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March 25, 2026BioMed Research InternationalOpen Access

Multifaceted Small Molecules as Enzyme Modulators: Cases of Drug Discovery/Repurposing Illustrating Nature′s Pragmatism

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Authors

MKMonika I. KonaklievaBPBalbina J. Plotkin

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Overview

This review explores challenges in enzyme modulation and drug repurposing, highlighting implications for drug design.

Key Points

  • The aim is to examine the challenges and opportunities in designing specific enzyme modulators and repurposing drugs.
  • Review literature on covalent drugs targeting bacterial and mammalian enzymes
  • Analyze the impact of substrate cross-reactivity on enzyme specificity
  • Discuss evolutionary differences between enzymes of various organisms
  • Identified issues related to 'one warhead-one target' design philosophy due to cross-reactivity
  • Found potential in repurposing existing drugs to overcome specificity challenges
  • Emphasized the need for developing covalent reversible drugs to address off-target effects

Cite This Study

Konaklieva et al. (2026) studied this question.

synapsesocial.com/papers/69c37be2b34aaaeb1a67ec82https://doi.org/10.1155/bmri/3429646
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