Targeted protein degradation: A promise for undruggable proteins
KTG Samarasinghe, CM Crews - Cell chemical biology, 2021 - cell.com
… Targeted Protein Degradation (TPD) strategies have also been explored to target previously
undruggable proteins… of the proteins targeted by PROTACs and the biological effects of their …
undruggable proteins… of the proteins targeted by PROTACs and the biological effects of their …
Targeted protein degradation: mechanisms, strategies and application
L Zhao, J Zhao, K Zhong, A Tong, D Jia - … transduction and targeted …, 2022 - nature.com
… expanding the range of substrates. In this review, we first provide a simple introduction of
protein degradation … , will not only provide powerful tools for biomedical research, but hold great …
protein degradation … , will not only provide powerful tools for biomedical research, but hold great …
Expanding the arsenal of E3 ubiquitin ligases for proximity-induced protein degradation
A Kannt, I Đikić - Cell chemical biology, 2021 - cell.com
… be hijacked for targeted protein degradation—is still … protein degradation and approaches
used to identify or design E3 ligands, and highlight challenges and opportunities for targeting …
used to identify or design E3 ligands, and highlight challenges and opportunities for targeting …
Major advances in targeted protein degradation: PROTACs, LYTACs, and MADTACs
SB Alabi, CM Crews - Journal of Biological Chemistry, 2021 - ASBMB
Of late, targeted protein degradation (TPD) has surfaced as a novel and innovative chemical
tool and therapeutic modality. By co-opting protein degradation pathways, TPD facilitates …
tool and therapeutic modality. By co-opting protein degradation pathways, TPD facilitates …
Prey for the proteasome: targeted protein degradation—a medicinal chemist's perspective
LM Luh, U Scheib, K Juenemann… - Angewandte Chemie …, 2020 - Wiley Online Library
… biology tools as well as therapeutic approaches inducing targeted protein degradation and
… and proteolysis targeting chimeras (PROTACs) paving the way to expand the druggable …
… and proteolysis targeting chimeras (PROTACs) paving the way to expand the druggable …
Advancing targeted protein degradation for cancer therapy
… of the target protein. The broad … that target oncoproteins with tissue, tumour and subcellular
selectivity. In this Review, we first discuss the molecular basis of targeted protein degradation…
selectivity. In this Review, we first discuss the molecular basis of targeted protein degradation…
Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation
… To expand the reach of TPD to degrade other “hard to drug” … synthesis, and molecular
biology, tools now exist to identify ligands for almost any protein. This is underscored by the recent …
biology, tools now exist to identify ligands for almost any protein. This is underscored by the recent …
Discovery of a covalent FEM1B recruiter for targeted protein degradation applications
NJ Henning, AG Manford, JN Spradlin… - Journal of the …, 2022 - ACS Publications
… the degradation of BRD4 and BCR-ABL, respectively. Our study showcases a covalent ligand
that targets … in expanding the arsenal of E3 ligase recruiters suitable for TPD applications. …
that targets … in expanding the arsenal of E3 ligase recruiters suitable for TPD applications. …
Improved Accuracy for Modeling PROTAC-Mediated Ternary Complex Formation and Targeted Protein Degradation via New In Silico Methodologies
ML Drummond, A Henry, H Li… - Journal of Chemical …, 2020 - ACS Publications
… In this current work, we extend upon our initial publication (41… Using these two new methods,
we then extend the test set … Figure 4 do suggest that the modeling tools of this work can …
we then extend the test set … Figure 4 do suggest that the modeling tools of this work can …
PROTAC: an effective targeted protein degradation strategy for cancer therapy
… future to achieve the desired degradation results. In this paper, … degradation strategies for
different target proteins (Table 1). … PROTACs can extend the "target space" to the PPI target. It …
different target proteins (Table 1). … PROTACs can extend the "target space" to the PPI target. It …
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