Review

Advances in AR-targeting chimeras: a case study of proteolysis-targeting chimeras from bench to bedside

Wu Du

*Author for correspondence:

Department of Medicinal Chemistry, Hinova Pharmaceuticals Inc., 5 Keyuan South Road, Rongyao Building Unit A 4th Floor, Chengdu, Sichuan, 610041, People's Republic of China

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Published Online:10 Oct 2022https://doi.org/10.4155/fmc-2022-0147

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Abstract

Proteolysis-targeting chimera (PROTAC) is an emerging revolutionary technology that promotes degradation of target proteins by proteolysis. AR-targeting PROTACs marked many milestones in the history of PROTAC development. In this review, the author discusses the development of AR-targeting PROTACs over the last two decades. Also included in this focused review are medicinal chemistry strategies, pharmacokinetic profiles and clinical development. Taking AR targeting PROTACs for case study, this review provides a target specific overview of how PROTAC technology has advanced from a revolutionary concept and achieved proof of concept leading to drug candidates that benefit patients.

Keywords:

Papers of special note have been highlighted as: • of interest

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Vol. 14, No. 20

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Received 24 June 2022

Accepted 28 August 2022

Published online 10 October 2022

Published in print October 2022

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Acknowledgements

The author wishes to thank X Li, J Li, F Perabo, I King and Y Chen for their suggestions to this manuscript.

Supplementary data

To view the supplementary data that accompany this paper please visit the journal website at: www.future-science.com/doi/suppl/10.4155/fmc-2022-0147

Financial & competing interests disclosure

The author is an employee of Hinova Pharmaceuticals Inc., who has an AR PROTAC compound HP518 in clinical development. The author has no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.

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