Results 41 to 50 of about 504,547 (295)

Structure-guided design and optimization of small molecules targeting the protein-protein interaction between the von hippel-lindau (VHL) E3 ubiquitin ligase and the hypoxia inducible factor (HIF) alpha subunit with in vitro nanomolar affinities [PDF]

, 2014
E3 ubiquitin ligases are attractive targets in the ubiquitin-proteasome system, however, the development of small-molecule ligands has been rewarded with limited success.
Dias, David M, Carles Galdeano (1305135), Galdeano, Carles, Dias, David M., David M. Dias (1340694), Van Molle, Inge, Gadd, Morgan Stuart, Ciulli, Alessio, Sarah Hewitt (1340700), Soares, Pedro, Galdeano , Carles, Pedro Soares (393566), Gadd, Morgan S., Salvatore Scaffidi (1340703), Inge Van Molle (1284120), Morgan S. Gadd (149371), Scaffidi, Salvatore, Ipek Birced (1340697), Alessio Ciulli (762789), Hewitt, Sarah, Birced, Ipek   +20 more
core   +1 more source

Disruption of the autoinhibited state primes the E3 ligase parkin for activation and catalysis [PDF]

, 2015
The PARK2 gene is mutated in 50% of autosomal recessive juvenile parkinsonism (ARJP) cases. It encodes parkin, an E3 ubiquitin ligase of the RBR family.
R Julio Martinez‐Torres, Shaw, Gary S., Kathryn R Barber, Knebel, Axel, Aguirre, Jacob D., Spratt, Donald E., Axel Knebel, Chaugule, Viduth K., Mercier, Pascal, Viduth K Chaugule, Condos, Tara E. C., Jacob D Aguirre, Pascal Mercier, Barber, Kathryn R., Rachel Toth, Ramasubramanian Sundaramoorthy, Helen Walden, Toth, Rachel, Gary S Shaw, Tara EC Condos, Walden, Helen, Condos, Tara E.C., Martinez-Torres, R. Julio, Donald E Spratt, Kumar, Atul, Sundaramoorthy, Ramasubramanian, Atul Kumar   +26 more
core   +1 more source

Assessing the Direct Binding of Ark-Like E3 RING Ligases to Ubiquitin and Its Implication on Their Protein Interaction Network

Molecules, 2020
The ubiquitin pathway required for most proteins’ targeted degradation involves three classes of enzymes: E1-activating enzyme, E2-conjugating enzyme, and E3-ligases.
Dimitris G. Mintis, Anastasia Chasapi, Konstantinos Poulas, George Lagoumintzis, Christos T. Chasapis   +4 more
doaj   +1 more source

The meaning of ubiquitylation of the DSL ligand Delta for the development of Drosophila

BMC Biology, 2023
Background Ubiquitylation (ubi) of the intracellular domain of the Notch ligand Delta (Dl) by the E3 ligases Neuralized (Neur) and Mindbomb1 (Mib1) on lysines (Ks) is thought to be essential for the its signalling activity.
Tobias Troost, Ekaterina Seib, Alina Airich, Nicole Vüllings, Aleksandar Necakov, Stefano De Renzis, Thomas Klein   +6 more
doaj   +1 more source

A caged E3 ligase ligand for PROTAC-mediated protein degradation with light

Chemical Communications, 2020
Caging of a widely used Von Hippel Lindau E3 ligase ligand for targeted protein degradation with PROTACs allows light-activated proteolysis.
Cyrille S. Kounde, Maria M. Shchepinova, Charlie N. Saunders, Marcel Muelbaier, Mark D. Rackham, John D. Harling, Edward W. Tate   +6 more
openaire   +4 more sources

The molecular basis of CRL4 ubiquitin ligase architecture, targeting and regulation [PDF]

, 2013
Members of the CUL4-RBX1-DDB1 (CRL4) E3 ubiquitin ligase family regulate multiple cellular processes including development, transcription, and DNA repair.
Fischer, Eric Sebastian
core   +1 more source

