bohacek RS, Wang Y, Sundaramoorthi R, Sliz P, Veach DR, Bornmann WG, Clarkson B, Dalgarno DC, Sawyer TK, Daley GQ.

Proc Natl Acad Sci U S A. 2006 Jun 13;103(24):9244-9. Epub 2006 Jun 5.

24.

Vascular endothelial growth factor receptor-1 mediates migration of human colorectal carcinoma cells by activation of Src family kinases.

Lesslie DP, Summy JM, Parikh NU, Fan F, Trevino JG, Sawyer TK, Metcalf CA, Shakespeare WC, Hicklin DJ, Ellis LM, Gallick GE.

Br J Cancer. 2006 Jun 5;94(11):1710-7.

25.

AP23846, a novel and highly potent Src family kinase inhibitor, reduces vascular endothelial growth factor and interleukin-8 expression in human solid tumor cell lines and abrogates downstream angiogenic processes.

Summy JM, Trevino JG, Lesslie DP, Baker CH, Shakespeare WC, Wang Y, Sundaramoorthi R, Metcalf CA 3rd, Keats JA, Sawyer TK, Gallick GE.

Mol Cancer Ther. 2005 Dec;4(12):1900-11.

26.

In vitro and in vivo activity of ATP-based kinase inhibitors AP23464 and AP23848 against activation-loop mutants of Kit.

Corbin AS, Demehri S, Griswold IJ, Wang Y, Metcalf CA 3rd, Sundaramoorthi R, Shakespeare WC, Snodgrass J, Wardwell S, Dalgarno D, Iuliucci J, Sawyer TK, Heinrich MC, Druker BJ, Deininger MW.

Blood. 2005 Jul 1;106(1):227-34. Epub 2005 Mar 3.

PMID:
15746079
27.

Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML.

O'Hare T, Pollock R, Stoffregen EP, Keats JA, Abdullah OM, Moseson EM, Rivera VM, Tang H, Metcalf CA 3rd, Bohacek RS, Wang Y, Sundaramoorthi R, Shakespeare WC, Dalgarno D, Clackson T, Sawyer TK, Deininger MW, Druker BJ.

Blood. 2004 Oct 15;104(8):2532-9. Epub 2004 Jul 15.

PMID:
15256422
28.

Structure-based design of novel nonpeptide inhibitors of the Src SH2 domain:phosphotyrosine mimetics exploiting multifunctional group replacement chemistry.

Sundaramoorthi R, Kawahata N, Yang MG, Shakespeare WC, Metcalf CA 3rd, Wang Y, Merry T, Eyermann CJ, Bohacek RS, Narula S, Dalgarno DC, Sawyer TK.

Biopolymers. 2003;71(6):717-29.

PMID:
14991680
29.

Novel bone-targeted Src tyrosine kinase inhibitor drug discovery.

Shakespeare WC, Metcalf CA 3rd, Wang Y, Sundaramoorthi R, Keenan T, Weigele M, Bohacek RS, Dalgarno DC, Sawyer TK.

Curr Opin Drug Discov Devel. 2003 Sep;6(5):729-41. Review.

PMID:
14579523
30.

Bone-targeted pyrido[2,3-d]pyrimidin-7-ones: potent inhibitors of Src tyrosine kinase as novel antiresorptive agents.

Vu CB, Luke GP, Kawahata N, Shakespeare WC, Wang Y, Sundaramoorthi R, Metcalf CA 3rd, Keenan TP, Pradeepan S, Corpuz E, Merry T, Bohacek RS, Dalgarno DC, Narula SS, van Schravendijk MR, Ram MK, Adams S, Liou S, Keats JA, Violette SM, Guan W, Weigele M, Sawyer TK.

Bioorg Med Chem Lett. 2003 Sep 15;13(18):3071-4.

PMID:
12941336
31.

Bone-targeted 2,6,9-trisubstituted purines: novel inhibitors of Src tyrosine kinase for the treatment of bone diseases.

Wang Y, Metcalf CA 3rd, Shakespeare WC, Sundaramoorthi R, Keenan TP, Bohacek RS, van Schravendijk MR, Violette SM, Narula SS, Dalgarno DC, Haraldson C, Keats J, Liou S, Mani U, Pradeepan S, Ram M, Adams S, Weigele M, Sawyer TK.

Bioorg Med Chem Lett. 2003 Sep 15;13(18):3067-70.

PMID:
12941335
32.

Bone-targeted Src kinase inhibitors: novel pyrrolo- and pyrazolopyrimidine analogues.

Sundaramoorthi R, Shakespeare WC, Keenan TP, Metcalf CA 3rd, Wang Y, Mani U, Taylor M, Liu S, Bohacek RS, Narula SS, Dalgarno DC, van Schravandijk MR, Violette SM, Liou S, Adams S, Ram MK, Keats JA, Weigle M, Sawyer TK, Weigele M.

Bioorg Med Chem Lett. 2003 Sep 15;13(18):3063-6. Erratum in: Bioorg Med Chem Lett. 2003 Dec 15;13(24):4519.

PMID:
12941334
33.

Novel protein kinase inhibitors: SMART drug design technology.

