Molecular glues for targeted protein degradation: from serendipity to rational discovery
Targeted protein degradation is a promising area in the discovery and development of
innovative therapeutics. Molecular glues mediate proximity-induced protein degradation and …
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
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 …
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 …
Immunotherapy has received tremendous attention for tumor treatment, but the efficacy is
greatly hindered by insufficient tumor‐infiltration of immune cells and immunosuppressive …
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 …
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 …
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 …
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
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 …
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
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 …
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 …
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 …
therapeutic resistance of cancer cells. Here, we identify an lncRNA, BDNF-AS, whose …