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Items: 39


Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor.

Janes MR, Zhang J, Li LS, Hansen R, Peters U, Guo X, Chen Y, Babbar A, Firdaus SJ, Darjania L, Feng J, Chen JH, Li S, Li S, Long YO, Thach C, Liu Y, Zarieh A, Ely T, Kucharski JM, Kessler LV, Wu T, Yu K, Wang Y, Yao Y, Deng X, Zarrinkar PP, Brehmer D, Dhanak D, Lorenzi MV, Hu-Lowe D, Patricelli MP, Ren P, Liu Y.

Cell. 2018 Jan 25;172(3):578-589.e17. doi: 10.1016/j.cell.2018.01.006.


Correction: Identification of a Tumor Specific, Active-Site Mutation in Casein Kinase 1α by Chemical Proteomics.

Okerberg ES, Hainley A, Brown H, Aban A, Alemayehu S, Shih A, Wu J, Patricelli MP, Kozarich JW, Nomanbhoy T, Rosenblum JS.

PLoS One. 2017 Feb 15;12(2):e0172649. doi: 10.1371/journal.pone.0172649. eCollection 2017.


Pathophysiological significance and therapeutic targeting of germinal center kinase in diffuse large B-cell lymphoma.

Matthews JM, Bhatt S, Patricelli MP, Nomanbhoy TK, Jiang X, Natkunam Y, Gentles AJ, Martinez E, Zhu D, Chapman JR, Cortizas E, Shyam R, Chinichian S, Advani R, Tan L, Zhang J, Choi HG, Tibshirani R, Buhrlage SJ, Gratzinger D, Verdun R, Gray NS, Lossos IS.

Blood. 2016 Jul 14;128(2):239-48. doi: 10.1182/blood-2016-02-696856. Epub 2016 May 5.


Identification of a Tumor Specific, Active-Site Mutation in Casein Kinase 1α by Chemical Proteomics.

Okerberg ES, Hainley A, Brown H, Aban A, Alemayehu S, Shih A, Wu J, Patricelli MP, Kozarich JW, Nomanbhoy T, Rosenblum JS.

PLoS One. 2016 Mar 31;11(3):e0152934. doi: 10.1371/journal.pone.0152934. eCollection 2016. Erratum in: PLoS One. 2017 Feb 15;12 (2):e0172649.


Selective Inhibition of Oncogenic KRAS Output with Small Molecules Targeting the Inactive State.

Patricelli MP, Janes MR, Li LS, Hansen R, Peters U, Kessler LV, Chen Y, Kucharski JM, Feng J, Ely T, Chen JH, Firdaus SJ, Babbar A, Ren P, Liu Y.

Cancer Discov. 2016 Mar;6(3):316-29. doi: 10.1158/2159-8290.CD-15-1105. Epub 2016 Jan 6.


Identification of novel therapeutic targets in acute leukemias with NRAS mutations using a pharmacologic approach.

Nonami A, Sattler M, Weisberg E, Liu Q, Zhang J, Patricelli MP, Christie AL, Saur AM, Kohl NE, Kung AL, Yoon H, Sim T, Gray NS, Griffin JD.

Blood. 2015 May 14;125(20):3133-43. doi: 10.1182/blood-2014-12-615906. Epub 2015 Apr 1.


Global Human-Kinase Screening Identifies Therapeutic Host Targets against Influenza.

Atkins C, Evans CW, Nordin B, Patricelli MP, Reynolds R, Wennerberg K, Noah JW.

J Biomol Screen. 2014 Jul;19(6):936-46. doi: 10.1177/1087057113518068. Epub 2014 Jan 24.


Profiling protein kinases and other ATP binding proteins in Arabidopsis using Acyl-ATP probes.

Villamor JG, Kaschani F, Colby T, Oeljeklaus J, Zhao D, Kaiser M, Patricelli MP, van der Hoorn RA.

Mol Cell Proteomics. 2013 Sep;12(9):2481-96. doi: 10.1074/mcp.M112.026278. Epub 2013 May 29.


Selective, reversible inhibitors of the AAA ATPase p97.

Chou TF, Li K, Nordin BE, Porubsky P, Frankowski K, Patricelli MP, Aubé J, Schoenen FJ, Deshaies R.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Apr 14 [updated 2013 May 1].


Characterization of Torin2, an ATP-competitive inhibitor of mTOR, ATM, and ATR.

