Klaus P. Hoeflich, Ph.D. - Publications

2001 University of Toronto, Toronto, ON, Canada 
Molecular Biology

50 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2016 Lee W, Crawford JJ, Aliagas I, Murray LJ, Tay S, Wang W, Heise CE, Hoeflich KP, La H, Mathieu S, Mintzer R, Ramaswamy S, Rouge L, Rudolph J. Synthesis and evaluation of a series of 4-azaindole-containing p21-activated kinase-1 inhibitors. Bioorganic & Medicinal Chemistry Letters. PMID 27346791 DOI: 10.1016/j.bmcl.2016.06.031  0.84
2016 Rudolph J, Murray LJ, Ndubaku CO, O'Brien T, Blackwood EM, Wang W, Aliagas I, Gazzard L, Crawford JJ, Drobnick J, Lee W, Zhao X, Hoeflich KP, Favor DA, Dong P, et al. Chemically diverse Group I p21-activated kinase (PAK) inhibitors impart acute cardiovascular toxicity with a narrow therapeutic window. Journal of Medicinal Chemistry. PMID 27167326 DOI: 10.1021/acs.jmedchem.6b00638  0.84
2015 Radu M, Lyle K, Hoeflich KP, Villamar-Cruz O, Koeppen H, Chernoff J. p21-Activated Kinase 2 Regulates Endothelial Development and Function through the Bmk1/Erk5 Pathway. Molecular and Cellular Biology. 35: 3990-4005. PMID 26391956 DOI: 10.1128/MCB.00630-15  0.84
2015 Rudolph J, Aliagas I, Crawford JJ, Mathieu S, Lee W, Chao Q, Dong P, Rouge L, Wang W, Heise C, Murray LJ, La H, Liu Y, Manning G, Diederich F, ... Hoeflich KP, et al. Leveraging the Pre-DFG Residue Thr-406 To Obtain High Kinase Selectivity in an Aminopyrazole-Type PAK1 Inhibitor Series. Acs Medicinal Chemistry Letters. 6: 711-5. PMID 26101579 DOI: 10.1021/acsmedchemlett.5b00151  0.84
2015 Crawford JJ, Lee W, Aliagas I, Mathieu S, Hoeflich KP, Zhou W, Wang W, Rouge L, Murray L, La H, Liu N, Fan PW, Cheong J, Heise CE, Ramaswamy S, et al. Structure-Guided Design of Group I Selective p21-Activated Kinase Inhibitors. Journal of Medicinal Chemistry. 58: 5121-36. PMID 26030457 DOI: 10.1021/acs.jmedchem.5b00572  0.84
2015 Gross S, Rahal R, Stransky N, Lengauer C, Hoeflich KP. Targeting cancer with kinase inhibitors. The Journal of Clinical Investigation. 125: 1780-9. PMID 25932675 DOI: 10.1172/JCI76094  0.84
2015 Ong CC, Gierke S, Pitt C, Sagolla M, Cheng CK, Zhou W, Jubb AM, Strickland L, Schmidt M, Duron SG, Campbell DA, Zheng W, Dehdashti S, Shen M, Yang N, ... ... Hoeflich KP, et al. Small molecule inhibition of group I p21-activated kinases in breast cancer induces apoptosis and potentiates the activity of microtubule stabilizing agents. Breast Cancer Research : Bcr. 17: 59. PMID 25902869 DOI: 10.1186/s13058-015-0564-5  0.84
2015 Chow HY, Dong B, Duron SG, Campbell DA, Ong CC, Hoeflich KP, Chang LS, Welling DB, Yang ZJ, Chernoff J. Group I Paks as therapeutic targets in NF2-deficient meningioma. Oncotarget. 6: 1981-94. PMID 25596744  0.84
2015 Rudolph J, Crawford JJ, Hoeflich KP, Wang W. Inhibitors of p21-activated kinases (PAKs). Journal of Medicinal Chemistry. 58: 111-29. PMID 25415869 DOI: 10.1021/jm501613q  0.84
