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Items: 24


RAF inhibitors that evade paradoxical MAPK pathway activation.

Zhang C, Spevak W, Zhang Y, Burton EA, Ma Y, Habets G, Zhang J, Lin J, Ewing T, Matusow B, Tsang G, Marimuthu A, Cho H, Wu G, Wang W, Fong D, Nguyen H, Shi S, Womack P, Nespi M, Shellooe R, Carias H, Powell B, Light E, Sanftner L, Walters J, Tsai J, West BL, Visor G, Rezaei H, Lin PS, Nolop K, Ibrahim PN, Hirth P, Bollag G.

Nature. 2015 Oct 22;526(7574):583-6. doi: 10.1038/nature14982. Epub 2015 Oct 14.


Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor.

Tap WD, Wainberg ZA, Anthony SP, Ibrahim PN, Zhang C, Healey JH, Chmielowski B, Staddon AP, Cohn AL, Shapiro GI, Keedy VL, Singh AS, Puzanov I, Kwak EL, Wagner AJ, Von Hoff DD, Weiss GJ, Ramanathan RK, Zhang J, Habets G, Zhang Y, Burton EA, Visor G, Sanftner L, Severson P, Nguyen H, Kim MJ, Marimuthu A, Tsang G, Shellooe R, Gee C, West BL, Hirth P, Nolop K, van de Rijn M, Hsu HH, Peterfy C, Lin PS, Tong-Starksen S, Bollag G.

N Engl J Med. 2015 Jul 30;373(5):428-37. doi: 10.1056/NEJMoa1411366.


Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor.

Zhang C, Ibrahim PN, Zhang J, Burton EA, Habets G, Zhang Y, Powell B, West BL, Matusow B, Tsang G, Shellooe R, Carias H, Nguyen H, Marimuthu A, Zhang KY, Oh A, Bremer R, Hurt CR, Artis DR, Wu G, Nespi M, Spevak W, Lin P, Nolop K, Hirth P, Tesch GH, Bollag G.

Proc Natl Acad Sci U S A. 2013 Apr 2;110(14):5689-94. doi: 10.1073/pnas.1219457110. Epub 2013 Mar 14.


Vemurafenib: the first drug approved for BRAF-mutant cancer.

Bollag G, Tsai J, Zhang J, Zhang C, Ibrahim P, Nolop K, Hirth P.

Nat Rev Drug Discov. 2012 Nov;11(11):873-86. doi: 10.1038/nrd3847. Epub 2012 Oct 12. Review.


The Raf kinase inhibitor PLX5568 slows cyst proliferation in rat polycystic kidney disease but promotes renal and hepatic fibrosis.

Buchholz B, Klanke B, Schley G, Bollag G, Tsai J, Kroening S, Yoshihara D, Wallace DP, Kraenzlin B, Gretz N, Hirth P, Eckardt KU, Bernhardt WM.

Nephrol Dial Transplant. 2011 Nov;26(11):3458-65. doi: 10.1093/ndt/gfr432. Epub 2011 Jul 29.


Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma.

Bollag G, Hirth P, Tsai J, Zhang J, Ibrahim PN, Cho H, Spevak W, Zhang C, Zhang Y, Habets G, Burton EA, Wong B, Tsang G, West BL, Powell B, Shellooe R, Marimuthu A, Nguyen H, Zhang KY, Artis DR, Schlessinger J, Su F, Higgins B, Iyer R, D'Andrea K, Koehler A, Stumm M, Lin PS, Lee RJ, Grippo J, Puzanov I, Kim KB, Ribas A, McArthur GA, Sosman JA, Chapman PB, Flaherty KT, Xu X, Nathanson KL, Nolop K.

Nature. 2010 Sep 30;467(7315):596-9. doi: 10.1038/nature09454.


Pharmacodynamic characterization of the efficacy signals due to selective BRAF inhibition with PLX4032 in malignant melanoma.

Tap WD, Gong KW, Dering J, Tseng Y, Ginther C, Pauletti G, Glaspy JA, Essner R, Bollag G, Hirth P, Zhang C, Slamon DJ.

Neoplasia. 2010 Aug;12(8):637-49.


Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity.

