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Items: 1 to 50 of 59

1.

Role of the E3 ubiquitin ligase RNF157 as a novel downstream effector linking PI3K and MAPK signaling pathways to the cell cycle.

Dogan T, Gnad F, Chan J, Phu L, Young A, Chen MJ, Doll S, Stokes MP, Belvin M, Friedman LS, Kirkpatrick DS, Hoeflich KP, Hatzivassiliou G.

J Biol Chem. 2017 Sep 1;292(35):14311-14324. doi: 10.1074/jbc.M117.792754. Epub 2017 Jun 27.

2.

Multiplexed gene expression profiling identifies the FGFR4 pathway as a novel biomarker in intrahepatic cholangiocarcinoma.

Yoo C, Kang J, Kim D, Kim KP, Ryoo BY, Hong SM, Hwang JJ, Jeong SY, Hwang S, Kim KH, Lee YJ, Hoeflich KP, Schmidt-Kittler O, Miller S, Choi EK.

Oncotarget. 2017 Jun 13;8(24):38592-38601. doi: 10.18632/oncotarget.16951.

3.

The PI3K inhibitor taselisib overcomes letrozole resistance in a breast cancer model expressing aromatase.

Hoeflich KP, Guan J, Edgar KA, O'Brien C, Savage H, Wilson TR, Neve RM, Friedman LS, Wallin JJ.

Genes Cancer. 2016 Mar;7(3-4):73-85. doi: 10.18632/genesandcancer.100.

4.

Synthesis and evaluation of a series of 4-azaindole-containing p21-activated kinase-1 inhibitors.

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.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3518-24. doi: 10.1016/j.bmcl.2016.06.031. Epub 2016 Jun 15.

PMID:
27346791
5.

Chemically Diverse Group I p21-Activated Kinase (PAK) Inhibitors Impart Acute Cardiovascular Toxicity with a Narrow Therapeutic Window.

Rudolph J, Murray LJ, Ndubaku CO, O'Brien T, Blackwood E, Wang W, Aliagas I, Gazzard L, Crawford JJ, Drobnick J, Lee W, Zhao X, Hoeflich KP, Favor DA, Dong P, Zhang H, Heise CE, Oh A, Ong CC, La H, Chakravarty P, Chan C, Jakubiak D, Epler J, Ramaswamy S, Vega R, Cain G, Diaz D, Zhong Y.

J Med Chem. 2016 Jun 9;59(11):5520-41. doi: 10.1021/acs.jmedchem.6b00638. Epub 2016 May 24.

PMID:
27167326
6.

Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety.

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, Lin B, Lyssikatos JP, Maksimoska J, Marmorstein R, Murray LJ, O'Brien T, Oh A, Ramaswamy S, Wang W, Zhao X, Zhong Y, Blackwood E, Rudolph J.

ACS Med Chem Lett. 2015 Oct 31;6(12):1241-6. doi: 10.1021/acsmedchemlett.5b00398. eCollection 2015 Dec 10.

7.

p21-Activated Kinase 2 Regulates Endothelial Development and Function through the Bmk1/Erk5 Pathway.

Radu M, Lyle K, Hoeflich KP, Villamar-Cruz O, Koeppen H, Chernoff J.

Mol Cell Biol. 2015 Dec;35(23):3990-4005. doi: 10.1128/MCB.00630-15. Epub 2015 Sep 21.

8.

Leveraging the Pre-DFG Residue Thr-406 To Obtain High Kinase Selectivity in an Aminopyrazole-Type PAK1 Inhibitor Series.

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.

ACS Med Chem Lett. 2015 May 20;6(6):711-5. doi: 10.1021/acsmedchemlett.5b00151. eCollection 2015 Jun 11.

9.

Structure-Guided Design of Group I Selective p21-Activated Kinase Inhibitors.

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, Mintzer R, Liu Y, Chao Q, Rudolph J.

J Med Chem. 2015 Jun 25;58(12):5121-36. doi: 10.1021/acs.jmedchem.5b00572. Epub 2015 Jun 12.

PMID:
26030457
10.

Targeting cancer with kinase inhibitors.

Gross S, Rahal R, Stransky N, Lengauer C, Hoeflich KP.

J Clin Invest. 2015 May;125(5):1780-9. doi: 10.1172/JCI76094. Epub 2015 May 1. Review.

