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Title:
PROBE FOR SELECTIVELY CHARACTERIZING ENZYMES INVOLVED IN XENOBIOTIC METABOLISM AND METHOD OF MAKING AND USING THE SAME
Document Type and Number:
WIPO Patent Application WO/2019/069297
Kind Code:
A3
Abstract:
Activity-based probes that can be used to selectively identify and characterize enzymes that are involved in different phases of xenobiotic metabolism in a host and its microbiota population(s) are described. The activity-based probes described specifically label only their target active enzymes involved in xenobiotic metabolism and therefore provide a measurement of true protein functional activity rather than transcript or protein abundance. The activity-based probes also provide multimodal profiling of these active enzymes. Methods for preparing the activity based probes and exemplary methods for their use also are disclosed.

Inventors:
WRIGHT AARON T (US)
RAMOS-HUNTER SUSAN (US)
WHIDBEY CHRISTOPHER (US)
Application Number:
PCT/IB2018/059536
Publication Date:
June 13, 2019
Filing Date:
November 30, 2018
Export Citation:
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Assignee:
WRIGHT AARON T (US)
RAMOS HUNTER SUSAN (US)
WHIDBEY CHRISTOPHER (US)
KILLINGER BYRAN J (US)
NAIR REJI N (US)
STODDARD ETHAN G (US)
International Classes:
G01N33/573; C07D203/26; C07D311/26; C07H15/22; C07H17/075; C07H19/06; G01N33/58
Domestic Patent References:
WO2004033397A22004-04-22
WO2001077684A22001-10-18
Foreign References:
US7736911B22010-06-15
Other References:
WU, L. ET AL.: "Activity-based probes for functional interrogation of retaining beta-glucuronidases", NAT. CHEM. BIOL., vol. 13, no. 8, 5 June 2017 (2017-06-05), pages 867 - 873, XP55614368
VERHELST, S. H.L.: "Probing Functional Tyrosines", CHEMISTRY & BIOLOGY, vol. 20, 2013, pages 457 - 458, XP55614370
STODDARD, E. G. ET AL.: "Activity-based probes for isoenzyme- and site-specific functional characterization of glutathione S-transferases", J. AM. CHEM. SOC., vol. 139, 25 October 2017 (2017-10-25), pages 16032 - 16035, XP55614374
Attorney, Agent or Firm:
SCHWARTZ, Johanna P. (US)
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