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Biased and unbiased strategies to identify biologically active small molecules.

Abstract：

:Small molecules are central players in chemical biology studies. They promote the perturbation of cellular processes underlying diseases and enable the identification of biological targets that can be validated for therapeutic intervention. Small molecules have been shown to accurately tune a single function of pluripotent proteins in a reversible manner with exceptional temporal resolution. The identification of molecular probes and drugs remains a worthy challenge that can be addressed by the use of biased and unbiased strategies. Hypothesis-driven methodologies employs a known biological target to synthesize complementary hits while discovery-driven strategies offer the additional means of identifying previously unanticipated biological targets. This review article provides a general overview of recent synthetic frameworks that gave rise to an impressive arsenal of biologically active small molecules with unprecedented cellular mechanisms.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Abet V,Mariani A,Truscott FR,Britton S,Rodriguez R

doi

10.1016/j.bmc.2014.04.019

subject

Has Abstract

pub_date

2014-08-15 00:00:00

pages

4474-89

issue

16

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(14)00273-9

journal_volume

22

pub_type

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