2015 Junttila MR, Devasthali V, Cheng JH, Castillo J, Metcalfe C, Clermont AC, Otter DD, Chan E, Bou-Reslan H, Cao T, Forrest W, Nannini MA, French D, Carano R, Merchant M, ... Hoeflich KP, et al. Modeling targeted inhibition of MEK and PI3 kinase in human pancreatic cancer. Molecular Cancer Therapeutics. 14: 40-7. PMID 25376606 DOI: 10.1158/1535-7163.MCT-14-0030  0.84
2015 Ndubaku CO, Crawford JJ, Drobnick J, Aliagas I, Campbell D, Dong P, Dornan LM, Duron S, Epler J, Gazzard L, Heise CE, Hoeflich KP, Jakubiak D, La H, Lee W, et al. Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pKa Polar Moiety Acs Medicinal Chemistry Letters. 6: 1241-1246. DOI: 10.1021/acsmedchemlett.5b00398  0.84
2014 Zhou W, Jubb AM, Lyle K, Xiao Q, Ong CC, Desai R, Fu L, Gnad F, Song Q, Haverty PM, Aust D, Grützmann R, Romero M, Totpal K, Neve RM, ... ... Hoeflich KP, et al. PAK1 mediates pancreatic cancer cell migration and resistance to MET inhibition. The Journal of Pathology. 234: 502-13. PMID 25074413 DOI: 10.1002/path.4412  0.84
2014 Staben ST, Feng JA, Lyle K, Belvin M, Boggs J, Burch JD, Chua CC, Cui H, DiPasquale AG, Friedman LS, Heise C, Koeppen H, Kotey A, Mintzer R, Oh A, ... ... Hoeflich KP, et al. Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors. Journal of Medicinal Chemistry. 57: 1033-45. PMID 24432870 DOI: 10.1021/jm401768t  0.84
2013 Rudolph J, Crawford JJ, Hoeflich KP, Chernoff J. p21-activated kinase inhibitors. The Enzymes. 34: 157-80. PMID 25034104 DOI: 10.1016/B978-0-12-420146-0.00007-X  0.84
2013 Kirkpatrick DS, Bustos DJ, Dogan T, Chan J, Phu L, Young A, Friedman LS, Belvin M, Song Q, Bakalarski CE, Hoeflich KP. Phosphoproteomic characterization of DNA damage response in melanoma cells following MEK/PI3K dual inhibition. Proceedings of the National Academy of Sciences of the United States of America. 110: 19426-31. PMID 24218548 DOI: 10.1073/pnas.1309473110  0.84
2013 Hatzivassiliou G, Haling JR, Chen H, Song K, Price S, Heald R, Hewitt JF, Zak M, Peck A, Orr C, Merchant M, Hoeflich KP, Chan J, Luoh SM, Anderson DJ, et al. Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers. Nature. 501: 232-6. PMID 23934108 DOI: 10.1038/nature12441  0.84
2013 Gnad F, Young A, Zhou W, Lyle K, Ong CC, Stokes MP, Silva JC, Belvin M, Friedman LS, Koeppen H, Minden A, Hoeflich KP. Systems-wide analysis of K-Ras, Cdc42, and PAK4 signaling by quantitative phosphoproteomics. Molecular & Cellular Proteomics : McP. 12: 2070-80. PMID 23608596 DOI: 10.1074/mcp.M112.027052  0.84
2013 Arias-Romero LE, Villamar-Cruz O, Huang M, Hoeflich KP, Chernoff J. Pak1 kinase links ErbB2 to β-catenin in transformation of breast epithelial cells. Cancer Research. 73: 3671-82. PMID 23576562 DOI: 10.1158/0008-5472.CAN-12-4453  0.84
2013 Ong CC, Jubb AM, Jakubiak D, Zhou W, Rudolph J, Haverty PM, Kowanetz M, Yan Y, Tremayne J, Lisle R, Harris AL, Friedman LS, Belvin M, Middleton MR, Blackwood EM, ... ... Hoeflich KP, et al. P21-activated kinase 1 (PAK1) as a therapeutic target in BRAF wild-type melanoma. Journal of the National Cancer Institute. 105: 606-7. PMID 23535073 DOI: 10.1093/jnci/djt054  0.84
