[HTML][HTML] PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)
M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - … and Targeted Therapy, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …
[HTML][HTML] COVID-19 and cellular senescence
CA Schmitt, T Tchkonia, LJ Niedernhofer… - Nature Reviews …, 2023 - nature.com
The clinical severity of coronavirus disease 2019 (COVID-19) is largely determined by host
factors. Recent advances point to cellular senescence, an ageing-related switch in cellular …
factors. Recent advances point to cellular senescence, an ageing-related switch in cellular …
Proximity-based modalities for biology and medicine
Molecular proximity orchestrates biological function, and blocking existing proximities is an
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …
[HTML][HTML] Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials
Undruggable proteins are a class of proteins that are often characterized by large, complex
structures or functions that are difficult to interfere with using conventional drug design …
structures or functions that are difficult to interfere with using conventional drug design …
[HTML][HTML] Strategies for the discovery of oral PROTAC degraders aimed at cancer therapy
In the past two decades, we have witnessed the discovery and development of many potent
and efficacious proteolysis-targeting chimera (PROTAC) degraders, with several in phase I/II …
and efficacious proteolysis-targeting chimera (PROTAC) degraders, with several in phase I/II …
[HTML][HTML] PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective
Abstract Mouse double minute 2 (MDM2) is an E3 ubiquitin ligase which effectively
degrades tumor suppressor p53. In the past two decades, many MDM2 inhibitors that disrupt …
degrades tumor suppressor p53. In the past two decades, many MDM2 inhibitors that disrupt …
[HTML][HTML] Targeted protein degradation in cancers: Orthodox PROTACs and beyond
Targeted protein degradation (TPD) is emerging as a strategy to overcome the limitations of
traditional small-molecule inhibitors. Proteolysis-targeting chimera (PROTAC) technology …
traditional small-molecule inhibitors. Proteolysis-targeting chimera (PROTAC) technology …
Strategies to Reduce the On‐Target Platelet Toxicity of Bcl‐xL Inhibitors: PROTACs, SNIPERs and Prodrug‐Based Approaches
A Negi, AS Voisin‐Chiret - ChemBioChem, 2022 - Wiley Online Library
Apoptosis is a highly regulated cellular process. Aberration in apoptosis is a common
characteristic of various disorders. Therefore, proteins involved in apoptosis are prime …
characteristic of various disorders. Therefore, proteins involved in apoptosis are prime …
[HTML][HTML] In Silico Computational Studies of Bioactive Secondary Metabolites from Wedelia trilobata against Anti-Apoptotic B-Cell Lymphoma-2 (Bcl-2) Protein …
HG Gowtham, F Ahmed, S Anandan, CS Shivakumara… - Molecules, 2023 - mdpi.com
In the present study, the binding affinity of 52 bioactive secondary metabolites from Wedelia
trilobata towards the anti-apoptotic B-cell lymphoma-2 (Bcl-2) protein (PDB: 2W3L) structure …
trilobata towards the anti-apoptotic B-cell lymphoma-2 (Bcl-2) protein (PDB: 2W3L) structure …