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Designing Chimeric Molecules for Drug Discovery by Leveraging Chemical Biology.

ABSTRACT: After the first seed concept introduced in the 18th century, different disciplines have attributed different names to dual-functional molecules depending on their application, including bioconjugates, bifunctional compounds, multitargeting molecules, chimeras, hybrids, engineered compounds. However, these engineered constructs share a general structure: a first component that targets a specific cell and a second component that exerts the pharmacological activity. A stable or cleavable linker connects the two modules of a chimera. Herein, we discuss the recent advances in the rapidly expanding field of chimeric molecules leveraging chemical biology concepts. This Perspective is focused on bifunctional compounds in which one component is a lead compound or a drug. In detail, we discuss chemical features of chimeric molecules and their use for targeted delivery and for target engagement studies.

SUBMITTER: Borsari C

PROVIDER: S-EPMC7997565 | biostudies-literature | 2020 Mar

REPOSITORIES: biostudies-literature

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Designing Chimeric Molecules for Drug Discovery by Leveraging Chemical Biology.

Borsari Chiara C Trader Darci J DJ Tait Annalisa A Costi Maria P MP

Journal of medicinal chemistry 20200219 5

After the first seed concept introduced in the 18th century, different disciplines have attributed different names to dual-functional molecules depending on their application, including bioconjugates, bifunctional compounds, multitargeting molecules, chimeras, hybrids, engineered compounds. However, these engineered constructs share a general structure: a first component that targets a specific cell and a second component that exerts the pharmacological activity. A stable or cleavable linker con ...[more]

PMID: 32023055

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