2012 Liu J, Lee W, Jiang Z, Chen Z, Jhunjhunwala S, Haverty PM, Gnad F, Guan Y, Gilbert HN, Stinson J, Klijn C, Guillory J, Bhatt D, Vartanian S, Walter K, ... ... Hoeflich KP, et al. Genome and transcriptome sequencing of lung cancers reveal diverse mutational and splicing events. Genome Research. 22: 2315-27. PMID 23033341 DOI: 10.1101/gr.140988.112  0.84
2012 Chow HY, Jubb AM, Koch JN, Jaffer ZM, Stepanova D, Campbell DA, Duron SG, O'Farrell M, Cai KQ, Klein-Szanto AJ, Gutkind JS, Hoeflich KP, Chernoff J. p21-Activated kinase 1 is required for efficient tumor formation and progression in a Ras-mediated skin cancer model. Cancer Research. 72: 5966-75. PMID 22983922 DOI: 10.1158/0008-5472.CAN-12-2246  0.84
2012 Baudy AR, Dogan T, Flores-Mercado JE, Hoeflich KP, Su F, van Bruggen N, Williams SP. FDG-PET is a good biomarker of both early response and acquired resistance in BRAFV600 mutant melanomas treated with vemurafenib and the MEK inhibitor GDC-0973. Ejnmmi Research. 2: 22. PMID 22651703 DOI: 10.1186/2191-219X-2-22  0.84
2012 Wallin JJ, Guan J, Edgar KA, Zhou W, Francis R, Torres AC, Haverty PM, Eastham-Anderson J, Arena S, Bardelli A, Griffin S, Goodall JE, Grimshaw KM, Hoeflich KP, Torrance C, et al. Active PI3K pathway causes an invasive phenotype which can be reversed or promoted by blocking the pathway at divergent nodes. Plos One. 7: e36402. PMID 22570710 DOI: 10.1371/journal.pone.0036402  0.84
2012 Wong H, Vernillet L, Peterson A, Ware JA, Lee L, Martini JF, Yu P, Li C, Del Rosario G, Choo EF, Hoeflich KP, Shi Y, Aftab BT, Aoyama R, Lam ST, et al. Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. 18: 3090-9. PMID 22496205 DOI: 10.1158/1078-0432.CCR-12-0445  0.84
2012 Crawford JJ, Hoeflich KP, Rudolph J. p21-Activated kinase inhibitors: a patent review. Expert Opinion On Therapeutic Patents. 22: 293-310. PMID 22404134 DOI: 10.1517/13543776.2012.668758  0.84
2012 Hatzivassiliou G, Liu B, O'Brien C, Spoerke JM, Hoeflich KP, Haverty PM, Soriano R, Forrest WF, Heldens S, Chen H, Toy K, Ha C, Zhou W, Song K, Friedman LS, et al. ERK inhibition overcomes acquired resistance to MEK inhibitors. Molecular Cancer Therapeutics. 11: 1143-54. PMID 22402123 DOI: 10.1158/1535-7163.MCT-11-1010  0.84
2012 Choo EF, Belvin M, Boggs J, Deng Y, Hoeflich KP, Ly J, Merchant M, Orr C, Plise E, Robarge K, Martini JF, Kassees R, Aoyama RG, Ramaiya A, Johnston SH. Preclinical disposition of GDC-0973 and prospective and retrospective analysis of human dose and efficacy predictions. Drug Metabolism and Disposition: the Biological Fate of Chemicals. 40: 919-27. PMID 22315332 DOI: 10.1124/dmd.111.043778  0.84
2012 Hoeflich KP, Merchant M, Orr C, Chan J, Den Otter D, Berry L, Kasman I, Koeppen H, Rice K, Yang NY, Engst S, Johnston S, Friedman LS, Belvin M. Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition. Cancer Research. 72: 210-9. PMID 22084396 DOI: 10.1158/0008-5472.CAN-11-1515  0.84
2011 Lee-Hoeflich ST, Pham TQ, Dowbenko D, Munroe X, Lee J, Li L, Zhou W, Haverty PM, Pujara K, Stinson J, Chan SM, Eastham-Anderson J, Pandita A, Seshagiri S, Hoeflich KP, et al. PPM1H is a p27 phosphatase implicated in trastuzumab resistance. Cancer Discovery. 1: 326-37. PMID 22586611 DOI: 10.1158/2159-8290.CD-11-0062  0.84
