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Items: 24


Efficacy of a Covalent ERK1/2 Inhibitor, CC-90003, in KRAS-Mutant Cancer Models Reveals Novel Mechanisms of Response and Resistance.

Aronchik I, Dai Y, Labenski M, Barnes C, Jones T, Qiao L, Beebe L, Malek M, Elis W, Shi T, Mavrommatis K, Bray GL, Filvaroff EH.

Mol Cancer Res. 2019 Feb;17(2):642-654. doi: 10.1158/1541-7786.MCR-17-0554. Epub 2018 Oct 1.


Transcriptional and post-translational modifications of B-Raf in quinol-thioether induced tuberous sclerosis renal cell carcinoma.

Cohen JD, Labenski M, Mastrandrea NJ, Canatsey RD, Monks TJ, Lau SS.

Mol Carcinog. 2016 Aug;55(8):1243-50. doi: 10.1002/mc.22366. Epub 2015 Aug 31.


S-adenosyl-l-methionine protection of acetaminophen mediated oxidative stress and identification of hepatic 4-hydroxynonenal protein adducts by mass spectrometry.

Brown JM, Kuhlman C, Terneus MV, Labenski MT, Lamyaithong AB, Ball JG, Lau SS, Valentovic MA.

Toxicol Appl Pharmacol. 2014 Dec 1;281(2):174-84. doi: 10.1016/j.taap.2014.08.027. Epub 2014 Sep 22.


In vitro and in vivo characterization of irreversible mutant-selective EGFR inhibitors that are wild-type sparing.

Tjin Tham Sjin R, Lee K, Walter AO, Dubrovskiy A, Sheets M, Martin TS, Labenski MT, Zhu Z, Tester R, Karp R, Medikonda A, Chaturvedi P, Ren Y, Haringsma H, Etter J, Raponi M, Simmons AD, Harding TC, Niu D, Nacht M, Westlin WF, Petter RC, Allen A, Singh J.

Mol Cancer Ther. 2014 Jun;13(6):1468-79. doi: 10.1158/1535-7163.MCT-13-0966. Epub 2014 Apr 10.


Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC.

Walter AO, Sjin RT, Haringsma HJ, Ohashi K, Sun J, Lee K, Dubrovskiy A, Labenski M, Zhu Z, Wang Z, Sheets M, St Martin T, Karp R, van Kalken D, Chaturvedi P, Niu D, Nacht M, Petter RC, Westlin W, Lin K, Jaw-Tsai S, Raponi M, Van Dyke T, Etter J, Weaver Z, Pao W, Singh J, Simmons AD, Harding TC, Allen A.

Cancer Discov. 2013 Dec;3(12):1404-15. doi: 10.1158/2159-8290.CD-13-0314. Epub 2013 Sep 24.


Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans.

Evans EK, Tester R, Aslanian S, Karp R, Sheets M, Labenski MT, Witowski SR, Lounsbury H, Chaturvedi P, Mazdiyasni H, Zhu Z, Nacht M, Freed MI, Petter RC, Dubrovskiy A, Singh J, Westlin WF.

J Pharmacol Exp Ther. 2013 Aug;346(2):219-28. doi: 10.1124/jpet.113.203489. Epub 2013 May 24.


Orally active fumagillin analogues: transformations of a reactive warhead in the gastric environment.

Arico-Muendel CC, Blanchette H, Benjamin DR, Caiazzo TM, Centrella PA, DeLorey J, Doyle EG, Johnson SR, Labenski MT, Morgan BA, O'Donovan G, Sarjeant AA, Skinner S, Thompson CD, Griffin ST, Westlin W, White KF.

ACS Med Chem Lett. 2013 Feb 22;4(4):381-6. doi: 10.1021/ml3003633. eCollection 2013 Apr 11.


Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kα.

Nacht M, Qiao L, Sheets MP, St Martin T, Labenski M, Mazdiyasni H, Karp R, Zhu Z, Chaturvedi P, Bhavsar D, Niu D, Westlin W, Petter RC, Medikonda AP, Singh J.

J Med Chem. 2013 Feb 14;56(3):712-21. doi: 10.1021/jm3008745. Epub 2013 Feb 5.


Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity.

Arico-Muendel CC, Belanger B, Benjamin D, Blanchette HS, Caiazzo TM, Centrella PA, DeLorey J, Doyle EG, Gradhand U, Griffin ST, Hill S, Labenski MT, Morgan BA, O'Donovan G, Prasad K, Skinner S, Taghizadeh N, Thompson CD, Wakefield J, Westlin W, White KF.

Drug Metab Dispos. 2013 Apr;41(4):814-26. doi: 10.1124/dmd.112.048355. Epub 2013 Jan 25.


The frequency of 1,4-benzoquinone-lysine adducts in cytochrome c correlate with defects in apoptosome activation.

Fisher AA, Labenski MT, Malladi S, Chapman JD, Bratton SB, Monks TJ, Lau SS.

Toxicol Sci. 2011 Jul;122(1):64-72. doi: 10.1093/toxsci/kfr085. Epub 2011 Apr 28.