11.

Small molecule inhibition of group I p21-activated kinases in breast cancer induces apoptosis and potentiates the activity of microtubule stabilizing agents.

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, Behnke ML, Huang W, McKew JC, Chernoff J, Forrest WF, Haverty PM, Chin SF, Rakha EA, Green AR, Ellis IO, Caldas C, O'Brien T, Friedman LS, Koeppen H, Rudolph J, Hoeflich KP.

Breast Cancer Res. 2015 Apr 23;17:59. doi: 10.1186/s13058-015-0564-5.

12.

Group I Paks as therapeutic targets in NF2-deficient meningioma.

Chow HY, Dong B, Duron SG, Campbell DA, Ong CC, Hoeflich KP, Chang LS, Welling DB, Yang ZJ, Chernoff J.

Oncotarget. 2015 Feb 10;6(4):1981-94.

13.

Inhibitors of p21-activated kinases (PAKs).

Rudolph J, Crawford JJ, Hoeflich KP, Wang W.

J Med Chem. 2015 Jan 8;58(1):111-29. doi: 10.1021/jm501613q. Epub 2014 Dec 3.

PMID:
25415869
14.

Modeling targeted inhibition of MEK and PI3 kinase in human pancreatic cancer.

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, Singh M.

Mol Cancer Ther. 2015 Jan;14(1):40-7. doi: 10.1158/1535-7163.MCT-14-0030. Epub 2014 Nov 5.

15.

PAK1 mediates pancreatic cancer cell migration and resistance to MET inhibition.

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, Yan Y, Forrest WF, Wang Y, Raja R, Pilarsky C, de Jesus-Acosta A, Belvin M, Friedman LS, Merchant M, Jaffee EM, Zheng L, Koeppen H, Hoeflich KP.

J Pathol. 2014 Dec;234(4):502-13. doi: 10.1002/path.4412. Epub 2014 Oct 6.

16.

Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors.

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, Roberts DA, Rouge L, Rudolph J, Tam C, Wang W, Xiao Y, Young A, Zhang Y, Hoeflich KP.

J Med Chem. 2014 Feb 13;57(3):1033-45. doi: 10.1021/jm401768t. Epub 2014 Feb 4.

PMID:
24432870
17.

Phosphoproteomic characterization of DNA damage response in melanoma cells following MEK/PI3K dual inhibition.

Kirkpatrick DS, Bustos DJ, Dogan T, Chan J, Phu L, Young A, Friedman LS, Belvin M, Song Q, Bakalarski CE, Hoeflich KP.

Proc Natl Acad Sci U S A. 2013 Nov 26;110(48):19426-31. doi: 10.1073/pnas.1309473110. Epub 2013 Nov 11. Erratum in: Proc Natl Acad Sci U S A. 2014 Jan 7;111(1):562.

18.

Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers.

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, Ludlam MJ, Wiesmann C, Ultsch M, Friedman LS, Malek S, Belvin M.

Nature. 2013 Sep 12;501(7466):232-6. doi: 10.1038/nature12441. Epub 2013 Aug 11. Erratum in: Nature. 2013 Oct 10;502(7470):258.

PMID:
23934108
19.

Systems-wide analysis of K-Ras, Cdc42, and PAK4 signaling by quantitative phosphoproteomics.

Gnad F, Young A, Zhou W, Lyle K, Ong CC, Stokes MP, Silva JC, Belvin M, Friedman LS, Koeppen H, Minden A, Hoeflich KP.

Mol Cell Proteomics. 2013 Aug;12(8):2070-80. doi: 10.1074/mcp.M112.027052. Epub 2013 Apr 22.

20.

Pak1 kinase links ErbB2 to β-catenin in transformation of breast epithelial cells.

Arias-Romero LE, Villamar-Cruz O, Huang M, Hoeflich KP, Chernoff J.

Cancer Res. 2013 Jun 15;73(12):3671-82. doi: 10.1158/0008-5472.CAN-12-4453. Epub 2013 Apr 10.

21.

P21-activated kinase 1 (PAK1) as a therapeutic target in BRAF wild-type melanoma.

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, Koeppen H, Hoeflich KP.

J Natl Cancer Inst. 2013 May 1;105(9):606-7. doi: 10.1093/jnci/djt054. Epub 2013 Mar 27.

PMID:
23535073
22.

p21-activated kinase inhibitors.

