Scripps VIVO scripps research logo

  • Index
  • Log in
  • Home
  • People
  • Organizations
  • Research
  • Events
Search form
As of April 1st VIVO Scientific Profiles will no longer updated for faculty, and the link to VIVO will be removed from the library website. Faculty profile pages will continue to be updated via Interfolio. VIVO will continue being used behind the scenes to update graduate student profiles. Please contact helplib@scripps.edu if you have questions.
How to download citations from VIVO | Alternative profile options

Chemical proteomic probes for profiling cytochrome P450 activities and drug interactions in vivo

Academic Article
uri icon
  • Overview
  • Identity
  • Additional Document Info
  • View All
scroll to property group menus

Overview

authors

  • Wright, A. T.
  • Cravatt, Benjamin

publication date

  • September 2007

journal

  • Chemistry & Biology  Journal

abstract

  • 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.

subject areas

  • Animals
  • Cytochrome P-450 Enzyme Inhibitors
  • Cytochrome P-450 Enzyme System
  • Drug Design
  • Drug Interactions
  • Enzyme Inhibitors
  • Humans
  • Mice
  • Molecular Probes
  • Naphthalenes
  • Proteomics
scroll to property group menus

Identity

PubMed Central ID

  • PMC2044501

International Standard Serial Number (ISSN)

  • 1074-5521

Digital Object Identifier (DOI)

  • 10.1016/j.chembiol.2007.08.008

PubMed ID

  • 17884636
scroll to property group menus

Additional Document Info

start page

  • 1043

end page

  • 1051

volume

  • 14

issue

  • 9

©2022 The Scripps Research Institute | Terms of Use | Powered by VIVO

  • About
  • Contact Us
  • Support