What question did this study set out to answer?

To provide an updated overview of emerging and re-emerging reactive functional groups (warheads) used in targeted covalent inhibitors and their applications across medicinal chemistry and chemical biology.

May 7, 2024Journal of Medicinal ChemistryOpen Access

Emerging and Re-emerging Warheads for Targeted Covalent Inhibitors: An Update

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Authors

LHLaura HillebrandGlobal Development Network XLXiaojun Julia LiangAcoustics Research Institute RSRicardo A. M. SerafimInstitut Químic de Sarrià

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Implication

Review demonstrates advances in covalent warhead chemistries for drug discovery, highlighting expanded targeting capabilities beyond traditional residues.

Key Points

To provide an updated overview of emerging and re-emerging reactive functional groups (warheads) used in targeted covalent inhibitors and their applications across medicinal chemistry and chemical biology.
Literature review tracking recent developments in covalent inhibitor design and warhead chemistry since 2019.
Documents recent clinical approvals and expanding medicinal applications of targeted covalent drugs.
Summarizes novel electrophilic warheads designed to selectively engage cysteine alongside non-cysteine amino acid residues with reversible or irreversible binding mechanisms.

Cite This Study

Hillebrand et al. (2024) studied this question.

synapsesocial.com/papers/69dabac1a6045d71bfa3df78 https://doi.org/10.1021/acs.jmedchem.3c01825

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Implication

Review demonstrates advances in covalent warhead chemistries for drug discovery, highlighting expanded targeting capabilities beyond traditional residues.

Emerging and Re-emerging Warheads for Targeted Covalent Inhibitors: An Update

Discussion

Member takes

Implication

Key Points

Cite This Study

Emerging and Re-emerging Warheads for Targeted Covalent Inhibitors: An Update

Discussion

Member takes

Implication

Key Points

Cite This Study

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