Results 251 to 260 of about 327,531 (416)

Development of C646‐Based Proteolysis Targeting Chimeras Degraders of the Lysine Acetyltransferases CBP and p300

ChemMedChem, EarlyView.
Two PROTAC‐based degraders targeting the cancer‐associated transcriptional co‐activators CBP/p300 weredeveloped. These degraders, combining the CBP/p300 inhibitor C646 with the CRBN ligand thalidomide, reduced CBP/p300 levels in lymphoma cells at low‐micromolar concentration.
Francesco Fiorentino, Filippo Spriano, Daniela Tomaselli, Giorgia Risi, Emanuele Fabbrizi, Valeria Pecci, Simona Nanni, Francesco Bertoni, Dante Rotili, Antonello Mai   +9 more
wiley   +1 more source

SIAH proteins regulate the degradation and intra‐mitochondrial aggregation of PINK1: Implications for mitochondrial pathology in Parkinson's disease

Aging Cell, Volume 21, Issue 12, December 2022., 2022
Our study reports that SIAH3 is increased in PD brains. We also found that SIAH3, along with PINK1, is aggregated in the mitochondria of PD brains. The intra‐mitochondrial aggregation of SIAH3 and PINK1 inactivates PINK1, depolarizes the mitochondria, and leads to neuronal death.
Fatimah Abd Elghani, Hazem Safory, Haya Hamza, Mor Savyon, Malik Farhoud, Michal Toren‐Hershoviz, Zagorka Vitic, Kirsten Ebanks, Vered Shani, Sleman Bisharat, Lihi Shaulov, Claude Brodski, Zhiyin Song, Rina Bandopadhyay, Simone Engelender   +14 more
wiley   +1 more source

Membrane Topology and Function of Der3/Hrd1p as a Ubiquitin-Protein Ligase (E3) Involved in Endoplasmic Reticulum Degradation [PDF]

, 2001
Péter Deák, Dieter H. Wolf
openalex   +1 more source

Replacing a Cereblon Ligand by a DDB1 and CUL4 Associated Factor 11 (DCAF11) Recruiter Converts a Selective Histone Deacetylase 6 PROTAC into a Pan‐Degrader

ChemMedChem, EarlyView.
This study introduced DCAF11 as an E3 ligase for PROTAC‐mediated histone deacetylase (HDAC) degradation. By replacing cereblon with DCAF11 as recruited E3 ligase, a selective HDAC6 degrader (A6) was transformed into pan‐HDAC degraders. The lead compound, 1j (FF2039), potently degraded HDACs from classes I, IIa, and IIb, showing strong antiproliferative
Felix Feller, Heiko Weber, Martina Miranda, Irina Honin, Maria Hanl, Finn K. Hansen   +5 more
wiley   +1 more source

Beyond destruction: emerging roles of the E3 ubiquitin ligase Hakai. [PDF]

Cell Mol Biol Lett
Escuder-Rodríguez JJ, Rodríguez-Alonso A, Jove L, Quiroga M, Alfonsín G, Figueroa A.   +5 more
europepmc   +1 more source

The autism-linked UBE3A T485A mutant E3 ubiquitin ligase activates the Wnt/β-catenin pathway by inhibiting the proteasome [PDF]

, 2017
Choudhury, Rajarshi, Emanuele, Michael J., Fragola, Giulia, Major, Michael B., Paranjape, Smita R., Walker, Matthew P., Wolter, Justin M., Yi, Jason J., Zylka, Mark J.   +8 more
core   +2 more sources

Nonperiodic Activity of the Human Anaphase-Promoting Complex–Cdh1 Ubiquitin Ligase Results in Continuous DNA Synthesis Uncoupled from Mitosis

, 2000
Claus Storgaard Sørensen, Claudia Lukas, Edgar R. Kramer, Jan‐Michael Peters, Jiří Bártek, Jiří Lukáš   +5 more
openalex   +1 more source

Neuralized functions as an E3 ubiquitin ligase during Drosophila development [PDF]

, 2001
Edward T.H. Yeh, Matt Dermer, Cosimo Commisso, Lily Zhou, C. Jane McGlade, Gabrielle L. Boulianne   +5 more
openalex   +1 more source

Beyond Docking: A Multi‐Tier Computational Pipeline for USP7 Inhibitor Optimization

ChemMedChem, Accepted Article.
Ubiquitin‐specific protease 7 (USP7) is a key deubiquitinating enzyme involved in tumor suppression, DNA repair, and epigenetic regulation. Given its critical role in cancer progression, USP7 has emerged as an attractive therapeutic target. In this study, we employed a multi‐tier computational approach, integrating ligand‐based virtual screening ...
Serdar Durdagi, Ehsan Sayyah, Muhammet Eren Ulug, Serdar Durdağı   +3 more
wiley   +1 more source

Ubiquitin Ligase Gene <i>OsPUB57</i> Negatively Regulates Rice Blast Resistance. [PDF]

Plants (Basel)
Zhang J, Du Q, Wu Y, Shen M, Gao F, Wang Z, Xiao X, Tang W, Chen Q.   +8 more
europepmc   +1 more source