Structural Diversity of Ubiquitin E3 Ligase

, 2021
The post-translational modification of proteins regulates many biological processes. Their dysfunction relates to diseases. Ubiquitination is one of the post-translational modifications that target lysine residue and regulate many cellular processes ...
29021, Shimizu, Toshiyuki, Toma-Fukai, Sachiko, 29020   +3 more
core   +2 more sources

Phytophthora infestans effector AVR3a is essential for virulence and manipulates plant immunity by stabilizing host E3 ligase CMPG1 [PDF]

, 2010
Fungal and oomycete plant pathogens translocate effector proteins into host cells to establish infection. However, virulence targets and modes of action of their effectors are unknown.
Hein, I., Dixelius, Christina, Hein, I, Hein, Ingo, Bryan, G, Dixelius, C., Kamoun, S., Gilroy, EM, Bos, JIB, Sadanandom, A, Boevink, PC, Gilroy, Eleanor M., Armstrong, MR, Bos, J. I. B., Taylor, RM, Bos, Jorunn I. B., Zhendong, T., Sadanandom, A., Boevink, Petra C., Dixelius, C, Engelhardt, Stefan, Bryan, Glenn, Birch, PRJ, Armstrong, M. R., Engelhardt, S, Hein, Ingo; id_orcid, Harrower, Brian, Kamoun, Sophien, Whisson, Stephen C., Vetukuri, R. R., Birch, Paul R. J.; id_orcid, Bryan, G., Vetukuri, RR, Engelhardt, S., Whisson, S. C., Tian, ZD, Whisson, SC, Boevink, P. C., Bryan, Glenn J., Bos, Jorunn, Gilroy, E. M., Sadanandom, Ari, Birch, Paul R. J., Harrower, B., Harrower, B, Vetukuri, Ramesh R., Birch, P. R. J., Taylor, R. M., Armstrong, Miles R., Taylor, Rosalind M., Zhendong, Tian, Kamoun, S, Tian, Zhendong, Sveriges lantbruksuniversitet., Ramesh, Vetukuri,, Dixelius, Christina,, Harrower, Brian,, Bos, Jorunn I. B.,, Bryan, Glenn,, Hein, Ingo,, Engelhardt, Stefan,, Swedish University of Agricultural Sciences., Boevink, Petra C.,, Vetukuri, Ramesh,, Sadanandom, Ari,, Armstrong, Miles R.,, Gilroy, Eleanor M.,, Whisson, Stephen, Taylor, Rosalind M.,, Zhendong, Tian,, Kamoun, Sophien,, Birch, Paul R. J.,   +71 more
core   +1 more source

The E3 ligase adapter cereblon targets the C-terminal cyclic imide degron

Nature, 2022
The ubiquitin E3 ligase substrate adapter cereblon (CRBN) is a target of thalidomide and lenalidomide 1 , therapeutic agents used in the treatment of haematopoietic malignancies 2 – 4 and as ligands for targeted protein degradation 5 – 7 .
Saki Ichikawa, Hope A. Flaxman, Wen-Qing Xu, N. Vallavoju, Hannah C. Lloyd, Bin-You Wang, Da-Cheng Shen, M. Pratt, Christina M. Woo   +8 more
semanticscholar   +1 more source

Targeted Protein Degradation by Chimeric Compounds using Hydrophobic E3 Ligands and Adamantane Moiety

Pharmaceuticals, 2020
Targeted protein degradation using small chimeric molecules, such as proteolysis-targeting chimeras (PROTACs) and specific and nongenetic inhibitors of apoptosis protein [IAP]-dependent protein erasers (SNIPERs), is a promising technology in drug ...
Takuji Shoda, Nobumichi Ohoka, Genichiro Tsuji, Takuma Fujisato, Hideshi Inoue, Yosuke Demizu, Mikihiko Naito, Masaaki Kurihara   +7 more
doaj   +1 more source