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Items: 1 to 20 of 56

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, Gr├╝tzmann 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 ╬▓-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.

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