Rudolph J, Crawford JJ, Hoeflich KP, Chernoff J.

Enzymes. 2013;34 Pt. B:157-80. doi: 10.1016/B978-0-12-420146-0.00007-X. Epub 2013 Nov 7. Review.

PMID:
25034104
23.

Genome and transcriptome sequencing of lung cancers reveal diverse mutational and splicing events.

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, Chan J, Holcomb T, Dijkgraaf P, Johnson S, Koeman J, Minna JD, Gazdar AF, Stern HM, Hoeflich KP, Wu TD, Settleman J, de Sauvage FJ, Gentleman RC, Neve RM, Stokoe D, Modrusan Z, Seshagiri S, Shames DS, Zhang Z.

Genome Res. 2012 Dec;22(12):2315-27. doi: 10.1101/gr.140988.112. Epub 2012 Oct 2.

24.

p21-Activated kinase 1 is required for efficient tumor formation and progression in a Ras-mediated skin cancer model.

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.

Cancer Res. 2012 Nov 15;72(22):5966-75. doi: 10.1158/0008-5472.CAN-12-2246. Epub 2012 Sep 14.

25.

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.

Baudy AR, Dogan T, Flores-Mercado JE, Hoeflich KP, Su F, van Bruggen N, Williams SP.

EJNMMI Res. 2012 May 31;2(1):22. doi: 10.1186/2191-219X-2-22.

26.

PPM1H is a p27 phosphatase implicated in trastuzumab resistance.

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, Turashvili G, Gelmon KA, Aparicio SA, Davis DP, Sliwkowski MX, Stern HM.

Cancer Discov. 2011 Sep;1(4):326-37. doi: 10.1158/2159-8290.CD-11-0062. Epub 2011 Jul 20.

27.

Active PI3K pathway causes an invasive phenotype which can be reversed or promoted by blocking the pathway at divergent nodes.

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, Belvin M, Friedman LS.

PLoS One. 2012;7(5):e36402. doi: 10.1371/journal.pone.0036402. Epub 2012 May 3.

28.

Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor.

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, Belvin M, Prescott J.

Clin Cancer Res. 2012 Jun 1;18(11):3090-9. doi: 10.1158/1078-0432.CCR-12-0445. Epub 2012 Apr 10.

29.

p21-Activated kinase inhibitors: a patent review.

Crawford JJ, Hoeflich KP, Rudolph J.

Expert Opin Ther Pat. 2012 Mar;22(3):293-310. doi: 10.1517/13543776.2012.668758. Epub 2012 Mar 11. Review.

PMID:
22404134
30.

ERK inhibition overcomes acquired resistance to MEK inhibitors.

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, Amler LC, Hampton GM, Moffat J, Belvin M, Lackner MR.

Mol Cancer Ther. 2012 May;11(5):1143-54. doi: 10.1158/1535-7163.MCT-11-1010. Epub 2012 Mar 8.

31.

Preclinical disposition of GDC-0973 and prospective and retrospective analysis of human dose and efficacy predictions.

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.

Drug Metab Dispos. 2012 May;40(5):919-27. doi: 10.1124/dmd.111.043778. Epub 2012 Feb 7.

32.

Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition.

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.

Cancer Res. 2012 Jan 1;72(1):210-9. doi: 10.1158/0008-5472.CAN-11-1515. Epub 2011 Nov 14.

33.

p21-activated kinase 1: PAK'ed with potential.

Ong CC, Jubb AM, Zhou W, Haverty PM, Harris AL, Belvin M, Friedman LS, Koeppen H, Hoeflich KP.

Oncotarget. 2011 Jun;2(6):491-6. Review.

34.

Targeting p21-activated kinase 1 (PAK1) to induce apoptosis of tumor cells.

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.

Proc Natl Acad Sci U S A. 2011 Apr 26;108(17):7177-82. doi: 10.1073/pnas.1103350108. Epub 2011 Apr 11.

35.

Ascl2 and 11p15.5 amplification in colorectal cancer.

Jubb AM, Hoeflich KP, Haverty PM, Wang J, Koeppen H.

Gut. 2011 Nov;60(11):1606-7; author reply 1607. doi: 10.1136/gut.2010.231746. Epub 2010 Nov 23. No abstract available.

PMID:
21106550
36.

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
37.

