Results 11 to 20 of about 194,539 (300)

IAPs as E3 ligases of Rac1 [PDF]

Small GTPases, 2012
Inhibitors of Apoptosis Proteins (IAPs) are well-studied E3 ubiquitin ligases predominantly known for regulation of apoptosis. We uncovered that IAPs can function as a direct E3 ubiquitin ligase of RhoGTPase Rac1. cIAP1 and XIAP directly conjugate polyubiquitin chains to Lysine 147 of activated Rac1 and target it for proteasomal degradation ...
Oberoi-Khanuja, Tripat Kaur, Rajalingam, Krishnaraj   +1 more
openaire   +5 more sources

Pharmacophore-based ML model to filter candidate E3 ligands and predict E3 Ligase binding probabilities

Informatics in Medicine Unlocked
Among the plethora of E3 Ligases, only a few have been utilized for the novel PROTAC technology. However, extensive knowledge of the preparation of E3 ligands and their utilization for PROTACs is already present in several databases.
Reagon Karki, Yojana Gadiya, Simran Shetty, Philip Gribbon, Andrea Zaliani   +4 more
doaj   +2 more sources

Pharmacophore-based ML model to predict ligand selectivity for E3 ligase binders [PDF]

, 2023
E3 ligases are enzymes that play a critical role in ubiquitin-mediated protein degradation and are involved in various cellular processes. Pharmacophore analysis is a useful approach for predicting E3 ligase binding selectivity, which involves ...
Andrea, Zaliani, Reagon, Karki, Philip , Gribbon, Yojana, Gadiya   +3 more
core   +2 more sources

MDM2 E3 ligase activity is essential for p53 regulation and cell cycle integrity.

PLoS Genetics, 2022
MDM2 and MDM4 are key regulators of p53 and function as oncogenes when aberrantly expressed. MDM2 and MDM4 partner to suppress p53 transcriptional transactivation and polyubiquitinate p53 for degradation.
Meenalakshmi Chinnam, Chao Xu, Rati Lama, Xiaojing Zhang, Carlos D Cedeno, Yanqing Wang, Aimee B Stablewski, David W Goodrich, Xinjiang Wang   +8 more
doaj   +1 more source

Discovery of E3 Ligase Ligands for Target Protein Degradation

Molecules, 2022
Target protein degradation has emerged as a promising strategy for the discovery of novel therapeutics during the last decade. Proteolysis-targeting chimera (PROTAC) harnesses a cellular ubiquitin-dependent proteolysis system for the efficient ...
Jaeseok Lee, Youngjun Lee, Young Mee Jung, Ju Hyun Park, Hyuk Sang Yoo, Jongmin Park   +5 more
doaj   +1 more source

A Comprehensive Atlas of E3 Ubiquitin Ligase Mutations in Neurological Disorders

Frontiers in Genetics, 2018
Protein ubiquitination is a posttranslational modification that plays an integral part in mediating diverse cellular functions. The process of protein ubiquitination requires an enzymatic cascade that consists of a ubiquitin activating enzyme (E1 ...
Arlene J. George, Yarely C. Hoffiz, Antoinette J. Charles, Ying Zhu, Angela M. Mabb   +4 more
doaj   +1 more source

Erioflorin stabilizes the tumor suppressor Pdcd4 by inhibiting its interaction with the E3-ligase β-TrCP1 [PDF]

, 2012
Loss of the tumor suppressor Pdcd4 was reported for various tumor entities and proposed as a prognostic marker in tumorigenesis. We previously characterized decreased Pdcd4 protein stability in response to mitogenic stimuli, which resulted from p70S6K1 ...
Bernhard Brüne, Milke, Larissa, Kathrin Schulz, Larissa Milke, Heidi R Bokesch, Schulz, Kathrin, Colburn, Nancy H., Blees, Johanna, Schmid, Tobias, Curtis J. Henrich (131182), Tobias Schmid, Kathrin Schulz (131170), Magdalena M. Bajer (131176), Heidi R. Bokesch (131163), Bajer, Magdalena M., Daniela Rübsamen (131166), Johanna S Blees, Henrich, Curtis J., Nancy H. Colburn (131186), James B McMahon, Magdalena M Bajer, James B. McMahon (7677), McMahon, James B., Daniela Rübsamen, Kirk R. Gustafson (131179), Tobias Schmid (131190), Nancy H Colburn, Brüne, Bernhard, Kirk R Gustafson, Rübsamen, Daniela, Bernhard Brüne (131193), Curtis J Henrich, Bokesch, Heidi R., Gustafson, Kirk R., Larissa Milke (131173), Johanna S. Blees (131161)   +35 more
core   +1 more source

BRCA1 is a histone-H2A-specific ubiquitin ligase [PDF]

, 2014
The RING domain proteins BRCA1 and BARD1 comprise a heterodimeric ubiquitin (E3) ligase that is required for the accumulation of ubiquitin conjugates at sites of DNA damage and for silencing at DNA satellite repeat regions. Despite its links to chromatin,
Donna L. Mallery, Mallery, D., Conor Larkin, Huang, Jeffrey T.J., Kalb, R., Kevin Hiom, Kalb, Reinhard, Reinhard Kalb, Huang, Jeffrey T. J.; id_orcid, Hiom, Kevin, Hiom, K., Jeffrey T.J. Huang, Larkin, C., Mallery, Donna L., Larkin, Conor, Huang, J.   +15 more
core   +1 more source

Structure of the Human FANCL RING-Ube2T Complex Reveals Determinants of Cognate E3-E2 Selection [PDF]

, 2014
The combination of an E2 ubiquitin-conjugating enzyme with an E3 ubiquitin-ligase is essential for ubiquitin modification of a substrate. Moreover, the pairing dictates both the substrate choice and the modification type. The molecular details of generic
Miles, Jennifer Anne, Hodson, Charlotte, Purkiss, Andrew, Walden, Helen   +3 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