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Can anyone provide information about pure competitive, non competitive
and
uncompetitive enzyme inhibition equations when an allosteric model is
indicated (Hill equation), in order to obtain Ki? Any published
references?.
Thank you very much,
M'Carmen Gomez
Metabolism & Pharmacokinetics Service
Research & Development Department
IPSEN-PHARMA S.A. Laboratories
Beaufour-Ipsen Group
Ctra. Laurea Miro 395
Sant Feliu de Llobregat, Barcelona, Spain
Telf.: 936858100
e-mail: m-carmen.gomez.-at-.ipsen.com
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A good recent review article on allosteric kinetics can be found at:
Atkins, W. "The impact of cytochrome P450 allosterism on
pharmacokinetics
and drug-drug interactions," **Drug Discovery Today**, Volume 9, Issue
15,
August 2004, Pages 636-637
It is a little light on mathematics, but will direct you to some other
useful references. The full text of the article (and PDF) are
avaialable
free from ScienceDirect.
Best Regards,
Jim Schmidt
Associate Scientist - DMPK
Lexicon Genetics
8800 Technology Forest Place
The Woodlands, TX (USA)
jschmidt.aaa.lexgen.com
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You may contact Dr. Tim Tracy of University of Minnesota
(tracy017.aaa.umn.edu). He's one of the speakers in Short Course 5: Enzyme
Kinetics and Allosterism in Drug Metabolism, ISSX meeting in Providence,
RI.
Jun
[Chapter 13 of Comprehensive Enzyme Kinetics by V. Leskovac ISBN
0-306-46712-7 might also be useful - db]
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