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.

Designing Chimeric Molecules for Drug Discovery by Leveraging Chemical Biology / Borsari, C.; Trader, D. J.; Tait, A.; Costi, M. P.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 63:5(2020), pp. 1908-1928. [10.1021/acs.jmedchem.9b01456]

Designing Chimeric Molecules for Drug Discovery by Leveraging Chemical Biology

Tait A.
Methodology
;
Costi M. P.
Funding Acquisition
2020

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.
2020
19-feb-2020
63
5
1908
1928
Designing Chimeric Molecules for Drug Discovery by Leveraging Chemical Biology / Borsari, C.; Trader, D. J.; Tait, A.; Costi, M. P.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 63:5(2020), pp. 1908-1928. [10.1021/acs.jmedchem.9b01456]
Borsari, C.; Trader, D. J.; Tait, A.; Costi, M. P.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11380/1208961
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