Selective irreversible inhibition of a protease by targeting a noncatalytic cysteine.

Hagel M, Niu D, St Martin T, Sheets MP, Qiao L, Bernard H, Karp RM, Zhu Z, Labenski MT, Chaturvedi P, Nacht M, Westlin WF, Petter RC, Singh J.

Nat Chem Biol. 2011 Jan;7(1):22-4. doi: 10.1038/nchembio.492. Epub 2010 Nov 28.


Identification of chemical-adducted proteins in urine by multi-dimensional protein identification technology (LC/LC-MS/MS).

Labenski MT, Fisher AA, Monks TJ, Lau SS.

Methods Mol Biol. 2011;691:339-47. doi: 10.1007/978-1-60761-849-2_21.


One-dimensional western blotting coupled to LC-MS/MS analysis to identify chemical-adducted proteins in rat urine.

Labenski MT, Fisher AA, Monks TJ, Lau SS.

Methods Mol Biol. 2011;691:327-38. doi: 10.1007/978-1-60761-849-2_20.


Utilization of LC-MS/MS analyses to identify site-specific chemical protein adducts in vitro.

Fisher AA, Labenski MT, Monks TJ, Lau SS.

Methods Mol Biol. 2011;691:317-26. doi: 10.1007/978-1-60761-849-2_19.


Utilization of MALDI-TOF to determine chemical-protein adduct formation in vitro.

Fisher AA, Labenski MT, Monks TJ, Lau SS.

Methods Mol Biol. 2011;691:303-16. doi: 10.1007/978-1-60761-849-2_18.


Carbamate analogues of fumagillin as potent, targeted inhibitors of methionine aminopeptidase-2.

Arico-Muendel CC, Benjamin DR, Caiazzo TM, Centrella PA, Contonio BD, Cook CM, Doyle EG, Hannig G, Labenski MT, Searle LL, Lind K, Morgan BA, Olson G, Paradise CL, Self C, Skinner SR, Sluboski B, Svendsen JL, Thompson CD, Westlin W, White KF.

J Med Chem. 2009 Dec 24;52(24):8047-56. doi: 10.1021/jm901260k.


Protein electrophile-binding motifs: lysine-rich proteins are preferential targets of quinones.

Labenski MT, Fisher AA, Lo HH, Monks TJ, Lau SS.

Drug Metab Dispos. 2009 Jun;37(6):1211-8. doi: 10.1124/dmd.108.026211. Epub 2009 Feb 27.


An inhibitor of methionine aminopeptidase type-2, PPI-2458, ameliorates the pathophysiological disease processes of rheumatoid arthritis.

Lazarus DD, Doyle EG, Bernier SG, Rogers AB, Labenski MT, Wakefield JD, Karp RM, Clark EJ, Lorusso J, Hoyt JG, Thompson CD, Hannig G, Westlin WF.

Inflamm Res. 2008 Jan;57(1):18-27. doi: 10.1007/s00011-007-7075-5.


Quinone electrophiles selectively adduct "electrophile binding motifs" within cytochrome c.

Fisher AA, Labenski MT, Malladi S, Gokhale V, Bowen ME, Milleron RS, Bratton SB, Monks TJ, Lau SS.

Biochemistry. 2007 Oct 2;46(39):11090-100. Epub 2007 Sep 7.


A novel methionine aminopeptidase-2 inhibitor, PPI-2458, inhibits non-Hodgkin's lymphoma cell proliferation in vitro and in vivo.

Cooper AC, Karp RM, Clark EJ, Taghizadeh NR, Hoyt JG, Labenski MT, Murray MJ, Hannig G, Westlin WF, Thompson CD.

Clin Cancer Res. 2006 Apr 15;12(8):2583-90.


Inhibition of melanoma tumor growth by a pharmacological inhibitor of MetAP-2, PPI-2458.

Hannig G, Lazarus DD, Bernier SG, Karp RM, Lorusso J, Qiu D, Labenski MT, Wakefield JD, Thompson CD, Westlin WF.

Int J Oncol. 2006 Apr;28(4):955-63.


A methionine aminopeptidase-2 inhibitor, PPI-2458, for the treatment of rheumatoid arthritis.

Bernier SG, Lazarus DD, Clark E, Doyle B, Labenski MT, Thompson CD, Westlin WF, Hannig G.

Proc Natl Acad Sci U S A. 2004 Jul 20;101(29):10768-73. Epub 2004 Jul 12.


Reversible in vitro growth of Alzheimer disease beta-amyloid plaques by deposition of labeled amyloid peptide.

Maggio JE, Stimson ER, Ghilardi JR, Allen CJ, Dahl CE, Whitcomb DC, Vigna SR, Vinters HV, Labenski ME, Mantyh PW.

Proc Natl Acad Sci U S A. 1992 Jun 15;89(12):5462-6.


Receptor binding sites for cholecystokinin, galanin, somatostatin, substance P and vasoactive intestinal polypeptide in sympathetic ganglia.

Mantyh PW, Catton MD, Allen CJ, Labenski ME, Maggio JE, Vigna SR.

Neuroscience. 1992;46(3):739-54.


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