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Items: 26


The p97 Inhibitor CB-5083 Is a Unique Disrupter of Protein Homeostasis in Models of Multiple Myeloma.

Le Moigne R, Aftab BT, Djakovic S, Dhimolea E, Valle E, Murnane M, King EM, Soriano F, Menon MK, Wu ZY, Wong ST, Lee GJ, Yao B, Wiita AP, Lam C, Rice J, Wang J, Chesi M, Bergsagel PL, Kraus M, Driessen C, Kiss von Soly S, Yakes FM, Wustrow D, Shawver L, Zhou HJ, Martin TG 3rd, Wolf JL, Mitsiades CS, Anderson DJ, Rolfe M.

Mol Cancer Ther. 2017 Nov;16(11):2375-2386. doi: 10.1158/1535-7163.MCT-17-0233. Epub 2017 Sep 6.


Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083).

Zhou HJ, Wang J, Yao B, Wong S, Djakovic S, Kumar B, Rice J, Valle E, Soriano F, Menon MK, Madriaga A, Kiss von Soly S, Kumar A, Parlati F, Yakes FM, Shawver L, Le Moigne R, Anderson DJ, Rolfe M, Wustrow D.

J Med Chem. 2015 Dec 24;58(24):9480-97. doi: 10.1021/acs.jmedchem.5b01346. Epub 2015 Dec 4.


Targeting the AAA ATPase p97 as an Approach to Treat Cancer through Disruption of Protein Homeostasis.

Anderson DJ, Le Moigne R, Djakovic S, Kumar B, Rice J, Wong S, Wang J, Yao B, Valle E, Kiss von Soly S, Madriaga A, Soriano F, Menon MK, Wu ZY, Kampmann M, Chen Y, Weissman JS, Aftab BT, Yakes FM, Shawver L, Zhou HJ, Wustrow D, Rolfe M.

Cancer Cell. 2015 Nov 9;28(5):653-665. doi: 10.1016/j.ccell.2015.10.002.


The Selective PI3K Inhibitor XL147 (SAR245408) Inhibits Tumor Growth and Survival and Potentiates the Activity of Chemotherapeutic Agents in Preclinical Tumor Models.

Foster P, Yamaguchi K, Hsu PP, Qian F, Du X, Wu J, Won KA, Yu P, Jaeger CT, Zhang W, Marlowe CK, Keast P, Abulafia W, Chen J, Young J, Plonowski A, Yakes FM, Chu F, Engell K, Bentzien F, Lam ST, Dale S, Yturralde O, Matthews DJ, Lamb P, Laird AD.

Mol Cancer Ther. 2015 Apr;14(4):931-40. doi: 10.1158/1535-7163.MCT-14-0833. Epub 2015 Jan 30.


Characterization of the activity of the PI3K/mTOR inhibitor XL765 (SAR245409) in tumor models with diverse genetic alterations affecting the PI3K pathway.

Yu P, Laird AD, Du X, Wu J, Won KA, Yamaguchi K, Hsu PP, Qian F, Jaeger CT, Zhang W, Buhr CA, Shen P, Abulafia W, Chen J, Young J, Plonowski A, Yakes FM, Chu F, Lee M, Bentzien F, Lam ST, Dale S, Matthews DJ, Lamb P, Foster P.

Mol Cancer Ther. 2014 May;13(5):1078-91. doi: 10.1158/1535-7163.MCT-13-0709. Epub 2014 Mar 14.


In vitro and in vivo activity of cabozantinib (XL184), an inhibitor of RET, MET, and VEGFR2, in a model of medullary thyroid cancer.

Bentzien F, Zuzow M, Heald N, Gibson A, Shi Y, Goon L, Yu P, Engst S, Zhang W, Huang D, Zhao L, Vysotskaia V, Chu F, Bautista R, Cancilla B, Lamb P, Joly AH, Yakes FM.

Thyroid. 2013 Dec;23(12):1569-77. doi: 10.1089/thy.2013.0137. Epub 2013 Sep 17.


The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.

Kim MH, Tsuhako AL, Co EW, Aftab DT, Bentzien F, Chen J, Cheng W, Engst S, Goon L, Klein RR, Le DT, Mac M, Parks JJ, Qian F, Rodriquez M, Stout TJ, Till JH, Won KA, Wu X, Yakes FM, Yu P, Zhang W, Zhao Y, Lamb P, Nuss JM, Xu W.

Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85. doi: 10.1016/j.bmcl.2012.06.029. Epub 2012 Jun 16.


Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth.

Yakes FM, Chen J, Tan J, Yamaguchi K, Shi Y, Yu P, Qian F, Chu F, Bentzien F, Cancilla B, Orf J, You A, Laird AD, Engst S, Lee L, Lesch J, Chou YC, Joly AH.

Mol Cancer Ther. 2011 Dec;10(12):2298-308. doi: 10.1158/1535-7163.MCT-11-0264. Epub 2011 Sep 16.


Inhibition of tumor cell growth, invasion, and metastasis by EXEL-2880 (XL880, GSK1363089), a novel inhibitor of HGF and VEGF receptor tyrosine kinases.

Qian F, Engst S, Yamaguchi K, Yu P, Won KA, Mock L, Lou T, Tan J, Li C, Tam D, Lougheed J, Yakes FM, Bentzien F, Xu W, Zaks T, Wooster R, Greshock J, Joly AH.