2011 Ong CC, Jubb AM, Zhou W, Haverty PM, Harris AL, Belvin M, Friedman LS, Koeppen H, Hoeflich KP. p21-activated kinase 1: PAK'ed with potential. Oncotarget. 2: 491-6. PMID 21653999  0.84
2011 Ong CC, Jubb AM, Haverty PM, Zhou W, Tran V, Truong T, Turley H, O'Brien T, Vucic D, Harris AL, Belvin M, Friedman LS, Blackwood EM, Koeppen H, Hoeflich KP. Targeting p21-activated kinase 1 (PAK1) to induce apoptosis of tumor cells. Proceedings of the National Academy of Sciences of the United States of America. 108: 7177-82. PMID 21482786 DOI: 10.1073/pnas.1103350108  0.84
2011 Jubb AM, Hoeflich KP, Haverty PM, Wang J, Koeppen H. Ascl2 and 11p15.5 amplification in colorectal cancer. Gut. 60: 1606-7; author reply. PMID 21106550 DOI: 10.1136/gut.2010.231746  0.84
2010 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, et al. RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth. Nature. 464: 431-5. PMID 20130576 DOI: 10.1038/nature08833  0.84
2009 Hoeflich KP, O'Brien C, Boyd Z, Cavet G, Guerrero S, Jung K, Januario T, Savage H, Punnoose E, Truong T, Zhou W, Berry L, Murray L, Amler L, Belvin M, et al. In vivo antitumor activity of MEK and phosphatidylinositol 3-kinase inhibitors in basal-like breast cancer models. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. 15: 4649-64. PMID 19567590 DOI: 10.1158/1078-0432.CCR-09-0317  0.84
2009 Yao E, Zhou W, Lee-Hoeflich ST, Truong T, Haverty PM, Eastham-Anderson J, Lewin-Koh N, Gunter B, Belvin M, Murray LJ, Friedman LS, Sliwkowski MX, Hoeflich KP. Suppression of HER2/HER3-mediated growth of breast cancer cells with combinations of GDC-0941 PI3K inhibitor, trastuzumab, and pertuzumab. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. 15: 4147-56. PMID 19509167 DOI: 10.1158/1078-0432.CCR-08-2814  0.84
2009 Jaiswal BS, Janakiraman V, Kljavin NM, Eastham-Anderson J, Cupp JE, Liang Y, Davis DP, Hoeflich KP, Seshagiri S. Combined targeting of BRAF and CRAF or BRAF and PI3K effector pathways is required for efficacy in NRAS mutant tumors. Plos One. 4: e5717. PMID 19492075 DOI: 10.1371/journal.pone.0005717  0.84
2009 Hoeflich KP, Herter S, Tien J, Wong L, Berry L, Chan J, O'Brien C, Modrusan Z, Seshagiri S, Lackner M, Stern H, Choo E, Murray L, Friedman LS, Belvin M. Antitumor efficacy of the novel RAF inhibitor GDC-0879 is predicted by BRAFV600E mutational status and sustained extracellular signal-regulated kinase/mitogen-activated protein kinase pathway suppression. Cancer Research. 69: 3042-51. PMID 19276360 DOI: 10.1158/0008-5472.CAN-08-3563  0.84
2009 Wong H, Belvin M, Herter S, Hoeflich KP, Murray LJ, Wong L, Choo EF. Pharmacodynamics of 2-[4-[(1E)-1-(hydroxyimino)-2,3-dihydro-1H-inden-5-yl]-3-(pyridine-4-yl)-1H-pyrazol-1-yl]ethan-1-ol (GDC-0879), a potent and selective B-Raf kinase inhibitor: understanding relationships between systemic concentrations, phosphorylated mitogen-activated protein kinase kinase 1 inhibition, and efficacy. The Journal of Pharmacology and Experimental Therapeutics. 329: 360-7. PMID 19147858 DOI: 10.1124/jpet.108.148189  0.84