Liu Q, Xu C, Kirubakaran S, Zhang X, Hur W, Liu Y, Kwiatkowski NP, Wang J, Westover KD, Gao P, Ercan D, Niepel M, Thoreen CC, Kang SA, Patricelli MP, Wang Y, Tupper T, Altabef A, Kawamura H, Held KD, Chou DM, Elledge SJ, Janne PA, Wong KK, Sabatini DM, Gray NS.

Cancer Res. 2013 Apr 15;73(8):2574-86. doi: 10.1158/0008-5472.CAN-12-1702. Epub 2013 Feb 22.


Brain Penetrant LRRK2 Inhibitor.

Choi HG, Zhang J, Deng X, Hatcher JM, Patricelli MP, Zhao Z, Alessi DR, Gray NS.

ACS Med Chem Lett. 2012 Aug 9;3(8):658-662. Epub 2012 Jun 18.


Chemoproteomic profiling identifies changes in DNA-PK as markers of early dengue virus infection.

Vetter ML, Rodgers MA, Patricelli MP, Yang PL.

ACS Chem Biol. 2012 Dec 21;7(12):2019-26. doi: 10.1021/cb300420z. Epub 2012 Oct 2.


Functional interplay between caspase cleavage and phosphorylation sculpts the apoptotic proteome.

Dix MM, Simon GM, Wang C, Okerberg E, Patricelli MP, Cravatt BF.

Cell. 2012 Jul 20;150(2):426-40. doi: 10.1016/j.cell.2012.05.040.


Kinome-wide selectivity profiling of ATP-competitive mammalian target of rapamycin (mTOR) inhibitors and characterization of their binding kinetics.

Liu Q, Kirubakaran S, Hur W, Niepel M, Westover K, Thoreen CC, Wang J, Ni J, Patricelli MP, Vogel K, Riddle S, Waller DL, Traynor R, Sanda T, Zhao Z, Kang SA, Zhao J, Look AT, Sorger PK, Sabatini DM, Gray NS.

J Biol Chem. 2012 Mar 23;287(13):9742-52. doi: 10.1074/jbc.M111.304485. Epub 2012 Jan 5.


In situ kinase profiling reveals functionally relevant properties of native kinases.

Patricelli MP, Nomanbhoy TK, Wu J, Brown H, Zhou D, Zhang J, Jagannathan S, Aban A, Okerberg E, Herring C, Nordin B, Weissig H, Yang Q, Lee JD, Gray NS, Kozarich JW.

Chem Biol. 2011 Jun 24;18(6):699-710. doi: 10.1016/j.chembiol.2011.04.011.


Reversible inhibitor of p97, DBeQ, impairs both ubiquitin-dependent and autophagic protein clearance pathways.

Chou TF, Brown SJ, Minond D, Nordin BE, Li K, Jones AC, Chase P, Porubsky PR, Stoltz BM, Schoenen FJ, Patricelli MP, Hodder P, Rosen H, Deshaies RJ.

Proc Natl Acad Sci U S A. 2011 Mar 22;108(12):4834-9. doi: 10.1073/pnas.1015312108. Epub 2011 Mar 7.


Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2.

Deng X, Dzamko N, Prescott A, Davies P, Liu Q, Yang Q, Lee JD, Patricelli MP, Nomanbhoy TK, Alessi DR, Gray NS.

Nat Chem Biol. 2011 Apr;7(4):203-5. doi: 10.1038/nchembio.538. Epub 2011 Mar 6.


Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein.

Yang Q, Deng X, Lu B, Cameron M, Fearns C, Patricelli MP, Yates JR 3rd, Gray NS, Lee JD.

Cancer Cell. 2010 Sep 14;18(3):258-67. doi: 10.1016/j.ccr.2010.08.008. Erratum in: Cancer Cell. 2010 Oct 19;18(4):396.


Proteomics analysis of cardiac muscle from rats with peroxisomal proliferator-activated receptor alpha (PPARalpha) stimulation.

Miyazaki M, Nakagawa I, Koga S, Kasahara Y, Patricelli MP.

J Toxicol Sci. 2010 Feb;35(1):131-5.


Determination of enzymatic source of alanine aminotransferase activity in serum from dogs with liver injury.

Miyazaki M, Rosenblum JS, Kasahara Y, Nakagawa I, Patricelli MP.

J Pharmacol Toxicol Methods. 2009 Nov-Dec;60(3):307-15. doi: 10.1016/j.vascn.2009.09.001. Epub 2009 Sep 11.


