Recent Advances in Developing Targeted Protein Degraders

B Cheng, H Li, X Peng, J Chen, C Shao… - European Journal of …, 2024 - Elsevier
Targeted protein degradation (TPD) represents a promising therapeutic approach,
encompassing several innovative strategies, including but not limited to proteolysis targeting …

Interleukin-1 Receptor-Associated Kinase 4 (IRAK4) Degraders for Treating Inflammatory Diseases: Advances and Prospects

Y Lin, L Zheng, Y Xu, X Wang, J Li… - Journal of Medicinal …, 2025 - ACS Publications
Interleukin-1 receptor-associated kinase 4 (IRAK4) is involved in various inflammation-
related diseases. Both the kinase and scaffolding functions of IRAK4 initiate pro …

Design and synthesis of novel Cereblon binders for use in targeted protein degradation

S Norris, X Ba, J Rhodes, D Huang… - Journal of Medicinal …, 2023 - ACS Publications
Modulating the chemical composition of cereblon (CRBN) binders is a critical step in the
optimization process of protein degraders that seek to hijack the function of this E3 ligase …

Property-based optimisation of PROTACs

JS Scott, IN Michaelides, M Schade - RSC Medicinal Chemistry, 2025 - pubs.rsc.org
PROTACs are an emerging therapeutic approach towards targeted protein degradation.
This article examines the leading examples of this modality that are in clinical development …

Discovery of an Azabicyclo [2.1. 1] hexane Piperazinium Salt and Its Application in Medicinal Chemistry via a Rearrangement

C He, X Ba, HP Shunatona, JT Edwards, YX Li… - Organic …, 2024 - ACS Publications
Herein we report the discovery of an azabicyclo [2.1. 1] hexane piperazinium
methanesulfonate salt from an unexpected rearrangement reaction in the preparation of …

Unleashing the Power of Covalent Drugs for Protein Degradation

MJ Fu, H Jin, SP Wang, L Shen, HM Liu… - Medicinal Research …, 2025 - Wiley Online Library
Targeted protein degradation (TPD) has emerged as a significant therapeutic approach for a
variety of diseases, including cancer. Advances in TPD techniques, such as molecular glue …

Evaluation of Cereblon-Directing Warheads for the Development of Orally Bioavailable PROTACs

M Actis, J Cresser-Brown, EA Caine… - Journal of Medicinal …, 2025 - ACS Publications
PROTACs usually occupy physicochemical space outside the one defined by classical drug-
like molecules, which often presents considerable challenges in their optimization and …

Discovery of the First Clinical Protein Degrader for the Treatment of Autoimmune Indications: Orally Bioavailable and Selective IRAK4 Degrader KT-474

SD Edmondson - Journal of Medicinal Chemistry, 2024 - ACS Publications
IRAK4 inhibitors have been sought for the treatment of a host of diseases, however, recent
evidence suggests a protein degradation approach might have advantages over an …

Development of a Buchwald–Hartwig Amination for an Accelerated Library Synthesis of Cereblon Binders

A Lejava, GA Miseo, T Phan, J Zhu… - ACS Medicinal …, 2024 - ACS Publications
In recent years, targeted protein degradation (TPD) has emerged as a powerful therapeutic
modality utilizing both heterobifunctional ligand-directed degraders (LDDs) and molecular …

[引用][C] HETEROBIFUNCTIONAL DEGRADERS OF IRAK4 FOR AUTOIMMUNE INDICATIONS

MM Weiss - 2024 Medicinal Chemistry Reviews, 2024 - ACS Publications