[HTML][HTML] Proteomic approaches advancing targeted protein degradation
G Sathe, GP Sapkota - Trends in pharmacological sciences, 2023 - cell.com
Targeted protein degradation (TPD) is an emerging modality for research and therapeutics.
Most TPD approaches harness cellular ubiquitin-dependent proteolytic pathways …
Most TPD approaches harness cellular ubiquitin-dependent proteolytic pathways …
[HTML][HTML] Breaking Bad Proteins—Discovery Approaches and the Road to Clinic for Degraders
Proteolysis-targeting chimeras (PROTACs) describe compounds that bind to and induce
degradation of a target by simultaneously binding to a ubiquitin ligase. More generally …
degradation of a target by simultaneously binding to a ubiquitin ligase. More generally …
Targeting a lineage-specific PI3Kɣ–Akt signaling module in acute myeloid leukemia using a heterobifunctional degrader molecule
LM Kelly, JC Rutter, KH Lin, F Ling, M Duchmann… - Nature Cancer, 2024 - nature.com
Dose-limiting toxicity poses a major limitation to the clinical utility of targeted cancer
therapies, often arising from target engagement in nonmalignant tissues. This obstacle can …
therapies, often arising from target engagement in nonmalignant tissues. This obstacle can …
Kinetic modeling of PROTAC‐induced protein degradation
Kinetics of the PROTAC‐induced protein degradation were modelled using the equilibrium
approximation, accounting for the protein recovery rate with a time lag. The simulated kinetic …
approximation, accounting for the protein recovery rate with a time lag. The simulated kinetic …
Discovery of Novel Potent and Fast BTK PROTACs for the Treatment of Osteoclasts-Related Inflammatory Diseases
J Huang, Z Ma, X Peng, Z Yang, Y Wu… - Journal of Medicinal …, 2024 - ACS Publications
Bruton's tyrosine kinase (BTK) is an attractive target in inflammatory and autoimmune
diseases. However, the effectiveness of BTK inhibitors is limited by side effects and drug …
diseases. However, the effectiveness of BTK inhibitors is limited by side effects and drug …
PROTACable is an Integrative Computational Pipeline of 3-D Modeling and Deep Learning to Automate the De Novo Design of PROTACs
Proteolysis-targeting chimeras (PROTACs) that engage two biological targets at once are a
promising technology in degrading clinically relevant protein targets. Since factors that …
promising technology in degrading clinically relevant protein targets. Since factors that …
PEG: the magic bullet for biophysical analysis of highly aggregating small molecules in aqueous solutions
J Ingersoll, AA Shcherbakov, A Vaish… - ACS Medicinal …, 2023 - ACS Publications
Biophysical research plays a crucial role in drug discovery, but many druglike molecules are
poorly soluble and prone to aggregation, making their analysis challenging and susceptible …
poorly soluble and prone to aggregation, making their analysis challenging and susceptible …
[HTML][HTML] Molecular glues for protein-protein interactions: Progressing toward a new dream
M Konstantinidou, MR Arkin - Cell Chemical Biology, 2024 - cell.com
The modulation of protein-protein interactions with small molecules is one of the most
rapidly developing areas in drug discovery. In this review, we discuss advances over the …
rapidly developing areas in drug discovery. In this review, we discuss advances over the …
Mechanism of degrader-targeted protein ubiquitinability
Small molecule degraders of disease-driving proteins offer a clinically proven modality with
enhanced therapeutic efficacy and the potential to tackle previously undrugged targets …
enhanced therapeutic efficacy and the potential to tackle previously undrugged targets …
Current strategic trends in drug discovery: the present as prologue
DR Janero - Expert Opinion on Drug Discovery, 2024 - Taylor & Francis
Introduction Escalating costs and inherent uncertainties associated with drug discovery
invite initiatives to improve its efficiency and de-risk campaigns for inventing better …
invite initiatives to improve its efficiency and de-risk campaigns for inventing better …