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Items: 32

1.

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.

PMID:
30613331
2.

Selective RET kinase inhibition for patients with RET-altered cancers.

Subbiah V, Velcheti V, Tuch BB, Ebata K, Busaidy NL, Cabanillas ME, Wirth LJ, Stock S, Smith S, Lauriault V, Corsi-Travali S, Henry D, Burkard M, Hamor R, Bouhana K, Winski S, Wallace RD, Hartley D, Rhodes S, Reddy M, Brandhuber BJ, Andrews S, Rothenberg SM, Drilon A.

Ann Oncol. 2018 Aug 1;29(8):1869-1876. doi: 10.1093/annonc/mdy137.

3.

A Next-Generation TRK Kinase Inhibitor Overcomes Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK Fusion-Positive Solid Tumors.

Drilon A, Nagasubramanian R, Blake JF, Ku N, Tuch BB, Ebata K, Smith S, Lauriault V, Kolakowski GR, Brandhuber BJ, Larsen PD, Bouhana KS, Winski SL, Hamor R, Wu WI, Parker A, Morales TH, Sullivan FX, DeWolf WE, Wollenberg LA, Gordon PR, Douglas-Lindsay DN, Scaltriti M, Benayed R, Raj S, Hanusch B, Schram AM, Jonsson P, Berger MF, Hechtman JF, Taylor BS, Andrews S, Rothenberg SM, Hyman DM.

Cancer Discov. 2017 Sep;7(9):963-972. doi: 10.1158/2159-8290.CD-17-0507. Epub 2017 Jun 3.

4.

Structure of the BRAF-MEK complex reveals a kinase activity independent role for BRAF in MAPK signaling.

Haling JR, Sudhamsu J, Yen I, Sideris S, Sandoval W, Phung W, Bravo BJ, Giannetti AM, Peck A, Masselot A, Morales T, Smith D, Brandhuber BJ, Hymowitz SG, Malek S.

Cancer Cell. 2014 Sep 8;26(3):402-413. doi: 10.1016/j.ccr.2014.07.007. Epub 2014 Aug 21.

5.

Discovery of danoprevir (ITMN-191/R7227), a highly selective and potent inhibitor of hepatitis C virus (HCV) NS3/4A protease.

Jiang Y, Andrews SW, Condroski KR, Buckman B, Serebryany V, Wenglowsky S, Kennedy AL, Madduru MR, Wang B, Lyon M, Doherty GA, Woodard BT, Lemieux C, Geck Do M, Zhang H, Ballard J, Vigers G, Brandhuber BJ, Stengel P, Josey JA, Beigelman L, Blatt L, Seiwert SD.

J Med Chem. 2014 Mar 13;57(5):1753-69. doi: 10.1021/jm400164c. Epub 2013 May 28.

PMID:
23672640
6.

Disruption of PH-kinase domain interactions leads to oncogenic activation of AKT in human cancers.

Parikh C, Janakiraman V, Wu WI, Foo CK, Kljavin NM, Chaudhuri S, Stawiski E, Lee B, Lin J, Li H, Lorenzo MN, Yuan W, Guillory J, Jackson M, Rondon J, Franke Y, Bowman KK, Sagolla M, Stinson J, Wu TD, Wu J, Stokoe D, Stern HM, Brandhuber BJ, Lin K, Skelton NJ, Seshagiri S.

Proc Natl Acad Sci U S A. 2012 Nov 20;109(47):19368-73. doi: 10.1073/pnas.1204384109. Epub 2012 Nov 7.

7.

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.

PMID:
22934575
8.

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.

9.

Non-oxime pyrazole based inhibitors of B-Raf kinase.

Newhouse BJ, Hansen JD, Grina J, Welch M, Topalov G, Littman N, Callejo M, Martinson M, Galbraith S, Laird ER, Brandhuber BJ, Vigers G, Morales T, Woessner R, Randolph N, Lyssikatos J, Olivero A.

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3488-92. doi: 10.1016/j.bmcl.2010.12.038. Epub 2010 Dec 17.

PMID:
21536432
10.

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.

PMID:
21420856
11.

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.

PMID:
21392984
12.

Non-oxime inhibitors of B-Raf(V600E) kinase.

Ren L, Wenglowsky S, Miknis G, Rast B, Buckmelter AJ, Ely RJ, Schlachter S, Laird ER, Randolph N, Callejo M, Martinson M, Galbraith S, Brandhuber BJ, Vigers G, Morales T, Voegtli WC, Lyssikatos J.

