Literature DB >> 3720956

Why is uncompetitive inhibition so rare? A possible explanation, with implications for the design of drugs and pesticides.

A Cornish-Bowden.   

Abstract

Uncompetitive inhibition is much less common in nature than consideration of enzyme structure and mechanism might lead one to expect. A possible explanation may be that uncompetitive inhibition of an enzyme in a metabolic pathway can have enormously larger effects on the concentrations of metabolic intermediates than competitive inhibition, under circumstances where their effects on the kinetics of the isolated enzyme are very similar. The severely toxic effects that an uncompetitive inhibitor might be expected to have may have caused enzymes to have evolved in such a way that there has been selection against structures that might favour uncompetitive inhibition.

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Year:  1986        PMID: 3720956     DOI: 10.1016/0014-5793(86)81424-7

Source DB:  PubMed          Journal:  FEBS Lett        ISSN: 0014-5793            Impact factor:   4.124


  40 in total

1.  Discovery of a novel inhibitor of NAD(P)(+)-dependent malic enzyme (ME2) by high-throughput screening.

Authors:  Yi Wen; Lei Xu; Fang-lei Chen; Jing Gao; Jing-ya Li; Li-hong Hu; Jia Li
Journal:  Acta Pharmacol Sin       Date:  2014-03-31       Impact factor: 6.150

2.  Eosin B as a novel antimalarial agent for drug-resistant Plasmodium falciparum.

Authors:  Kristen M Massimine; Michael T McIntosh; Lanxuan T Doan; Chloé E Atreya; Stephan Gromer; Worachart Sirawaraporn; David A Elliott; Keith A Joiner; R Heiner Schirmer; Karen S Anderson
Journal:  Antimicrob Agents Chemother       Date:  2006-09       Impact factor: 5.191

3.  Network-based selectivity of antiparasitic inhibitors.

Authors:  Barbara M Bakker; Heike E Assmus; Frank Bruggeman; Jurgen R Haanstra; Edda Klipp; Hans Westerhoff
Journal:  Mol Biol Rep       Date:  2002       Impact factor: 2.316

4.  Solution kinetics measurements suggest HIV-1 protease has two binding sites for darunavir and amprenavir.

Authors:  Andrey Y Kovalevsky; Arun K Ghosh; Irene T Weber
Journal:  J Med Chem       Date:  2008-09-20       Impact factor: 7.446

5.  Hydroxybenzaldoximes Are D-GAP-Competitive Inhibitors of E. coli 1-Deoxy-D-Xylulose-5-Phosphate Synthase.

Authors:  David Bartee; Francine Morris; Amer Al-Khouja; Caren L Freel Meyers
Journal:  Chembiochem       Date:  2015-07-15       Impact factor: 3.164

6.  Target mediated drug disposition with drug-drug interaction, Part II: competitive and uncompetitive cases.

Authors:  Gilbert Koch; William J Jusko; Johannes Schropp
Journal:  J Pharmacokinet Pharmacodyn       Date:  2017-01-10       Impact factor: 2.745

7.  Characteristics necessary for an interconvertible enzyme cascade to generate a highly sensitive response to an effector.

Authors:  M L Cárdenas; A Cornish-Bowden
Journal:  Biochem J       Date:  1989-01-15       Impact factor: 3.857

8.  Identification of Bidentate Salicylic Acid Inhibitors of PTP1B.

Authors:  Sina Haftchenary; Andriana O Jouk; Isabelle Aubry; Andrew M Lewis; Melissa Landry; Daniel P Ball; Andrew E Shouksmith; Catherine V Collins; Michel L Tremblay; Patrick T Gunning
Journal:  ACS Med Chem Lett       Date:  2015-07-22       Impact factor: 4.345

Review 9.  Mechanistic enzymology in drug discovery: a fresh perspective.

Authors:  Geoffrey A Holdgate; Thomas D Meek; Rachel L Grimley
Journal:  Nat Rev Drug Discov       Date:  2017-12-01       Impact factor: 84.694

10.  Isolation and characterization of an anticoagulant present in the salivary glands of the bont-legged tick, Hyalomma truncatum.

Authors:  A M Joubert; J C Crause; A R Gaspar; F C Clarke; A M Spickett; A W Neitz
Journal:  Exp Appl Acarol       Date:  1995-02       Impact factor: 2.132

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