Results 81 to 90 of about 5,184,182 (156)

Protein Degradation in Focus

In May 2024, ‘Protein Degradation in Focus’, a special symposium aimed at bringing together scientists in the targeted protein degradation (TPD) field, was held in Dundee, UK.
McAulay, Kirsten; id_orcid, Zollman, David   +1 more
core   +1 more source

Targeted protein degradation: species, diseases and efficient utilization

Journal of Translational Medicine
Background Targeted protein degradation (TPD) is a novel protein modulation strategy distinct from traditional inhibitors. Its core mechanism involves labeling proteins of interest to initiate endogenous protein clearance pathways, mainly including the ...
Tian Yue, Jian He, Jun Hou
doaj   +1 more source

DCAF1-based PROTACs with activity against clinically validated targets overcoming intrinsic- and acquired-degrader resistance

Nature Communications
Targeted protein degradation (TPD) mediates protein level through small molecule induced redirection of E3 ligases to ubiquitinate neo-substrates and mark them for proteasomal degradation. TPD has recently emerged as a key modality in drug discovery.
Martin Schröder, Martin Renatus, Xiaoyou Liang, Fabian Meili, Thomas Zoller, Sandrine Ferrand, Francois Gauter, Xiaoyan Li, Frederic Sigoillot, Scott Gleim, Therese-Marie Stachyra, Jason R. Thomas, Damien Begue, Maryam Khoshouei, Peggy Lefeuvre, Rita Andraos-Rey, BoYee Chung, Renate Ma, Benika Pinch, Andreas Hofmann, Markus Schirle, Niko Schmiedeberg, Patricia Imbach, Delphine Gorses, Keith Calkins, Beatrice Bauer-Probst, Magdalena Maschlej, Matt Niederst, Rob Maher, Martin Henault, John Alford, Erik Ahrne, Luca Tordella, Greg Hollingworth, Nicolas H. Thomä, Anna Vulpetti, Thomas Radimerski, Philipp Holzer, Seth Carbonneau, Claudio R. Thoma   +39 more
doaj   +1 more source

Emerging biologic modalities for targeted protein degradation

Targeted protein degradation (TPD) has emerged as a powerful approach for eliminating disease-associated proteins by harnessing the ubiquitin\u2013proteasome system.
Caldwell, Alana G., Parmar, Harshil, Zhang, Xiaoyu   +2 more
core   +1 more source

Cellular parameters shaping pathways of targeted protein degradation. [PDF]

In recent years the development of proteolysis-targeting chimeras (PROTACs) has enhanced the field of ubiquitin signalling through advancing therapeutic targeted protein degradation (TPD) strategies and generating tools to explore the ubiquitin landscape.

core   +2 more sources

Structural basis of NSD2 degradation via targeted recruitment of SCF-FBXO22

Nature Communications
Targeted protein degradation (TPD) through the ubiquitin-proteasome system is driven by compound-mediated polyubiquitination of a protein-of-interest by an E3 ubiquitin (Ub) ligase.
Kevin C. Robertson, Sascha J. Amann, Tongkun Liu, Adam V. Funk, Xianxi Wang, Irina Grishkovskaya, Aamir Mehmood, John R. Tabor, Jacqueline L. Norris-Drouin, Cheryl H. Arrowsmith, Jon L. Collins, Yinglong Miao, Michael J. Emanuele, David Haselbach, Lindsey I. James, Nicholas G. Brown   +15 more
doaj   +1 more source

HaloPROTAC3 does not trigger the degradation of the halotagged parasitophorous vacuole membrane protein UIS4 during Plasmodium liver stage development

Scientific Reports
Targeted protein degradation (TPD) is a novel strategy for developing therapeutics against pathogens. Prior to causing malaria, Plasmodium parasites replicate within hepatocytes as liver stages, surrounded by a parasitophorous vacuole membrane (PVM).
Melanie Lam, Alexandra Probst, Laura Torres, Ashley A. Lantigua, Matthew E. Fishbaugher, Jyothsna R. Kumar, Manuel Saldivia, Allison Torres, Shreeya Hegde, Maya Aleshnick, Charlie Jennison, Sarah G. H. Roberson, Chester J. Joyner, Ashley M. Vaughan, Brandon K. Wilder, Carole Manneville, Erika L. Flannery, David Marcellin, Beat Nyfeler, Zacharias Thiel, Sebastian A. Mikolajczak, Anke Harupa, Gabriel Mitchell   +22 more
doaj   +1 more source

Drug discovery of Targeted Protein Degradation (TPD)

Proceedings for Annual Meeting of The Japanese Pharmacological Society, 2023
openaire   +1 more source

The cellular fate of mutant rhodopsin: quality control, degradation and aggresome formation [PDF]

, 2002
Mutations in the photopigment rhodopsin are the major cause of autosomal dominant retinitis pigmentosa. The majority of mutations in rhodopsin lead to misfolding of the protein.
Munro, PMG, Cheetham, ME, Saliba, RS, Luthert, PJ   +3 more
core  

Heterobifunctional proteomimetic polymers for targeted degradation of MYC and KRAS

Nature Communications
Targeted protein degradation (TPD) has enabled modulation of previously undruggable proteins. However, existing small-molecule approaches require arduous optimization and are largely confined to targets bearing ligandable pockets.
Max M. Wang, Mihai I. Truica, Brayley S. Gattis, Julia Oktawiec, Vinay Sagar, Ananya A. Basu, Paul A. Bertin, Xiaoyu Zhang, Sarki A. Abdulkadir, Nathan C. Gianneschi   +9 more
doaj   +1 more source