Cancer Res. 2009 Oct 15;69(20):8009-16. doi: 10.1158/0008-5472.CAN-08-4889. Epub 2009 Oct 6.


Inhibition of the T790M gatekeeper mutant of the epidermal growth factor receptor by EXEL-7647.

Gendreau SB, Ventura R, Keast P, Laird AD, Yakes FM, Zhang W, Bentzien F, Cancilla B, Lutman J, Chu F, Jackman L, Shi Y, Yu P, Wang J, Aftab DT, Jaeger CT, Meyer SM, De Costa A, Engell K, Chen J, Martini JF, Joly AH.

Clin Cancer Res. 2007 Jun 15;13(12):3713-23.


Pharmacological abrogation of S-phase checkpoint enhances the anti-tumor activity of gemcitabine in vivo.

Matthews DJ, Yakes FM, Chen J, Tadano M, Bornheim L, Clary DO, Tai A, Wagner JM, Miller N, Kim YD, Robertson S, Murray L, Karnitz LM.

Cell Cycle. 2007 Jan 1;6(1):104-10. Epub 2007 Jan 7.


Functional studies on the anti-pathoangiogenic properties of CM101.

Yan HP, Carter CE, Wang EZ, Page DL, Washington K, Wamil BD, Yakes FM, Thurman GB, Hellerqvist CG.

Angiogenesis. 1998;2(3):219-33.


Loss of PTEN/MMAC1/TEP in EGF receptor-expressing tumor cells counteracts the antitumor action of EGFR tyrosine kinase inhibitors.

Bianco R, Shin I, Ritter CA, Yakes FM, Basso A, Rosen N, Tsurutani J, Dennis PA, Mills GB, Arteaga CL.

Oncogene. 2003 May 8;22(18):2812-22.


PKB/Akt mediates cell-cycle progression by phosphorylation of p27(Kip1) at threonine 157 and modulation of its cellular localization.

Shin I, Yakes FM, Rojo F, Shin NY, Bakin AV, Baselga J, Arteaga CL.

Nat Med. 2002 Oct;8(10):1145-52. Epub 2002 Sep 16.


HER (erbB) tyrosine kinase inhibitors in the treatment of breast cancer.

Arteaga CL, Moulder SL, Yakes FM.

Semin Oncol. 2002 Jun;29(3 Suppl 11):4-10. Review.


Herceptin-induced inhibition of phosphatidylinositol-3 kinase and Akt Is required for antibody-mediated effects on p27, cyclin D1, and antitumor action.

Yakes FM, Chinratanalab W, Ritter CA, King W, Seelig S, Arteaga CL.

Cancer Res. 2002 Jul 15;62(14):4132-41.


Mutations associated with base excision repair deficiency and methylation-induced genotoxic stress.

Sobol RW, Watson DE, Nakamura J, Yakes FM, Hou E, Horton JK, Ladapo J, Van Houten B, Swenberg JA, Tindall KR, Samson LD, Wilson SH.

Proc Natl Acad Sci U S A. 2002 May 14;99(10):6860-5. Epub 2002 Apr 30.


Identification of a novel membrane protein, HP59, with therapeutic potential as a target of tumor angiogenesis.

Fu C, Bardhan S, Cetateanu ND, Wamil BD, Wang Y, Yan HP, Shi E, Carter C, Venkov C, Yakes FM, Page DL, Lloyd RS, Mernaugh RL, Hellerqvist CG.

Clin Cancer Res. 2001 Dec;7(12):4182-94.


Tyrosine kinase inhibitors: rationale, mechanisms of action, and implications for drug resistance.

Busse D, Yakes FM, Lenferink AE, Arteaga CL.

Semin Oncol. 2001 Oct;28(5 Suppl 16):47-55. Review.


ErbB2/neu kinase modulates cellular p27(Kip1) and cyclin D1 through multiple signaling pathways.

Lenferink AE, Busse D, Flanagan WM, Yakes FM, Arteaga CL.

Cancer Res. 2001 Sep 1;61(17):6583-91.


Cyclin-dependent kinase inhibitor p27(Kip1) is required for mouse mammary gland morphogenesis and function.

Muraoka RS, Lenferink AE, Simpson J, Brantley DM, Roebuck LR, Yakes FM, Arteaga CL.

J Cell Biol. 2001 May 28;153(5):917-32.


CM101 treatment overrides tumor-induced immunoprivilege leading to apoptosis.

Yakes FM, Wamil BD, Sun F, Yan HP, Carter CE, Hellerqvist CG.

Cancer Res. 2000 Oct 15;60(20):5740-6.


Hydrogen peroxide- and peroxynitrite-induced mitochondrial DNA damage and dysfunction in vascular endothelial and smooth muscle cells.

Ballinger SW, Patterson C, Yan CN, Doan R, Burow DL, Young CG, Yakes FM, Van Houten B, Ballinger CA, Freeman BA, Runge MS.

Circ Res. 2000 May 12;86(9):960-6.


Up-regulation of base excision repair correlates with enhanced protection against a DNA damaging agent in mouse cell lines.

Chen KH, Yakes FM, Srivastava DK, Singhal RK, Sobol RW, Horton JK, Van Houten B, Wilson SH.

Nucleic Acids Res. 1998 Apr 15;26(8):2001-7.


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