Ligandability of E3 ligases for targeted protein degradation applications

BP Belcher, CC Ward, DK Nomura - Biochemistry, 2021 - ACS Publications
Targeted protein degradation (TPD) using proteolysis targeting chimeras (PROTACs) and
molecular glue degraders has arisen as a powerful therapeutic modality for eliminating …

[HTML][HTML] Targeted protein degrader development for cancer: advances, challenges, and opportunities

Y Fang, S Wang, S Han, Y Zhao, C Yu, H Liu… - Trends in …, 2023 - cell.com
Anticancer-targeted therapies inhibit various kinases implicated in cancer and have been
used in clinical settings for decades. However, many cancer-related targets are proteins …

Development of PDE6D and CK1α degraders through chemical derivatization of FPFT-2216

M Teng, W Lu, KA Donovan, J Sun… - Journal of medicinal …, 2021 - ACS Publications
Immunomodulatory drugs are a class of drugs approved for the treatment of multiple
myeloma. These compounds exert their clinical effects by inducing interactions between the …

Targeting cereblon in hematologic malignancies

O Fuchs - Blood Reviews, 2023 - Elsevier
The protein cereblon (CRBN) is a substrate receptor of the cullin 4-really interesting new
gene (RING) E3 ubiquitin ligase complex CRL4 CRBN. Targeting CRBN mediates selective …

[HTML][HTML] Advances in the potential roles of Cullin-RING ligases in regulating autoimmune diseases

X Zhang, Y Liu, T Zhang, Y Tan, X Dai… - Frontiers in …, 2023 - frontiersin.org
Cullin-RING ligases (CRLs) are the largest class of E3 ubiquitin ligases regulating the
stability and subsequent activity of a large number of important proteins responsible for the …

PROTACs: A novel strategy for cancer drug discovery and development

X Han, Y Sun - MedComm, 2023 - Wiley Online Library
Proteolysis targeting chimera (PROTAC) technology has become a powerful strategy in drug
discovery, especially for undruggable targets/proteins. A typical PROTAC degrader consists …

[PDF][PDF] Pan-cancer analysis reveals the prognostic and immunologic roles of cereblon and its significance for PROTAC design

SH Zhang, N Zeng, JX Sun, CQ Liu, JZ Xu, MY Xu… - Heliyon, 2023 - cell.com
Background Cereblon (CRBN) has emerged as a vital E3 ubiquitin ligase for Proteolysis-
targeting chimera (PROTAC) design. However, few studies focus on the physiological …

Branched ubiquitin code: from basic biology to targeted protein degradation

F Ohtake - The Journal of Biochemistry, 2022 - academic.oup.com
Protein ubiquitylation regulates numerous pathways, and the diverse information encoded
by various forms of ubiquitylation is known as the ubiquitin code. Recent studies revealed …

Protein degraders-from thalidomide to new PROTACs

T Ito - The Journal of Biochemistry, 2024 - academic.oup.com
Recently, the development of protein degraders (protein-degrading compounds) has
prominently progressed. There are two remarkable classes of protein degraders: proteolysis …

Perspectives on Nuclear Magnetic Resonance Spectroscopy in Drug Discovery Research

J Caceres-Cortes, B Falk, L Mueller… - Journal of Medicinal …, 2024 - ACS Publications
The drug discovery landscape has undergone a significant transformation over the past
decade, owing to research endeavors in a wide range of areas leading to strategies for …