Identifying genotype-dependent efficacy of single and combined PI3K- and MAPK-pathway inhibition in cancer.

Sos ML, Fischer S, Ullrich R, Peifer M, Heuckmann JM, Koker M, Heynck S, Stückrath I, Weiss J, Fischer F, Michel K, Goel A, Regales L, Politi KA, Perera S, Getlik M, Heukamp LC, Ansén S, Zander T, Beroukhim R, Kashkar H, Shokat KM, Sellers WR, Rauh D, Orr C, Hoeflich KP, Friedman L, Wong KK, Pao W, Thomas RK.

Proc Natl Acad Sci U S A. 2009 Oct 27;106(43):18351-6. doi: 10.1073/pnas.0907325106. Epub 2009 Oct 5.

38.

In vivo antitumor activity of MEK and phosphatidylinositol 3-kinase inhibitors in basal-like breast cancer models.

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, Friedman LS, Lackner MR.

Clin Cancer Res. 2009 Jul 15;15(14):4649-64. doi: 10.1158/1078-0432.CCR-09-0317. Epub 2009 Jun 30.

39.

Suppression of HER2/HER3-mediated growth of breast cancer cells with combinations of GDC-0941 PI3K inhibitor, trastuzumab, and pertuzumab.

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.

Clin Cancer Res. 2009 Jun 15;15(12):4147-56. doi: 10.1158/1078-0432.CCR-08-2814. Epub 2009 Jun 9.

40.

Combined targeting of BRAF and CRAF or BRAF and PI3K effector pathways is required for efficacy in NRAS mutant tumors.

Jaiswal BS, Janakiraman V, Kljavin NM, Eastham-Anderson J, Cupp JE, Liang Y, Davis DP, Hoeflich KP, Seshagiri S.

PLoS One. 2009 May 27;4(5):e5717. doi: 10.1371/journal.pone.0005717.

41.

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.

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.

Cancer Res. 2009 Apr 1;69(7):3042-51. doi: 10.1158/0008-5472.CAN-08-3563. Epub 2009 Mar 10.

43.

Akt inhibition promotes autophagy and sensitizes PTEN-null tumors to lysosomotropic agents.

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, Friedman LS, Lin K.

J Cell Biol. 2008 Oct 6;183(1):101-16. doi: 10.1083/jcb.200801099.

44.

A central role for HER3 in HER2-amplified breast cancer: implications for targeted therapy.

Lee-Hoeflich ST, Crocker L, Yao E, Pham T, Munroe X, Hoeflich KP, Sliwkowski MX, Stern HM.

Cancer Res. 2008 Jul 15;68(14):5878-87. doi: 10.1158/0008-5472.CAN-08-0380.

45.

Inducible BRAF suppression models for melanoma tumorigenesis.

Hoeflich KP, Jaiswal B, Davis DP, Seshagiri S.

Methods Enzymol. 2008;439:25-38. doi: 10.1016/S0076-6879(07)00403-X.

PMID:
18374154
46.

pHUSH: a single vector system for conditional gene expression.

Gray DC, Hoeflich KP, Peng L, Gu Z, Gogineni A, Murray LJ, Eby M, Kljavin N, Seshagiri S, Cole MJ, Davis DP.

BMC Biotechnol. 2007 Sep 26;7:61.

47.

Regulation of ERK3/MAPK6 expression by BRAF.

Hoeflich KP, Eby MT, Forrest WF, Gray DC, Tien JY, Stern HM, Murray LJ, Davis DP, Modrusan Z, Seshagiri S.

Int J Oncol. 2006 Oct;29(4):839-49.

PMID:
16964379
48.

Oncogenic BRAF is required for tumor growth and maintenance in melanoma models.

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.

Cancer Res. 2006 Jan 15;66(2):999-1006.

49.

Characterization of dual substrate binding sites in the homodimeric structure of Escherichia coli mRNA interferase MazF.

Li GY, Zhang Y, Chan MC, Mal TK, Hoeflich KP, Inouye M, Ikura M.

J Mol Biol. 2006 Mar 17;357(1):139-50. Epub 2005 Dec 27.

PMID:
16413577
50.

Radixin: cytoskeletal adopter and signaling protein.

Hoeflich KP, Ikura M.

Int J Biochem Cell Biol. 2004 Nov;36(11):2131-6. Review.

PMID:
15313460

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