Rapid PROTAC Discovery Platform: Nanomole-Scale Array Synthesis and Direct Screening of Reaction Mixtures-Reference-Cited by-同舟云学术

Rapid PROTAC Discovery Platform: Nanomole-Scale Array Synthesis and Direct Screening of Reaction Mixtures

Published:2023-11-11 Issue:12 Volume:14 Page:1882-1890
ISSN:1948-5875
Container-title:ACS Medicinal Chemistry Letters
language:en
Short-container-title:ACS Med. Chem. Lett.

Author:

Plesniak Mateusz P.¹^ORCID,Taylor Emilia K.¹,Eisele Frederik²,Kourra Christopher M. B. K.³,Michaelides Iacovos N.⁴^ORCID,Oram Alice³,Wernevik Johan²,Valencia Zulma Santisteban²,Rowbottom Hannah²,Mann Nadia²,Fredlund Linda²^ORCID,Pivnytska Valentyna²,Novén Anna²,Pirmoradian Mohammad²,Lundbäck Thomas²^ORCID,Storer R. Ian⁵,Pettersson Mariell¹,De Donatis Gian M.⁶,Rehnström Marie⁷

Affiliation:

1. Medicinal Chemistry, Research and Early Development, Cardiovascular, Renal and Metabolism (CVRM), BioPharmaceuticals R&D, AstraZeneca, Gothenburg 431 83, Sweden

2. Mechanistic & Structural Biology, Discovery Sciences, R&D, AstraZeneca, Gothenburg 431 83, Sweden

3. iLAB, Compound Synthesis & Management, Discovery Sciences, R&D, AstraZeneca, Gothenburg 431 83, Sweden

4. Fragment Based Lead Generation, Hit Discovery, Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 0WG, U.K.

5. Hit Discovery, Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 0WG, U.K.

6. Cellular Assay Development, Discovery Biology, Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 0WG, U.K.

7. Cell Culture Sciences & Banking, Discovery Biology, Discovery Sciences, R&D, AstraZeneca, Gothenburg 431 83, Sweden

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Drug Discovery,Biochemistry

Link

https://pubs.acs.org/doi/pdf/10.1021/acsmedchemlett.3c00314

Reference41 articles.

1. Kenten, J. H.; Roberts, S. F.; Lebowitz, M. S. Controlling Protein Levels in Eukaryotic Organisms Using Novel Compounds Comprising a Ubiquitination Recognition Element and a Protein Binding Element. WO2000047220A1, 2000.

2. Protacs: Chimeric molecules that target proteins to the Skp1-Cullin-F box complex for ubiquitination and degradation

3. Targeted protein degraders crowd into the clinic

4. PROTAC targeted protein degraders: the past is prologue

5. PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)