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Discovery of a novel mode of protein kinase inhibition characterized by the mechanism of inhibition of human mesenchymal-epithelial transition factor (c-Met) protein autophosphorylation by ARQ 197.

Eathiraj S, Palma R, Volckova E, Hirschi M, France DS, Ashwell MA, Chan TC.

J Biol Chem. 2011 Jun 10;286(23):20666-76. doi: 10.1074/jbc.M110.213801.


Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.

Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP, Treiber DK.

Chem Biol. 2010 Nov 24;17(11):1241-9. doi: 10.1016/j.chembiol.2010.09.010.


ARQ 197, a novel and selective inhibitor of the human c-Met receptor tyrosine kinase with antitumor activity.

Munshi N, Jeay S, Li Y, Chen CR, France DS, Ashwell MA, Hill J, Moussa MM, Leggett DS, Li CJ.

Mol Cancer Ther. 2010 Jun;9(6):1544-53. doi: 10.1158/1535-7163.MCT-09-1173.


Asymmetric receptor contact is required for tyrosine autophosphorylation of fibroblast growth factor receptor in living cells.

Bae JH, Boggon TJ, Tomé F, Mandiyan V, Lax I, Schlessinger J.

Proc Natl Acad Sci U S A. 2010 Feb 16;107(7):2866-71. doi: 10.1073/pnas.0914157107.


Discovery of novel fibroblast growth factor receptor 1 kinase inhibitors by structure-based virtual screening.

Ravindranathan KP, Mandiyan V, Ekkati AR, Bae JH, Schlessinger J, Jorgensen WL.

J Med Chem. 2010 Feb 25;53(4):1662-72. doi: 10.1021/jm901386e.


Fibroblast growth factor signalling: from development to cancer.

Turner N, Grose R.

Nat Rev Cancer. 2010 Feb;10(2):116-29. doi: 10.1038/nrc2780. Review.


An autoinhibitory tyrosine motif in the cell-cycle-regulated Nek7 kinase is released through binding of Nek9.

Richards MW, O'Regan L, Mas-Droux C, Blot JM, Cheung J, Hoelder S, Fry AM, Bayliss R.

Mol Cell. 2009 Nov 25;36(4):560-70. doi: 10.1016/j.molcel.2009.09.038.


Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT.

Dubreuil P, Letard S, Ciufolini M, Gros L, Humbert M, Castéran N, Borge L, Hajem B, Lermet A, Sippl W, Voisset E, Arock M, Auclair C, Leventhal PS, Mansfield CD, Moussy A, Hermine O.

PLoS One. 2009 Sep 30;4(9):e7258. doi: 10.1371/journal.pone.0007258.


Protein kinase inhibitors: contributions from structure to clinical compounds.

Johnson LN.

Q Rev Biophys. 2009 Feb;42(1):1-40. doi: 10.1017/S0033583508004745. Review.


The precise sequence of FGF receptor autophosphorylation is kinetically driven and is disrupted by oncogenic mutations.

Lew ED, Furdui CM, Anderson KS, Schlessinger J.

Sci Signal. 2009 Feb 17;2(58):ra6. doi: 10.1126/scisignal.2000021.


Structural biology contributions to tyrosine kinase drug discovery.

Cowan-Jacob SW, Möbitz H, Fabbro D.

Curr Opin Cell Biol. 2009 Apr;21(2):280-7. doi: 10.1016/ Review.


KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients.

Gajiwala KS, Wu JC, Christensen J, Deshmukh GD, Diehl W, DiNitto JP, English JM, Greig MJ, He YA, Jacques SL, Lunney EA, McTigue M, Molina D, Quenzer T, Wells PA, Yu X, Zhang Y, Zou A, Emmett MR, Marshall AG, Zhang HM, Demetri GD.

Proc Natl Acad Sci U S A. 2009 Feb 3;106(5):1542-7. doi: 10.1073/pnas.0812413106.


Type-II kinase inhibitor docking, screening, and profiling using modified structures of active kinase states.

Kufareva I, Abagyan R.

J Med Chem. 2008 Dec 25;51(24):7921-32. doi: 10.1021/jm8010299.


'Reverse' alpha-ketoamide-based p38 MAP kinase inhibitors.

Montalban AG, Boman E, Chang CD, Ceide SC, Dahl R, Dalesandro D, Delaet NG, Erb E, Gibbs A, Kahl J, Kessler L, Lundström J, Miller S, Nakanishi H, Roberts E, Saiah E, Sullivan R, Wang Z, Larson CJ.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5456-9. doi: 10.1016/j.bmcl.2008.09.028.


Modulation of kinase-inhibitor interactions by auxiliary protein binding: crystallography studies on Aurora A interactions with VX-680 and with TPX2.

Zhao B, Smallwood A, Yang J, Koretke K, Nurse K, Calamari A, Kirkpatrick RB, Lai Z.

Protein Sci. 2008 Oct;17(10):1791-7. doi: 10.1110/ps.036590.108.


FGFR2-amplified gastric cancer cell lines require FGFR2 and Erbb3 signaling for growth and survival.

Kunii K, Davis L, Gorenstein J, Hatch H, Yashiro M, Di Bacco A, Elbi C, Lutterbach B.

Cancer Res. 2008 Apr 1;68(7):2340-8. doi: 10.1158/0008-5472.CAN-07-5229. Erratum in: Cancer Res. 2008 May 1;68(9):3550.


Allosteric cooperativity in protein kinase A.

Masterson LR, Mascioni A, Traaseth NJ, Taylor SS, Veglia G.

Proc Natl Acad Sci U S A. 2008 Jan 15;105(2):506-11. doi: 10.1073/pnas.0709214104.


Structural basis for reduced FGFR2 activity in LADD syndrome: Implications for FGFR autoinhibition and activation.

Lew ED, Bae JH, Rohmann E, Wollnik B, Schlessinger J.

Proc Natl Acad Sci U S A. 2007 Dec 11;104(50):19802-7.


A molecular brake in the kinase hinge region regulates the activity of receptor tyrosine kinases.

Chen H, Ma J, Li W, Eliseenkova AV, Xu C, Neubert TA, Miller WT, Mohammadi M.

Mol Cell. 2007 Sep 7;27(5):717-30.


A novel platform for accelerated pharmacodynamic profiling for lead optimization of anticancer drug candidates.

Szwaya J, Bruseo C, Nakuci E, McSweeney D, Xiang X, Senator D, France D, Chen CR.

J Biomol Screen. 2007 Mar;12(2):159-66.

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