2008 Degtyarev M, De Mazière A, Orr C, Lin J, Lee BB, Tien JY, Prior WW, van Dijk S, Wu H, Gray DC, Davis DP, Stern HM, Murray LJ, Hoeflich KP, Klumperman J, et al. Akt inhibition promotes autophagy and sensitizes PTEN-null tumors to lysosomotropic agents. The Journal of Cell Biology. 183: 101-16. PMID 18838554 DOI: 10.1083/jcb.200801099  0.84
2008 Lee-Hoeflich ST, Crocker L, Yao E, Pham T, Munroe X, Hoeflich KP, Sliwkowski MX, Stern HM. A central role for HER3 in HER2-amplified breast cancer: implications for targeted therapy. Cancer Research. 68: 5878-87. PMID 18632642 DOI: 10.1158/0008-5472.CAN-08-0380  0.84
2008 Hoeflich KP, Jaiswal B, Davis DP, Seshagiri S. Inducible BRAF suppression models for melanoma tumorigenesis. Methods in Enzymology. 439: 25-38. PMID 18374154 DOI: 10.1016/S0076-6879(07)00403-X  0.84
2007 Gray DC, Hoeflich KP, Peng L, Gu Z, Gogineni A, Murray LJ, Eby M, Kljavin N, Seshagiri S, Cole MJ, Davis DP. pHUSH: a single vector system for conditional gene expression. Bmc Biotechnology. 7: 61. PMID 17897455 DOI: 10.1186/1472-6750-7-61  0.84
2006 Hoeflich KP, Eby MT, Forrest WF, Gray DC, Tien JY, Stern HM, Murray LJ, Davis DP, Modrusan Z, Seshagiri S. Regulation of ERK3/MAPK6 expression by BRAF. International Journal of Oncology. 29: 839-49. PMID 16964379  0.84
2006 Hoeflich KP, Gray DC, Eby MT, Tien JY, Wong L, Bower J, Gogineni A, Zha J, Cole MJ, Stern HM, Murray LJ, Davis DP, Seshagiri S. Oncogenic BRAF is required for tumor growth and maintenance in melanoma models. Cancer Research. 66: 999-1006. PMID 16424035 DOI: 10.1158/0008-5472.CAN-05-2720  0.84
2001 Ali A, Hoeflich KP, Woodgett JR. Glycogen synthase kinase-3: properties, functions, and regulation. Chemical Reviews. 101: 2527-40. PMID 11749387 DOI: 10.1021/cr000110o  0.84
2001 Hoeflich KP, Woodgett JR. Chapter 13 Mitogen-activated protein kinases and stress Cell and Molecular Response to Stress. 2: 175-193. DOI: 10.1016/S1568-1254(01)80015-2  0.84
2000 Hoeflich KP, Luo J, Rubie EA, Tsao MS, Jin O, Woodgett JR. Requirement for glycogen synthase kinase-3beta in cell survival and NF-kappaB activation. Nature. 406: 86-90. PMID 10894547 DOI: 10.1038/35017574  0.84
1999 Hoeflich KP, Yeh WC, Yao Z, Mak TW, Woodgett JR. Mediation of TNF receptor-associated factor effector functions by apoptosis signal-regulating kinase-1 (ASK1). Oncogene. 18: 5814-20. PMID 10523862 DOI: 10.1038/sj.onc.1202975  0.84
1999 Cannons JL, Hoeflich KP, Woodgett JR, Watts TH. Role of the stress kinase pathway in signaling via the T cell costimulatory receptor 4-1BB. Journal of Immunology (Baltimore, Md. : 1950). 163: 2990-8. PMID 10477561  0.84
1999 Lee ST, Hoeflich KP, Wasfy GW, Woodgett JR, Leber B, Andrews DW, Hedley DW, Penn LZ. Bcl-2 targeted to the endoplasmic reticulum can inhibit apoptosis induced by Myc but not etoposide in Rat-1 fibroblasts. Oncogene. 18: 3520-8. PMID 10376530 DOI: 10.1038/sj.onc.1202716  0.84
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