Chemical proteomic probes for profiling cytochrome p450 activities and drug interactions in vivo.

Chemical proteomic probes for profiling cytochrome p450 activities and drug interactions in vivo. Research Abstract Details 

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Chemical proteomic probes for profiling cytochrome p450 activities and drug interactions in vivo. Abstract Text:

Aaron T Wright,Benjamin F Cravatt,

The cytochrome P450 (P450) superfamily metabolizes many endogenous signaling molecules and drugs. P450 enzymes are regulated by posttranslational mechanisms in vivo, which hinders their functional characterization by conventional genomic or proteomic methods. Here we describe a chemical proteomic strategy to profile P450 activities directly in living systems. Derivatization of a mechanism-based inhibitor with a "clickable" handle provided an activity-based probe that labels multiple P450s both in proteomic extracts and in vivo. This probe was used to record alterations in liver P450 activities triggered by chemical agents, including inducers of P450 expression and direct P450 inhibitors. The chemical proteomic strategy described herein thus offers a versatile method to monitor P450 activities and small-molecule interactions in any biological system and, through doing so, should facilitate the functional characterization of this large and diverse enzyme class.

Chemical proteomic probes for profiling cytochrome p450 activities and drug interactions in vivo. Publishing Authors By Initials

AT Wright,BF Cravatt,

For similar biological sciences: biochemistry: proteomics research abstracts see: biological sciences: biochemistry: proteomics research

PUBMED ID PMID:

MEDLINE DATE:

Chemical proteomic probes for profiling cytochrome p450 activities and drug interactions in vivo. Journal Published:

PUBLICATION TYPE: Research Support, N.I.H., Extr

Journal: Chemistry & biology

VOLUME: 14

Page Numbers: 1043-51

Journal Abbreviation: Chem. Biol.

ISSN: 1074-5521

DAY: 30

MONTH: Sep

YEAR: 2007

Chemical proteomic probes for profiling cytochrome p450 activities and drug interactions in vivo. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 9500160

Chemical proteomic probes for profiling cytochrome p450 activities and drug interactions in vivo. Keywords Mesh Terms:

KEYWORDS: Proteomics

MESH TERMS: methods

Chemical & Substance for Abstract: Chemical proteomic probes for profiling cytochrome p450 activities and drug interactions in vivo. Information

Substance Name: Cytochrome P-450 Enzyme System

Registry Number: 9035-51-2

Grant and Affiliation Information for Chemical proteomic probes for profiling cytochrome p450 activities and drug interactions in vivo.

AFFILIATION: The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.

Country: England

AGENCY: United States NCI

GRANT: CA087660

ACRONYM: CA

MEDLINETA: Chem Biol

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