Design and synthesis of AX4697, a bisindolylmaleimide exo-affinity probe that labels protein kinase C alpha and beta.

Liu Y, Wu J, Weissig H, Betancort JM, Gai WZ, Leventhal PS, Patricelli MP, Samii B, Szardenings AK, Shreder KR, Kozarich JW.

Bioorg Med Chem Lett. 2008 Nov 15;18(22):5955-8. doi: 10.1016/j.bmcl.2008.08.045. Epub 2008 Aug 19.


Functional interrogation of the kinome using nucleotide acyl phosphates.

Patricelli MP, Szardenings AK, Liyanage M, Nomanbhoy TK, Wu M, Weissig H, Aban A, Chun D, Tanner S, Kozarich JW.

Biochemistry. 2007 Jan 16;46(2):350-8.


High-resolution functional proteomics by active-site peptide profiling.

Okerberg ES, Wu J, Zhang B, Samii B, Blackford K, Winn DT, Shreder KR, Burbaum JJ, Patricelli MP.

Proc Natl Acad Sci U S A. 2005 Apr 5;102(14):4996-5001. Epub 2005 Mar 28.


Class assignment of sequence-unrelated members of enzyme superfamilies by activity-based protein profiling.

Jessani N, Young JA, Diaz SL, Patricelli MP, Varki A, Cravatt BF.

Angew Chem Int Ed Engl. 2005 Apr 15;44(16):2400-3. No abstract available.


Activity-based probes for functional proteomics.

Patricelli MP.

Brief Funct Genomic Proteomic. 2002 Jul;1(2):151-8.


Mapping enzyme active sites in complex proteomes.

Adam GC, Burbaum J, Kozarich JW, Patricelli MP, Cravatt BF.

J Am Chem Soc. 2004 Feb 11;126(5):1363-8.


Direct visualization of serine hydrolase activities in complex proteomes using fluorescent active site-directed probes.

Patricelli MP, Giang DK, Stamp LM, Burbaum JJ.

Proteomics. 2001 Sep;1(9):1067-71.


Supersensitivity to anandamide and enhanced endogenous cannabinoid signaling in mice lacking fatty acid amide hydrolase.

Cravatt BF, Demarest K, Patricelli MP, Bracey MH, Giang DK, Martin BR, Lichtman AH.

Proc Natl Acad Sci U S A. 2001 Jul 31;98(16):9371-6. Epub 2001 Jul 24.


Characterization and manipulation of the acyl chain selectivity of fatty acid amide hydrolase.

Patricelli MP, Cravatt BF.

Biochemistry. 2001 May 22;40(20):6107-15.


Proteins regulating the biosynthesis and inactivation of neuromodulatory fatty acid amides.

Patricelli MP, Cravatt BF.

Vitam Horm. 2001;62:95-131. Review.


Fatty acid amide hydrolase substrate specificity.

Boger DL, Fecik RA, Patterson JE, Miyauchi H, Patricelli MP, Cravatt BF.

Bioorg Med Chem Lett. 2000 Dec 4;10(23):2613-6.


Exceptionally potent inhibitors of fatty acid amide hydrolase: the enzyme responsible for degradation of endogenous oleamide and anandamide.

Boger DL, Sato H, Lerner AE, Hedrick MP, Fecik RA, Miyauchi H, Wilkie GD, Austin BJ, Patricelli MP, Cravatt BF.

Proc Natl Acad Sci U S A. 2000 May 9;97(10):5044-9.


Clarifying the catalytic roles of conserved residues in the amidase signature family.

Patricelli MP, Cravatt BF.

J Biol Chem. 2000 Jun 23;275(25):19177-84.


Activity-based protein profiling: the serine hydrolases.

Liu Y, Patricelli MP, Cravatt BF.

Proc Natl Acad Sci U S A. 1999 Dec 21;96(26):14694-9.


Trifluoromethyl ketone inhibitors of fatty acid amide hydrolase: a probe of structural and conformational features contributing to inhibition.

Boger DL, Sato H, Lerner AE, Austin BJ, Patterson JE, Patricelli MP, Cravatt BF.

Bioorg Med Chem Lett. 1999 Jan 18;9(2):265-70.


An endogenous sleep-inducing compound is a novel competitive inhibitor of fatty acid amide hydrolase.

Patricelli MP, Patterson JE, Boger DL, Cravatt BF.

Bioorg Med Chem Lett. 1998 Mar 17;8(6):613-8.


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