Bioorg Med Chem Lett. 2011 Feb 15;21(4):1243-7. doi: 10.1016/j.bmcl.2010.12.061. Epub 2010 Dec 19.

PMID:
21251822
13.

The discovery of furo[2,3-c]pyridine-based indanone oximes as potent and selective B-Raf inhibitors.

Buckmelter AJ, Ren L, Laird ER, Rast B, Miknis G, Wenglowsky S, Schlachter S, Welch M, Tarlton E, Grina J, Lyssikatos J, Brandhuber BJ, Morales T, Randolph N, Vigers G, Martinson M, Callejo M.

Bioorg Med Chem Lett. 2011 Feb 15;21(4):1248-52. doi: 10.1016/j.bmcl.2010.12.039. Epub 2010 Dec 10.

PMID:
21211972
14.

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.

PMID:
20971641
15.

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.

16.

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.

PMID:
20810279
17.

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth.

Hatzivassiliou G, Song K, Yen I, Brandhuber BJ, Anderson DJ, Alvarado R, Ludlam MJ, Stokoe D, Gloor SL, Vigers G, Morales T, Aliagas I, Liu B, Sideris S, Hoeflich KP, Jaiswal BS, Seshagiri S, Koeppen H, Belvin M, Friedman LS, Malek S.

Nature. 2010 Mar 18;464(7287):431-5. doi: 10.1038/nature08833. Epub 2010 Feb 3.

PMID:
20130576
18.

Inhibition and binding kinetics of the hepatitis C virus NS3 protease inhibitor ITMN-191 reveals tight binding and slow dissociative behavior.

Rajagopalan R, Misialek S, Stevens SK, Myszka DG, Brandhuber BJ, Ballard JA, Andrews SW, Seiwert SD, Kossen K.

Biochemistry. 2009 Mar 24;48(11):2559-68. doi: 10.1021/bi900038p.

PMID:
19209850
19.

Potent and selective pyrazole-based inhibitors of B-Raf kinase.

Hansen JD, Grina J, Newhouse B, Welch M, Topalov G, Littman N, Callejo M, Gloor S, Martinson M, Laird E, Brandhuber BJ, Vigers G, Morales T, Woessner R, Randolph N, Lyssikatos J, Olivero A.

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4692-5. doi: 10.1016/j.bmcl.2008.07.002. Epub 2008 Jul 5.

PMID:
18676143
20.

Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor.

Yeh TC, Marsh V, Bernat BA, Ballard J, Colwell H, Evans RJ, Parry J, Smith D, Brandhuber BJ, Gross S, Marlow A, Hurley B, Lyssikatos J, Lee PA, Winkler JD, Koch K, Wallace E.

Clin Cancer Res. 2007 Mar 1;13(5):1576-83.

21.

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.

22.

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.

23.

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.

PMID:
9062193
24.

Seeing double: crystal structures of the type I TNF receptor.

Naismith JH, Brandhuber BJ, Devine TQ, Sprang SR.

J Mol Recognit. 1996 Mar-Apr;9(2):113-7.

PMID:
8877801
25.

Crystallographic evidence for dimerization of unliganded tumor necrosis factor receptor.

Naismith JH, Devine TQ, Brandhuber BJ, Sprang SR.

J Biol Chem. 1995 Jun 2;270(22):13303-7.

26.

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.

27.

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.

28.

Interleukin 1 receptor antagonist is a member of the interleukin 1 gene family: evolution of a cytokine control mechanism.

Eisenberg SP, Brewer MT, Verderber E, Heimdal P, Brandhuber BJ, Thompson RC.

Proc Natl Acad Sci U S A. 1991 Jun 15;88(12):5232-6.

29.

Interleukin-1 (IL-1) receptor antagonist binds to the 80-kDa IL-1 receptor but does not initiate IL-1 signal transduction.

Dripps DJ, Brandhuber BJ, Thompson RC, Eisenberg SP.

J Biol Chem. 1991 Jun 5;266(16):10331-6.

30.

Mapping the enzymatic active site of Pseudomonas aeruginosa exotoxin A.

Brandhuber BJ, Allured VS, Falbel TG, McKay DB.

Proteins. 1988;3(3):146-54.

PMID:
3151219
31.

Three-dimensional structure of interleukin-2.

Brandhuber BJ, Boone T, Kenney WC, McKay DB.

Science. 1987 Dec 18;238(4834):1707-9.

PMID:
3500515
32.

Crystals and a low resolution structure of interleukin-2.

Brandhuber BJ, Boone T, Kenney WC, McKay DB.

J Biol Chem. 1987 Sep 5;262(25):12306-8.

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