Open Access Medical Books



Edited by Rakesh Sharma .

330 pages .
Open Access .
ISBN 978-953-51-0585-5 .

Enzyme is a protein molecule exhibiting specific activity and binding affinity with its substrate molecule to complete enzyme reaction or biocatalytic reaction. Substrate analogues can inhibit the enzyme reaction and act as enzyme inhibitor. Enzyme inhibition (Enz-ai-m ie-ni-hi-bi-son) means reducing or blocking an enzyme action on specific location of enzyme active site by specific substrate or analogue so called enzyme inhibitor. In modern times, most of the pharmaceutical as well as nutriceutical compounds are marketed as enzyme inhibitors and such inhibitors exhibit their specific action in enzyme inhibition inside cells, bacteria, virus, animal plants and human body. The action of enzyme inhibitors in drug discovery has become a fundamental approach to pharmacology at any pharmaceutical industry, university research lab or drug research center. The present issue has been compiled from various data sources with aim of incorporating a wide range of basic concepts and applied enzyme inhibition evaluation methods in drug discovery. It is aimed at those who are embarking on drug discovery research projects, immobilized enzyme solid state devices as well as relatively experienced pharmacologists, biochemists and pharmacy scientists who might wish to develop their experiments further to the advanced level. While it is not possible to detail and include every possible technique related with enzyme inhibition evaluation in drug design by using specific inhibitors at specific metabolic mechanism(s), the present issue attempts to provide working tips with examples and analysis relevant to a wide range of more commonly available enzyme inhibition techniques.
The methods and concepts described in this book are aimed at giving the reader a glimpse of some existing enzyme inhibition studies and also methods with context of each enzyme inhibition method applied for, as well as providing some basis of familiarizing oneself with these biochemical methods. While enzyme inhibition has been used as major approach in drug design in the research and industry over last two decades, it was only later part of 20th century that it has become a major part of so many applications in biochemical engineering, biomedical engineering of miniatured clinical chemistry devices in microbiological, bacteriological, immunological, hormonal testing, nanotechnology, physiological monitoring in health science, plant science and environment research work. This is, at least in part, due to the continued development of new solid state polymer platform, pure enzymes and specific inhibitors available, better understanding of enzyme inhibition mechanisms and precise detection methods, new awareness of drug discovery and design, with scanning and monitoring accessories. Thanks to the continued joint efforts of governmental, industrial and academic institutions globally to promote the need of new generations of drugs or enzyme inhibitors and new mechanisms of enzyme inhibition. Regardless of the enzymes or drugs and their brands that are used, one should always be able to understand and justify the use of right inhibitor or drug action on enzyme of right choice to drug design for specific study. With this aim, different approaches of enzyme inhibition methods are presented in separate chapters on the use of different enzyme inhibitors. For learners, basic concepts, mechanistic issues, limitations in drug testing, skepticism in enzyme inhibition approach and drug variability due to non-specific analogues of enzyme inhibitors or substrates is presented with a working enzyme inhibition protocols for drug design and analysis of their inhibitory action.....

Rakesh Sharma, Ph.D
Professor (Nanotechnology)
Amity University,

Research Professor, Center of Nano-Biotechnology,
Florida State University, Tallahassee, FL,


Section 1 Basic Concepts of Enzyme Inhibition .

 1 Enzyme Inhibition: Mechanisms and Scope 3 Rakesh Sharma

Section 2 Applications of Enzyme Inhibition .

 2 Cytochrome P450 Enzyme Inhibitors from Nature 39 Simone Badal, Mario Shields and Rupika Delgoda

 3 Pharmacomodulation of Broad Spectrum Matrix Metalloproteinase Inhibitors Towards Regulation of Gelatinases 57 Erika Bourguet, William Hornebeck, Janos Sapi, Alain Jean-Paul Alix and Gautier Moroy

 4 Non-Enzymatic Glycation of Aminotransferases and the Possibilities of Its Modulation 85 Iva Boušová, Lenka Srbová and Jaroslav Dršata

 5 Inhibition of Nitric Oxide Synthase Gene Expression: In vivo Imaging Approaches of Nitric Oxide with Multimodal Imaging 115 Rakesh Sharma

 6 Transcriptional Bursting in the Tryptophan Operon of E. coli and Its Effect on the System Stochastic Dynamics 179 Emanuel Salazar-Cavazos and Moisés Santillán

 7 Mechanisms of Hepatocellular Dysfunction and Regeneration: Enzyme Inhibition by Nitroimidazole and Human Liver Regeneration 195 Rakesh Sharma

 8 Reversible Inhibition of Tyrosine Protein Phosphatases by Redox Reactions 253 Daniela Cosentino-Gomes and José Roberto Meyer-Fernandes

 9 Feasible Novozym 435-Catalyzed Process to Fatty Acid Methyl Ester Production from Waste Frying Oil: Role of Lipase Inhibition 277 Laura Azócar, Gustavo Ciudad, Robinson Muñoz, David Jeison, Claudio Toro and Rodrigo Navia

 10 Urease Inhibition 303 Muhammad Raza Shah and Zahid Hussain Soomro .

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Published by: Unknown - Sunday, June 23, 2013


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