Sawyer TK, Bohacek RS, Metcalf CA 3rd, Shakespeare WC, Wang Y, Sundaramoorthi R, Keenan T, Narula S, Weigele M, Dalgarno DC.

Biotechniques. 2003 Jun;Suppl:2-10, 12-5. Review. No abstract available.

PMID:
12813899
34.

SRC homology-2 inhibitors: peptidomimetic and nonpeptide.

Sawyer TK, Bohacek RS, Dalgarno DC, Eyermann CJ, Kawahata N, Metcalf CA 3rd, Shakespeare WC, Sundaramoorthi R, Wang Y, Yang MG.

Mini Rev Med Chem. 2002 Oct;2(5):475-88. Review.

PMID:
12370048
35.

A novel phosphotyrosine mimetic 4'-carboxymethyloxy-3'-phosphonophenylalanine (Cpp): exploitation in the design of nonpeptide inhibitors of pp60(Src) SH2 domain.

Kawahata N, Yang MG, Luke GP, Shakespeare WC, Sundaramoorthi R, Wang Y, Johnson D, Merry T, Violette S, Guan W, Bartlett C, Smith J, Hatada M, Lu X, Dalgarno DC, Eyermann CJ, Bohacek RS, Sawyer TK.

Bioorg Med Chem Lett. 2001 Sep 3;11(17):2319-23.

PMID:
11527723
36.

SH2 domain inhibition: a problem solved?

Shakespeare WC.

Curr Opin Chem Biol. 2001 Aug;5(4):409-15. Review.

PMID:
11470604
37.

X-Ray structure of citrate bound to Src SH2 leads to a high-affinity, bone-targeted Src SH2 inhibitor.

Bohacek RS, Dalgarno DC, Hatada M, Jacobsen VA, Lynch BA, Macek KJ, Merry T, Metcalf CA 3rd, Narula SS, Sawyer TK, Shakespeare WC, Violette SM, Weigele M.

J Med Chem. 2001 Mar 1;44(5):660-3. No abstract available.

PMID:
11262076
38.

Bone-targeted Src SH2 inhibitors block Src cellular activity and osteoclast-mediated resorption.

Violette SM, Guan W, Bartlett C, Smith JA, Bardelay C, Antoine E, Rickles RJ, Mandine E, van Schravendijk MR, Adams SE, Lynch BA, Shakespeare WC, Yang M, Jacobsen VA, Takeuchi CS, Macek KJ, Bohacek RS, Dalgarno DC, Weigele M, Lesuisse D, Sawyer TK, Baron R.

Bone. 2001 Jan;28(1):54-64.

PMID:
11165943
39.

Structure-based design of novel bicyclic nonpeptide inhibitors for the src SH2 domain.

Shakespeare WC, Bohacek RS, Azimioara MD, Macek KJ, Luke GP, Dalgarno DC, Hatada MH, Lu X, Violette SM, Bartlett C, Sawyer TK.

J Med Chem. 2000 Oct 19;43(21):3815-9. No abstract available.

PMID:
11052784
40.

Signal transduction drug discovery: targets, mechanisms and structure-based design.

Dalgarno DC, Metcalf CA Jr, Shakespeare WC, Sawyer TK.

Curr Opin Drug Discov Devel. 2000 Sep;3(5):549-64.

PMID:
19649883
41.

A Src SH2 selective binding compound inhibits osteoclast-mediated resorption.

Violette SM, Shakespeare WC, Bartlett C, Guan W, Smith JA, Rickles RJ, Bohacek RS, Holt DA, Baron R, Sawyer TK.

Chem Biol. 2000 Mar;7(3):225-35.

42.

An efficient synthesis of a 4'-phosphonodifluoromethyl-3'-formyl-phenylalanine containing SRC SH2 ligand.

Shakespeare WC, Bohacek RS, Narula SS, Azimioara MD, Yuan RW, Dalgarno DC, Madden L, Botfield MC, Holt DA.

Bioorg Med Chem Lett. 1999 Nov 1;9(21):3109-12.

PMID:
10560734
43.

A novel mechanism-based mammalian cell assay for the identification of SH2-domain-specific protein-protein inhibitors.

Rickles RJ, Henry PA, Guan W, Azimioara M, Shakespeare WC, Violette S, Zoller MJ.

Chem Biol. 1998 Oct;5(10):529-38.

44.

Modulation of receptor and receptor subtype affinities using diastereomeric and enantiomeric monosaccharide scaffolds as a means to structural and biological diversity. A new route to ether synthesis.

Hirschmann R, Hynes J Jr, Cichy-Knight MA, van Rijn RD, Sprengeler PA, Spoors PG, Shakespeare WC, Pietranico-Cole S, Barbosa J, Liu J, Yao W, Rohrer S, Smith AB 3rd.

J Med Chem. 1998 Apr 23;41(9):1382-91.

PMID:
9554871
45.

ARL 17477, a potent and selective neuronal NOS inhibitor decreases infarct volume after transient middle cerebral artery occlusion in rats.

Zhang ZG, Reif D, Macdonald J, Tang WX, Kamp DK, Gentile RJ, Shakespeare WC, Murray RJ, Chopp M.

J Cereb Blood Flow Metab. 1996 Jul;16(4):599-604.

PMID:
8964798

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