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Items: 1 to 50 of 52

1.

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
2.

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
3.

Identification of novel rapamycin derivatives as low-level impurities in active pharmaceutical ingredients.

Zech SG, Carr M, Mohemmad QK, Narasimhan NI, Murray C, Rozamus LW, Dalgarno DC.

J Antibiot (Tokyo). 2011 Sep;64(9):649-54. doi: 10.1038/ja.2011.61. Epub 2011 Jul 27.

PMID:
21792211
4.

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
5.

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
6.

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
7.

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
8.

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.

9.

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
10.

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.

11.

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.

12.

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
13.

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
14.

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.

15.

Differences in F36VMpl-based in vivo selection among large animal models.

Richard RE, De Claro RA, Yan J, Chien S, Von Recum H, Morris J, Kiem HP, Dalgarno DC, Heimfeld S, Clackson T, Andrews R, Blau CA.

Mol Ther. 2004 Oct;10(4):730-40.

16.

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
17.

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
18.

Pharmacologically regulated Fas-mediated death of adoptively transferred T cells in a nonhuman primate model.

Berger C, Blau CA, Huang ML, Iuliucci JD, Dalgarno DC, Gaschet J, Heimfeld S, Clackson T, Riddell SR.

Blood. 2004 Feb 15;103(4):1261-9. Epub 2003 Oct 16.

PMID:
14563634
19.

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
20.

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
21.

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
22.

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
23.

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
24.

Targeting protein kinases for bone disease: discovery and development of Src inhibitors.

Metcalf CA 3rd, van Schravendijk MR, Dalgarno DC, Sawyer TK.

Curr Pharm Des. 2002;8(23):2049-75. Review.

PMID:
12171518
25.

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
26.

Selective inhibition of Src SH2 by a novel thiol-targeting tricarbonyl-modified inhibitor and mechanistic analysis by (1)H/(13)C NMR spectroscopy.

Sundaramoorthi R, Siedem C, Vu CB, Dalgarno DC, Laird EC, Botfield MC, Combs AB, Adams SE, Yuan RW, Weigele M, Narula SS.

Bioorg Med Chem Lett. 2001 Jul 9;11(13):1665-9.

PMID:
11425533
27.

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
28.

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
29.

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
30.

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
31.

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
32.

Structure-based design and synthesis of a novel class of Src SH2 inhibitors.

Buchanan JL, Bohacek RS, Luke GP, Hatada M, Lu X, Dalgarno DC, Narula SS, Yuan R, Holt DA.

Bioorg Med Chem Lett. 1999 Aug 16;9(16):2353-8.

PMID:
10476868
33.

SH3 domains and drug design: ligands, structure, and biological function.

Dalgarno DC, Botfield MC, Rickles RJ.

Biopolymers. 1997;43(5):383-400. Review.

PMID:
9566119
34.

Structural basis for the binding of proline-rich peptides to SH3 domains.

Yu H, Chen JK, Feng S, Dalgarno DC, Brauer AW, Schreiber SL.

Cell. 1994 Mar 11;76(5):933-45.

PMID:
7510218
35.

1H and 15N assignments and secondary structure of the PI3K SH3 domain.

Koyama S, Yu H, Dalgarno DC, Shin TB, Zydowsky LD, Schreiber SL.

FEBS Lett. 1993 Jun 7;324(1):93-8.

36.

Structure of the PI3K SH3 domain and analysis of the SH3 family.

Koyama S, Yu H, Dalgarno DC, Shin TB, Zydowsky LD, Schreiber SL.

Cell. 1993 Mar 26;72(6):945-52.

PMID:
7681364
37.

Solution conformation of endothelin and point mutants by nuclear magnetic resonance spectroscopy.

Dalgarno DC, Slater L, Chackalamannil S, Senior MM.

Int J Pept Protein Res. 1992 Dec;40(6):515-23.

PMID:
1286935
38.

NMR analysis of the structure and metal sequestering properties of metallothioneins.

Armitage IM, Dalgarno DC, Johnson BA.

Experientia Suppl. 1987;52:159-69.

PMID:
2959502
39.

1H NMR studies on bovine cyclophilin: preliminary structural characterization of this specific cyclosporin A binding protein.

Dalgarno DC, Harding MW, Lazarides A, Handschumacher RE, Armitage IM.

Biochemistry. 1986 Nov 4;25(22):6778-84.

PMID:
3542017
40.

Characterization of the actin-binding site on the alkali light chain of myosin.

Henry GD, Winstanley MA, Dalgarno DC, Scott GM, Levine BA, Trayer IP.

Biochim Biophys Acta. 1985 Aug 23;830(3):233-43.

PMID:
4027251
41.

Solution conformation of the C-terminal domain of skeletal troponin C. Cation, trifluoperazine and troponin I binding effects.

Drabikowski W, Dalgarno DC, Levine BA, Gergely J, Grabarek Z, Leavis PC.

Eur J Biochem. 1985 Aug 15;151(1):17-28.

42.

The nature of the trifluoperazine binding sites on calmodulin and troponin-C.

Dalgarno DC, Klevit RE, Levine BA, Scott GM, Williams RJ, Gergely J, Grabarek Z, Leavis PC, Grand RJ, Drabikowski W.

Biochim Biophys Acta. 1984 Dec 7;791(2):164-72.

PMID:
6509062
43.

1H-NMR studies of calmodulin. The nature of the Ca2+-dependent conformational change.

Klevit RE, Dalgarno DC, Levine BA, Williams RJ.

Eur J Biochem. 1984 Feb 15;139(1):109-14.

44.

1H NMR studies of calmodulin. Resonance assignments by use of tryptic fragments.

Dalgarno DC, Klevit RE, Levine BA, Williams RJ, Dobrowolski Z, Drabikowski W.

Eur J Biochem. 1984 Jan 16;138(2):281-9.

45.

Elucidation of the structure and metal sequestering properties of metallothionein by nuclear magnetic resonance.

Dalgarno DC, Armitage IM.

Adv Inorg Biochem. 1984;6:113-38. Review. No abstract available.

PMID:
6398962
46.

Proton-NMR studies of the solution conformations of vitamin-D-induced bovine intestinal calcium-binding protein.

Dalgarno DC, Levine BA, Williams RJ, Fullmer CS, Wasserman RH.

Eur J Biochem. 1983 Dec 15;137(3):523-9.

47.

The dynamics and function of calcium-binding proteins.

Levine BA, Dalgarno DC.

Biochim Biophys Acta. 1983 Sep 15;726(3):187-204. Review. No abstract available.

PMID:
6351918
48.

Structural information from NMR secondary chemical shifts of peptide alpha C-H protons in proteins.

Dalgarno DC, Levine BA, Williams RJ.

Biosci Rep. 1983 May;3(5):443-52.

PMID:
6882888
49.

The mobility of calcium-trigger proteins and its function.

Levine BA, Dalgarno DC, Esnouf MP, Klevit RE, Scott GM, Williams RJ.

Ciba Found Symp. 1983;93:72-97.

PMID:
6551233
50.

Identification of a surface actin-binding site on myosin.

Dalgarno DC, Prince HP, Levine BA, Trayer IP.

Biochim Biophys Acta. 1982 Sep 22;707(1):81-8.

PMID:
7138881

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