[HTML][HTML] PROTAC targeted protein degraders: the past is prologue
Targeted protein degradation (TPD) is an emerging therapeutic modality with the potential to
tackle disease-causing proteins that have historically been highly challenging to target with …
tackle disease-causing proteins that have historically been highly challenging to target with …
[HTML][HTML] An expanded lexicon for the ubiquitin code
I Dikic, BA Schulman - Nature Reviews Molecular Cell Biology, 2023 - nature.com
Our understanding of the ubiquitin code has greatly evolved from conventional E1, E2 and
E3 enzymes that modify Lys residues on specific substrates with a single type of ubiquitin …
E3 enzymes that modify Lys residues on specific substrates with a single type of ubiquitin …
Target and tissue selectivity of PROTAC degraders
RG Guenette, SW Yang, J Min, B Pei… - Chemical Society …, 2022 - pubs.rsc.org
Targeted protein degradation (TPD) strategies have revolutionized how scientists tackle
challenging protein targets deemed undruggable with traditional small molecule inhibitors …
challenging protein targets deemed undruggable with traditional small molecule inhibitors …
[HTML][HTML] E3 ubiquitin ligases: styles, structures and functions
Q Yang, J Zhao, D Chen, Y Wang - Molecular biomedicine, 2021 - Springer
E3 ubiquitin ligases are a large family of enzymes that join in a three-enzyme ubiquitination
cascade together with ubiquitin activating enzyme E1 and ubiquitin conjugating enzyme E2 …
cascade together with ubiquitin activating enzyme E1 and ubiquitin conjugating enzyme E2 …
[PDF][PDF] Targeted protein degradation: A promise for undruggable proteins
KTG Samarasinghe, CM Crews - Cell chemical biology, 2021 - cell.com
Summary Protein homeostasis, or" proteostasis," is indispensable for a balanced, healthy
environment within the cell. However, when natural proteostasis mechanisms are …
environment within the cell. However, when natural proteostasis mechanisms are …
[HTML][HTML] Development of a BCL-xL and BCL-2 dual degrader with improved anti-leukemic activity
Abstract PROteolysis-TArgeting Chimeras (PROTACs) have emerged as an innovative drug
development platform. However, most PROTACs have been generated empirically because …
development platform. However, most PROTACs have been generated empirically because …
[HTML][HTML] Expanding PROTACtable genome universe of E3 ligases
Proteolysis-targeting chimera (PROTAC) and other targeted protein degradation (TPD)
molecules that induce degradation by the ubiquitin-proteasome system (UPS) offer new …
molecules that induce degradation by the ubiquitin-proteasome system (UPS) offer new …
The complementarity of DDR, nucleic acids and anti-tumour immunity
Immune checkpoint blockade (ICB) immunotherapy is a first-line treatment for selected
cancers, yet the mechanisms of its efficacy remain incompletely understood. Furthermore …
cancers, yet the mechanisms of its efficacy remain incompletely understood. Furthermore …
E3 ligases and deubiquitinating enzymes regulating the MAPK signaling pathway in cancers
HB Park, KH Baek - Biochimica et Biophysica Acta (BBA)-Reviews on …, 2022 - Elsevier
The mitogen-activated protein kinase (MAPK) signaling pathway is the primary regulatory
module of various cellular processes such as cell proliferation, differentiation, and stress …
module of various cellular processes such as cell proliferation, differentiation, and stress …
Discovery of nanomolar DCAF1 small molecule ligands
ASM Li, S Kimani, B Wilson, M Noureldin… - Journal of Medicinal …, 2023 - ACS Publications
DCAF1 is a substrate receptor of two distinct E3 ligases (CRL4DCAF1 and EDVP), plays a
critical physiological role in protein degradation, and is considered a drug target for various …
critical physiological role in protein degradation, and is considered a drug target for various …