Molecular glues for targeted protein degradation: from serendipity to rational discovery

G Dong, Y Ding, S He, C Sheng - Journal of medicinal chemistry, 2021 - ACS Publications
Targeted protein degradation is a promising area in the discovery and development of
innovative therapeutics. Molecular glues mediate proximity-induced protein degradation and …

[PDF][PDF] Haven't got a glue: protein surface variation for the design of molecular glue degraders

Z Kozicka, NH Thomä - Cell Chemical Biology, 2021 - cell.com
Molecular glue degraders are small, drug-like compounds that induce interactions between
an E3 ubiquitin ligase and a target, which result in ubiquitination and subsequent …

Semiconducting polymer nanoparticles with surface‐mimicking protein secondary structure as lysosome‐targeting chimaeras for self‐synergistic cancer …

J Qi, S Jia, X Kang, X Wu, Y Hong, K Shan… - Advanced …, 2022 - Wiley Online Library
Immunotherapy has received tremendous attention for tumor treatment, but the efficacy is
greatly hindered by insufficient tumor‐infiltration of immune cells and immunosuppressive …

Supramolecular Self‐Assembly‐Facilitated Aggregation of Tumor‐Specific Transmembrane Receptors for Signaling Activation and Converting Immunologically Cold …

J Li, Y Fang, Y Zhang, H Wang, Z Yang… - Advanced …, 2021 - Wiley Online Library
Supramolecular self‐assembling peptide systems are attracting increasing interest in the
field of cancer theranostics. Additionally, transformation of the immunologically cold tumor …

Identification of potent, selective, and orally bioavailable small-molecule GSPT1/2 degraders from a focused library of cereblon modulators

G Nishiguchi, F Keramatnia, J Min… - Journal of medicinal …, 2021 - ACS Publications
Whereas the PROTAC approach to target protein degradation greatly benefits from rational
design, the discovery of small-molecule degraders relies mostly on phenotypic screening …

PROTAC technology: A new drug design for chemical biology with many challenges in drug discovery

N Guedeney, M Cornu, F Schwalen, C Kieffer… - Drug Discovery …, 2023 - Elsevier
Abstract Target Protein Degradation TPD is a new avenue and revolutionary for therapeutics
because redefining the principles of classical drug discovery and guided by event-based …

[HTML][HTML] The importance of cellular degradation kinetics for understanding mechanisms in targeted protein degradation

KM Riching, EA Caine, M Urh, DL Daniels - Chemical Society Reviews, 2022 - pubs.rsc.org
Targeted protein degradation has exploded over the past several years due to preclinical
and early clinical therapeutic success of numerous compounds, and the emergence of new …

[HTML][HTML] Direct-to-biology, automated, nano-scale synthesis, and phenotypic screening-enabled E3 ligase modulator discovery

Z Wang, S Shaabani, X Gao, YLD Ng… - Nature …, 2023 - nature.com
Thalidomide and its analogs are molecular glues (MGs) that lead to targeted ubiquitination
and degradation of key cancer proteins via the cereblon (CRBN) E3 ligase. Here, we …

[HTML][HTML] Advancing targeted protein degradation for metabolic diseases therapy

QQ Zhou, HT Xiao, F Yang, YD Wang, P Li… - Pharmacological …, 2023 - Elsevier
The development and application of traditional drugs represented by small molecule
chemical drugs and biological agents, especially inhibitors, have become the mainstream …

[PDF][PDF] Enhancer-driven lncRNA BDNF-AS induces endocrine resistance and malignant progression of breast cancer through the RNH1/TRIM21/mTOR cascade

X Lin, X Dinglin, S Cao, S Zheng, C Wu, W Chen, Q Li… - Cell reports, 2020 - cell.com
Epigenomic alterations can give rise to various tumor-promoting properties, including
therapeutic resistance of cancer cells. Here, we identify an lncRNA, BDNF-AS, whose …