Tsai J, Lee JT, Wang W, Zhang J, Cho H, Mamo S, Bremer R, Gillette S, Kong J, Haass NK, Sproesser K, Li L, Smalley KS, Fong D, Zhu YL, Marimuthu A, Nguyen H, Lam B, Liu J, Cheung I, Rice J, Suzuki Y, Luu C, Settachatgul C, Shellooe R, Cantwell J, Kim SH, Schlessinger J, Zhang KY, West BL, Powell B, Habets G, Zhang C, Ibrahim PN, Hirth P, Artis DR, Herlyn M, Bollag G.

Proc Natl Acad Sci U S A. 2008 Feb 26;105(8):3041-6. doi: 10.1073/pnas.0711741105. Epub 2008 Feb 19.


The science-business tango. Interview by Mari Paul.

Hirth P.

Nat Biotechnol. 2006 Aug;24(8):1035-6. No abstract available.


A bradykinin antagonist and a caspase inhibitor prevent severe pulmonary hypertension in a rat model.

Taraseviciene-Stewart L, Gera L, Hirth P, Voelkel NF, Tuder RM, Stewart JM.

Can J Physiol Pharmacol. 2002 Apr;80(4):269-74.


Inhibition of the VEGF receptor 2 combined with chronic hypoxia causes cell death-dependent pulmonary endothelial cell proliferation and severe pulmonary hypertension.

Taraseviciene-Stewart L, Kasahara Y, Alger L, Hirth P, Mc Mahon G, Waltenberger J, Voelkel NF, Tuder RM.

FASEB J. 2001 Feb;15(2):427-38.


Inhibition of VEGF receptors causes lung cell apoptosis and emphysema.

Kasahara Y, Tuder RM, Taraseviciene-Stewart L, Le Cras TD, Abman S, Hirth PK, Waltenberger J, Voelkel NF.

J Clin Invest. 2000 Dec;106(11):1311-9.


Inhibition of platelet-derived growth factor and epidermal growth factor receptor signaling events after treatment of cells with specific synthetic inhibitors of tyrosine kinase phosphorylation.

Lipson KE, Pang L, Huber LJ, Chen H, Tsai JM, Hirth P, Gazit A, Levitzki A, McMahon G.

J Pharmacol Exp Ther. 1998 May;285(2):844-52.


Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors.

Mohammadi M, McMahon G, Sun L, Tang C, Hirth P, Yeh BK, Hubbard SR, Schlessinger J.

Science. 1997 May 9;276(5314):955-60.


Tyrphostins IV--highly potent inhibitors of EGF receptor kinase. Structure-activity relationship study of 4-anilidoquinazolines.

Gazit A, Chen J, App H, McMahon G, Hirth P, Chen I, Levitzki A.

Bioorg Med Chem. 1996 Aug;4(8):1203-7.


The metabolism of recombinant erythropoietin in the isolated perfused rat liver.

Nielsen OJ, Egfjord M, Hirth P.

Liver. 1990 Dec;10(6):343-9.


Erythropoietin metabolism in the isolated perfused rat liver.

Nielsen OJ, Egfjord M, Hirth P.

Contrib Nephrol. 1989;76:90-5; discussion 95-7. No abstract available.


Evaluation of the stability of human erythropoietin in samples for radioimmunoassay.

Eckardt KU, Kurtz A, Hirth P, Scigalla P, Wieczorek L, Bauer C.

Klin Wochenschr. 1988 Mar 15;66(6):241-5.


Molecular biology of erythropoietin.

Hirth P, Wieczorek L, Scigalla P.

Contrib Nephrol. 1988;66:38-53. No abstract available.


Probing an adhesion mutant of Dictyostelium discoideum with cDNA clones and monoclonal antibodies indicates a specific defect in the contact site A glycoprotein.

Noegel A, Harloff C, Hirth P, Merkl R, Modersitzki M, Stadler J, Weinhart U, Westphal M, Gerisch G.

EMBO J. 1985 Dec 30;4(13B):3805-10.


Early Dictyostelium development: control mechanisms bypassed by sequential mutagenesis.

Gerisch G, Hagmann J, Hirth P, Rossier C, Weinhart U, Westphal M.

Cold Spring Harb Symp Quant Biol. 1985;50:813-22. No abstract available.


Cell-free synthesis of enterotoxin of E. coli from a cloned gene.

Lathe R, Hirth P, DeWilde M, Harford N, Lecocq JP.

Nature. 1980 Apr 3;284(5755):473-4. No abstract available.


Cell free synthesis of bacteriophage lambda replication proteins.

Raab C, Klein A, Kluding H, Hirth P, Fuchs E.

FEBS Lett. 1977 Aug 15;80(2):275-8. No abstract available.

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