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Items: 23


The KRASG12C Inhibitor, MRTX849, Provides Insight Toward Therapeutic Susceptibility of KRAS Mutant Cancers in Mouse Models and Patients.

Hallin J, Engstrom LD, Hargis L, Calinisan A, Aranda R, Briere DM, Sudhakar N, Bowcut V, Baer BR, Ballard JA, Burkard MR, Fell JB, Fischer JP, Vigers GP, Xue JY, Gatto S, Fernandez-Banet J, Pavlicek A, Velastegui K, Chao RC, Barton J, Pierobon M, Baldelli E, Patricoin EF, Cassidy DP, Marx MA, Rybkin II, Johnson ML, Ou SI, Lito P, Papadopoulos KP, Janne PA, Olson P, Christensen JG.

Cancer Discov. 2019 Oct 28. pii: CD-19-1167. doi: 10.1158/2159-8290.CD-19-1167. [Epub ahead of print]


Activation loop dynamics are controlled by conformation-selective inhibitors of ERK2.

Pegram LM, Liddle JC, Xiao Y, Hoh M, Rudolph J, Iverson DB, Vigers GP, Smith D, Zhang H, Wang W, Moffat JG, Ahn NG.

Proc Natl Acad Sci U S A. 2019 Jul 30;116(31):15463-15468. doi: 10.1073/pnas.1906824116. Epub 2019 Jul 16.


Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity.

Fell JB, Fischer JP, Baer BR, Ballard J, Blake JF, Bouhana K, Brandhuber BJ, Briere DM, Burgess LE, Burkard MR, Chiang H, Chicarelli MJ, Davidson K, Gaudino JJ, Hallin J, Hanson L, Hee K, Hicken EJ, Hinklin RJ, Marx MA, Mejia MJ, Olson P, Savechenkov P, Sudhakar N, Tang TP, Vigers GP, Zecca H, Christensen JG.

ACS Med Chem Lett. 2018 Nov 7;9(12):1230-1234. doi: 10.1021/acsmedchemlett.8b00382. eCollection 2018 Dec 13.


Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors.

Volgraf M, Chan L, Huestis MP, Purkey HE, Burkard M, Geck Do M, Harris J, Hunt KW, Liu X, Lyssikatos JP, Rana S, Thomas AA, Vigers GP, Siu M.

Bioorg Med Chem Lett. 2014 Jun 1;24(11):2477-80. doi: 10.1016/j.bmcl.2014.04.012. Epub 2014 Apr 13.


Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.

Blake JF, Xu R, Bencsik JR, Xiao D, Kallan NC, Schlachter S, Mitchell IS, Spencer KL, Banka AL, Wallace EM, Gloor SL, Martinson M, Woessner RD, Vigers GP, Brandhuber BJ, Liang J, Safina BS, Li J, Zhang B, Chabot C, Do S, Lee L, Oeh J, Sampath D, Lee BB, Lin K, Liederer BM, Skelton NJ.

J Med Chem. 2012 Sep 27;55(18):8110-27. Epub 2012 Sep 18.


An ATP-site on-off switch that restricts phosphatase accessibility of Akt.

Lin K, Lin J, Wu WI, Ballard J, Lee BB, Gloor SL, Vigers GP, Morales TH, Friedman LS, Skelton N, Brandhuber BJ.

Sci Signal. 2012 May 8;5(223):ra37. doi: 10.1126/scisignal.2002618.


Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA.

Xu R, Banka A, Blake JF, Mitchell IS, Wallace EM, Bencsik JR, Kallan NC, Spencer KL, Gloor SL, Martinson M, Risom T, Gross SD, Morales TH, Wu WI, Vigers GP, Brandhuber BJ, Skelton NJ.

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2335-40. doi: 10.1016/j.bmcl.2011.02.098. Epub 2011 Feb 26.


Discovery and SAR of spirochromane Akt inhibitors.

Kallan NC, Spencer KL, Blake JF, Xu R, Heizer J, Bencsik JR, Mitchell IS, Gloor SL, Martinson M, Risom T, Gross SD, Morales TH, Wu WI, Vigers GP, Brandhuber BJ, Skelton NJ.

