Results 31 to 40 of about 504,547 (295)

BH3‐ligand regulates access of MCL‐1 to its E3 ligase [PDF]

FEBS Letters, 2005
A genome wide search for new BH3‐containing Bcl‐2 family members was conducted using position weight matrices (PWM) and identified a large (480 kDa), novel BH3‐only protein, originally called LASU1 (now also known as Ureb‐1, E3histone, ARF‐BP1, and Mule).
Warr, Matthew R., Acoca, Stephane, Liu, Zhiqian, Germain, Marc, Watson, Mark, Blanchette, Mathieu, Wing, Simon S., Shore, Gordon C.   +7 more
openaire   +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

Expanding the Structural Diversity at the Phenylene Core of Ligands for the von Hippel–Lindau E3 Ubiquitin Ligase: Development of Highly Potent Hypoxia-Inducible Factor-1α Stabilizers

Journal of Medicinal Chemistry, 2023
Hypoxia-inducible factor-1α (HIF-1α) constitutes the principal mediator of cellular adaptation to hypoxia in humans. The HIF-1α protein level and activity are tightly regulated by the ubiquitin E3 ligase von Hippel–Lindau (VHL).
Lan Phuong Vu, Claudia J Diehl, Ryan Casement, A. Bond, C. Steinebach, Nika Strašek, Aleša Bricelj, Andrej Perdih, Gregor Schnakenburg, I. Sosič, A. Ciulli, M. Gütschow   +11 more
semanticscholar   +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, 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.   +14 more
core   +1 more source

Protocol for Biochemical Analysis and Structure Determination of the ZZ Domain of the E3 Ubiquitin Ligase HERC2

STAR Protocols, 2020
Summary: Since its discovery, several ligands of the ZZ domain have been identified; however, molecular and structural information underlying binding of these ligands remains limited.
Jiuyang Liu, Zhaoyu Xue, Kendra R. Vann, Xiaobing Shi, Tatiana G. Kutateladze   +4 more
doaj   +1 more source

SUMO chain-induced dimerization activates RNF4 [PDF]

, 2014
Dimeric RING E3 ligases interact with protein substrates and conformationally restrain the ubiquitin-E2-conjugating enzyme thioester complex such that it is primed for catalysis.
Hay, Ronald T, Rojas-Fernandez, Alejandro, Hattersley, Neil, Plechanovová, Anna, Tatham, Michael H, Jaffray, Ellis   +5 more
core   +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

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

LGR4 and LGR5 form distinct homodimers that only LGR4 complexes with RNF43/ZNRF3 to provide high affinity binding of R-spondin ligands

Scientific Reports, 2023
LGR4 and LGR5 are two homologous receptors that potentiate Wnt/β-catenin signaling in response to R-spondin (RSPO) ligands. The RSPO and LGR4 complex binds to and inhibits activities of two related E3 ubiquitin ligases, RNF43 and ZNRF3, and thus protects
Yukimatsu Toh, Ling Wu, Soohyun Park, Allison Wang, Jianghua Tu, Wangsheng Yu, Mingxin Zuo, Kendra S. Carmon, Qingyun J. Liu   +8 more
doaj   +1 more source

Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands.

Journal of Medicinal Chemistry, 2019
Androgen receptor (AR) is a validated therapeutic target for the treatment of metastatic castration-resistant prostate cancer (mCRPC). We report herein our design, synthesis, and biological characterization of highly potent small-molecule proteolysis ...
Xin-Jun Han, Li-Jie Zhao, Wei-Guo Xiang, Chong Qin, Bukeyan Miao, Tianfeng Xu, Mi Wang, Chao-Yie Yang, Krishnapriya Chinnaswamy, J. Stuckey, Shao-Meng Wang   +10 more
semanticscholar   +1 more source