From thalidomide to rational molecular glue design for targeted protein degradation

V Oleinikovas, P Gainza, T Ryckmans… - Annual Review of …, 2024 - annualreviews.org
Thalidomide and its derivatives are powerful cancer therapeutics that are among the best-
understood molecular glue degraders (MGDs). These drugs selectively reprogram the E3 …

Relapsed/refractory multiple myeloma: A review of available therapies and clinical scenarios encountered in myeloma relapse

P Bhatt, C Kloock, R Comenzo - Current Oncology, 2023 - mdpi.com
Multiple myeloma remains an incurable disease with the usual disease course requiring
induction therapy, autologous stem cell transplantation for eligible patients, and long-term …

Defining molecular glues with a dual-nanobody cannabidiol sensor

S Cao, S Kang, H Mao, J Yao, L Gu, N Zheng - Nature communications, 2022 - nature.com
Abstract “Molecular glue”(MG) is a term coined to describe the mechanism of action of the
plant hormone auxin and subsequently used to characterize synthetic small molecule …

Novel promising benzoxazole/benzothiazole‐derived immunomodulatory agents: Design, synthesis, anticancer evaluation, and in silico ADMET analysis

H Elkady, K El‐Adl, H Sakr… - Archiv der …, 2023 - Wiley Online Library
Eleven novel benzoxazole/benzothiazole‐based thalidomide analogs were designed and
synthesized to obtain new effective antitumor immunomodulatory agents. The synthesized …

Target protein localization and its impact on PROTAC-mediated degradation

LM Simpson, L Glennie, A Brewer, JF Zhao… - Cell Chemical …, 2022 - cell.com
Proteolysis-targeting chimeras (PROTACs) bring a protein of interest (POI) into spatial
proximity of an E3 ubiquitin ligase, promoting POI ubiquitylation and proteasomal …

Hydrogel coatings on universal medical devices with water-responsive Janus adhesion and acidity-triggered transformation for adaptive antibacterial treatment and …

Y Liu, M Li, Y Zheng, C Liu, Y Cao, W Guo, M Liu… - Chemical Engineering …, 2024 - Elsevier
Hydrogel coatings of catheters have attracted extensive attention in the field of medical
devices due to its hydrophilicity and softness, while scarcities of Janus adhesion, adaptive …

Cereblon influences the timing of muscle differentiation in Ciona tadpoles

J Long, A Mariossi, C Cao, Z Mo… - Proceedings of the …, 2023 - National Acad Sciences
Thalidomide has a dark history as a teratogen, but in recent years, its derivates have been
shown to function as potent chemotherapeutic agents. These drugs bind cereblon (CRBN) …

Fragment linker prediction using the deep encoder-decoder network for PROTACs drug design

CT Kao, CT Lin, CL Chou, CC Lin - Journal of chemical …, 2023 - ACS Publications
A drug discovery and development pipeline is a prolonged and complex process that
remains challenging for both computational methods and medicinal chemists and has not …

Wnt/β-catenin signaling pathway in carcinogenesis and cancer therapy

P Song, Z Gao, Y Bao, L Chen, Y Huang, Y Liu… - Journal of Hematology & …, 2024 - Springer
The Wnt/β-catenin signaling pathway plays a crucial role in various physiological processes,
encompassing development, tissue homeostasis, and cell proliferation. Under normal …

The casein kinase 1α agonist pyrvinium attenuates Wnt-mediated CK1α degradation via interaction with the E3 ubiquitin ligase component Cereblon

C Shen, A Nayak, LR Neitzel, F Yang, B Li… - Journal of Biological …, 2022 - ASBMB
The Cullin-RING ligase 4 E3 ubiquitin ligase component Cereblon (CRBN) is a well-
established target for a class of small molecules termed immunomodulatory drugs (IMiDs) …