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2410-4. doi: 10.1016/j.bmcl.2011.02.073. Epub 2011 Feb 18.


Discovery of dihydrothieno- and dihydrofuropyrimidines as potent pan Akt inhibitors.

Bencsik JR, Xiao D, Blake JF, Kallan NC, Mitchell IS, Spencer KL, Xu R, Gloor SL, Martinson M, Risom T, Woessner RD, Dizon F, Wu WI, Vigers GP, Brandhuber BJ, Skelton NJ, Prior WW, Murray LJ.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):7037-41. doi: 10.1016/j.bmcl.2010.09.112. Epub 2010 Sep 29.


Crystal structure of human AKT1 with an allosteric inhibitor reveals a new mode of kinase inhibition.

Wu WI, Voegtli WC, Sturgis HL, Dizon FP, Vigers GP, Brandhuber BJ.

PLoS One. 2010 Sep 23;5(9):e12913. doi: 10.1371/journal.pone.0012913.


Discovery of pyrrolopyrimidine inhibitors of Akt.

Blake JF, Kallan NC, Xiao D, Xu R, Bencsik JR, Skelton NJ, Spencer KL, Mitchell IS, Woessner RD, Gloor SL, Risom T, Gross SD, Martinson M, Morales TH, Vigers GP, Brandhuber BJ.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5607-12. doi: 10.1016/j.bmcl.2010.08.053. Epub 2010 Aug 13.


Multiple active site corrections for docking and virtual screening.

Vigers GP, Rizzi JP.

J Med Chem. 2004 Jan 1;47(1):80-9.


X-ray crystal structure of a small antagonist peptide bound to interleukin-1 receptor type 1.

Vigers GP, Dripps DJ, Edwards CK 3rd, Brandhuber BJ.

J Biol Chem. 2000 Nov 24;275(47):36927-33.


Potent selective nonpeptidic inhibitors of human lung tryptase.

Burgess LE, Newhouse BJ, Ibrahim P, Rizzi J, Kashem MA, Hartman A, Brandhuber BJ, Wright CD, Thomson DS, Vigers GP, Koch K.

Proc Natl Acad Sci U S A. 1999 Jul 20;96(15):8348-52.


Crystal structure of the type-I interleukin-1 receptor complexed with interleukin-1beta.

Vigers GP, Anderson LJ, Caffes P, Brandhuber BJ.

Nature. 1997 Mar 13;386(6621):190-4.


Mapping receptor binding sites in interleukin (IL)-1 receptor antagonist and IL-1 beta by site-directed mutagenesis. Identification of a single site in IL-1ra and two sites in IL-1 beta.

Evans RJ, Bray J, Childs JD, Vigers GP, Brandhuber BJ, Skalicky JJ, Thompson RC, Eisenberg SP.

J Biol Chem. 1995 May 12;270(19):11477-83.


X-ray structure of interleukin-1 receptor antagonist at 2.0-A resolution.

Vigers GP, Caffes P, Evans RJ, Thompson RC, Eisenberg SP, Brandhuber BJ.

J Biol Chem. 1994 Apr 29;269(17):12874-9.


Regulation of nuclear envelope precursor functions during cell division.

Vigers GP, Lohka MJ.

J Cell Sci. 1992 Jun;102 ( Pt 2):273-84.


Fluorescent microtubules break up under illumination.

Vigers GP, Coue M, McIntosh JR.

J Cell Biol. 1988 Sep;107(3):1011-24.


Characterization of the microtubule movement produced by sea urchin egg kinesin.

Porter ME, Scholey JM, Stemple DL, Vigers GP, Vale RD, Sheetz MP, McIntosh JR.

J Biol Chem. 1987 Feb 25;262(6):2794-802.


Location of the 100 kd-50 kd accessory proteins in clathrin coats.

Vigers GP, Crowther RA, Pearse BM.

EMBO J. 1986 Sep;5(9):2079-85.


Three-dimensional structure of clathrin cages in ice.

Vigers GP, Crowther RA, Pearse BM.

EMBO J. 1986 Mar;5(3):529-34.

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