A schematic representation of the enzyme IspD complexed to inhibitor 3, and a seriesof inhibitors 3-5 are shown below.Ala202lle240mwwwNHNHVal263ОНwwwHNN-lle177HN'N'CI3 X = N4 X = C-CN5 X = C-COO IC50 274 µMIC50 140 nMIC50 35 nMNH2HNVal266N-NO-H---- NHN%3DArg157HNwwwwlle265Explain why structure 4 is a more potent inhibitor (lower IC50 value) than inhibitor 3 and whystructure 5 is a much weaker inhibitor (higher IC50 value) than 3 and 4.

IC50 is the total concentration of inhibitor that is required to reach 50% inhibition. This means…

Answered: Explain why structure 4 is a more…

Explain why structure 4 is a more potent inhibitor (lower IC50 value) than inhibitor 3 and why structure 5 is a much weaker inhibitor (higher IC50 value) than 3 and 4.

Biochemistry

9th Edition

ISBN:9781319114671

Author:Lubert Stryer, Jeremy M. Berg, John L. Tymoczko, Gregory J. Gatto Jr.

Publisher:Lubert Stryer, Jeremy M. Berg, John L. Tymoczko, Gregory J. Gatto Jr.

Chapter1: Biochemistry: An Evolving Science

Section: Chapter Questions

Problem 1P

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Concept explainers

Metabolic pathways

Metabolism is defined as the group of life-supporting, enzyme-mediated chemical reactions in organisms. A metabolic pathway is a set of these chemical reactions that involve anabolism (synthesis of complex biomolecules) and catabolism (breakdown of biomolecules into small molecules) that occur inside a cell. Metabolites are the reacting substances, products, and intermediate substances of an enzymatic process that are altered by a series of chemical events catalyzed by enzymes.

Question

A schematic representation of the enzyme IspD complexed to inhibitor 3, and a series
of inhibitors 3-5 are shown below.
Ala202
lle240
mwww
NH
NH
Val263
ОН
www
HN
N-
lle177
HN
'N'
CI
3 X = N
4 X = C-CN
5 X = C-COO IC50 274 µM
IC50 140 nM
IC50 35 nM
NH2
HN
Val266
N
-N
O-H---- N
HN
%3D
Arg157
HN
wwww
lle265
Explain why structure 4 is a more potent inhibitor (lower IC50 value) than inhibitor 3 and why
structure 5 is a much weaker inhibitor (higher IC50 value) than 3 and 4.

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