News & Publications

Brochures

Press Releases

Publications

KiNativ Method:

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. In situ kinase profiling reveals functionally relevant properties of native kinases. Chem. Biol. 2011 Jun 24;18(6):699-710. PubMed 21700206; PubMed Central PMCID: PMC3142620.

Cravatt BF, Wright AT, Kozarich JW. Activity-Based Protein Profiling: From Enzyme Chemistry to Proteomic Chemistry. Annu. Rev. Biochem. 2008 Mar 26;77:383-414. PubMed 18366325;

Patricelli MP, Szardenings AK, Liyanage M, Nomanbhoy TK, Wu M, Weissig H, Aban A, Chun D, Tanner S, Kozarich JW. Functional Interrogation of the Kinome Using Nucleotide Acyl Phosphates. Biochemistry. 2007 Jan 16;46(2):350-8. PubMed 17209545.

Customer/Collaborator Publications:

KiNativ kinase profiling

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. Kinome-wide selectivity profiling of ATP-competitive mammalian target of rapamycin (mTOR) inhibitors and characterization of their binding kinetics. J Biol Chem. 2012 Mar 23;287(13):9742-52. Epub 2012 Jan 5. PMID: 22223645 [PubMed - indexed for MEDLINE].

Zhang T, Inesta-Vaquera F, Niepel M, Zhang J, Ficarro SB, Machleidt T, Xie T, Marto JA, Kim N, Sim T, Laughlin JD, Park H, LoGrasso PV, Patricelli M, Nomanbhoy TK, Sorger PK, Alessi DR, Gray NS. High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors. Chem Biol. 2012 Jan 27;19(1):140-54. PMID: 22284361 [PubMed - indexed for MEDLINE].

Miduturu CV, Deng X, Kwiatkowski N, Yang W, Brault L, Filippakopoulos P, Chung E, Yang Q, Schwaller J, Knapp S, King RW, Lee JD, Herrgard S, Zarrinkar P, Gray NS. Discovery of potent and selective covalent inhibitors of JNK. Chem Biol. 2011 Jul 29;18(7):868-79. PMID: 21802008 [PubMed - indexed for MEDLINE].

Guo C, McAlpine I, Zhang J, Knighton DD, Kephart S, Johnson MC, Li H, Bouzida D, Yang A, Dong L, Marakovits J, Tikhe J, Richardson P, Guo LC, Kania R, Edwards MP, Kraynov E, Christensen J, Piraino J, Lee J, Dagostino E, Del-Carmen C, Deng YL, Smeal T, Murray BW. Discovery of Pyrroloaminopyrazoles as Novel PAK Inhibitors. J Med Chem. 2012 May 24;55(10):4728-39. Epub 2012 May 14. PMID: 22554206 [PubMed - in process].

Deng X, Dzamko N, Prescott A, Davies P, Liu Q, Yang Q, Lee JD, Patricelli MP, Nomanbhoy TK, Alessi DR, Gray NS. Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2. Nat Chem Biol. 2011 Apr;7(4):203-5. Epub 2011 Mar 6. PubMed 21378983.

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. Reversible inhibitor of p97, DBeQ, impairs both ubiquitin-dependent and autophagic protein clearance pathways. Proc Natl Acad Sci U S A. 2011 Mar 22;108(12):4834-9. Epub 2011 Mar 7. PubMed 21383145; PubMed Central PMCID: PMC3064330.

Yang Q, Deng X, Lu B, Cameron M, Fearns C, Patricelli MP, Yates JR 3rd, Gray NS, Lee JD. Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein. Cancer Cell. 2010 Sep 14;18(3):258-67. Erratum in: Cancer Cell. 2010 Oct 19;18(4):396. PubMed 20832753; PubMed Central PMCID: PMC2939729.

Hydrolase platform

Ahn K, Smith SE, Liimatta MB, Beidler D, Sadagopan N, Dudley DT, Young T, Wren P, Zhang Y, Swaney S, Van Becelaere K, Blankman JL, Nomura DK, Bhattachar SN, Stiff C, Nomanbhoy TK, Weerapana E, Johnson DS, Cravatt BF. Mechanistic and pharmacological characterization of PF-04457845: a highly potent and selective fatty acid amide hydrolase inhibitor that reduces inflammatory and noninflammatory pain. J Pharmacol Exp Ther. 2011 Jul;338(1):114-24. Epub 2011 Apr 19. PubMed 21505060; PubMed Central PMCID: PMC3126636.

Johnson DS, Stiff C, Lazerwith SE, Kesten SR, Fay LK, Morris M, Beidler D, Liimatta MB, Smith SE, Dudley DT, Sadagopan N, Bhattachar SN, Kesten SJ, Nomanbhoy TK, Cravatt BF, Ahn K. Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. ACS Med Chem Lett. 2011 Feb 10;2(2):91-96. PubMed 21666860; PubMed Central PMCID: PMC3109749.

Johnson DS, Ahn K, Kesten S, Lazerwith SE, Song Y, Morris M, Fay L, Gregory T, Stiff C, Dunbar JB Jr, Liimatta M, Beidler D, Smith S, Nomanbhoy TK, Cravatt BF. Benzothiophene piperazine and piperidine urea inhibitors of fatty acid amide hydrolase (FAAH). Bioorg Med Chem Lett. 2009 May 15;19(10):2865-9. Epub 2009 Mar 24. PubMed 19386497; PubMed Central PMCID: PMC3150822.

Ahn K, Johnson DS, Fitzgerald LR, Liimatta M, Arendse A, Stevenson T, Lund ET, Nugent RA, Nomanbhoy TK, Alexander JP, Cravatt BF. Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity. Biochemistry. 2007 Nov 13;46(45):13019-30. Epub 2007 Oct 19. PubMed 17949010.

Other ActivX Activity Based Profiling Publications:

Okerberg ES, Wu J, Zhang B, Samii B, Blackford K, Winn DT, Shreder KR, Burbaum JJ, Patricelli MP. High-resolution functional proteomics by active-site peptide profiling. Proc Natl Acad Sci U S A. 2005 Apr 5;102(14):4996-5001. Epub 2005 Mar 28. PubMed 15795380; PubMed Central PMCID: PMC555687.

Jessani N, Young JA, Diaz SL, Patricelli MP, Varki A, Cravatt BF. Class assignment of sequence-unrelated members of enzyme superfamilies by activity-based protein profiling. Angew Chem Int Ed Engl. 2005 Apr 15;44(16):2400-3. PubMed 15765498.

Adam GC, Burbaum J, Kozarich JW, Patricelli MP, Cravatt BF. Mapping enzyme active sites in complex proteomes. J Am Chem Soc. 2004 Feb 11;126(5):1363-8. PubMed 14759193.

Patricelli MP. Activity-based probes for functional proteomics. Brief Funct Genomic Proteomic. 2002 Jul;1(2):151-8. PubMed 15239901.

Patricelli MP, Giang DK, Stamp LM, Burbaum JJ. Direct visualization of serine hydrolase activities in complex proteomes using fluorescent active site-directed probes. Proteomics. 2001 Sep;1(9):1067-71. PubMed 11990500.

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