Results 51 to 60 of about 13,195 (282)

Advances in targeted degradation of endogenous proteins [PDF]

, 2019
Protein silencing is often employed as a means to aid investigations in protein function and is increasingly desired as a therapeutic approach. Several types of protein silencing methodologies have been developed, including targeting the encoding genes ...
Fulcher, Luke, Roth, Sascha, Sapkota, Gopal   +2 more
core   +2 more sources

Proteolysis‐targeting chimeras in drug development: A safety perspective [PDF]

British Journal of Pharmacology, 2020
Proteolysis‐targeting chimeras are a new drug modality that exploits the endogenous ubiquitin proteasome system to degrade a protein of interest for therapeutic benefit. As the first‐generation of proteolysis‐targeting chimeras have now entered clinical trials for oncology indications, it is timely to consider the theoretical safety risks inherent with
Kevin Moreau, Muireann Coen, Andrew X. Zhang, Fiona Pachl, M. Paola Castaldi, Goran Dahl, Helen Boyd, Clay Scott, Pete Newham   +8 more
openaire   +3 more sources

Coassembly of Mgm1 isoforms requires cardiolipin and mediates mitochondrial inner membrane fusion [PDF]

, 2009
Two dynamin-related protein (DRP) families are essential for fusion of the outer and inner mitochondrial membranes, Fzo1 (yeast)/Mfn1/Mfn2 (mammals) and Mgm1 (yeast)/Opa1 (mammals), respectively.
Rachel M. DeVay, Lenin Dominguez-Ramirez, Laura L. Lackner, Suzanne Hoppins, Henning Stahlberg, Jodi Nunnari, Cipolat, Crowther, Danino, Daum, Duvezin-Caubet, Esser, Frezza, Gasper, Gipson, Gipson, Gray, Griffin, Griparic, Herlan, Herlan, Hermann, Hoppins, Hoppins, Ingerman, Ishihara, Ishihara, Koshiba, Lassmann, Lévy, Longtine, Low, Martí-Renom, McGuffin, McQuibban, Meeusen, Meeusen, Meglei, Naylor, Pettersen, Quan, Ramachandran, Rapaport, Siegel, Sesaki, Song, Sperka-Gottlieb, Tovchigrechko, Wong, Zick, Zinser   +50 more
core   +2 more sources

Proteolysis of HCF-1 by Ser/Thr glycosylation-incompetent O-GlcNAc transferase:UDP-GlcNAc complexes [PDF]

, 2016
In complex with the cosubstrate UDP-N-acetylglucosamine (UDP-GlcNAc),O-linked-GlcNAc transferase (OGT) catalyzes Ser/ThrO-GlcNAcylation of many cellular proteins and proteolysis of the transcriptional coregulator HCF-1.
Bhuiyan, Tanja, Borodkin, Vladimir S., Herr, Winship, Kapuria, Vaibhav, Röhrig, Ute F., van Aalten, Daan M F, Zoete, Vincent   +6 more
core   +3 more sources

Matrix metalloproteinases at key junctions in the pathomechanism of stroke [PDF]

, 2011
Matrix metalloproteinases play a crucial role in the remodelling of the extracellular matrix through direct degradation of its structural proteins and control of extracellular signaling.
Amento, Ang, Asahi, Asahi, Barkho, Bergers, Bini, Cao, Cardone, Chinopoulos, Cunningham, Denker, Dong, Fabunmi, Fisher, Frisch, Galis, Galis, Galis, Galis, Gidday, Godin, Gross, Gu, Gu, Gurney, Haas, Haddad, Halliwell, Hamann, Harkness, Herman, Hornig, Hyslop, Itoh, Kumura, Langton, Lapchak, Larsen, Lee, Lelongt, Loftus, Lucivero, Luttun, McQuibban, Meredith, Montaner, Montaner, Nagase, Nagel, Nagy, Nagy, Nikkari, Pagenstecher, Qi, Rajagopalan, Ramos, Rekhter, Rolfe, Romanic, Rosell, Rosenberg, Rosenberg, Rosenberg, Rosenberg, Sarén, Sato, Seo, Shrivastava, Shubayev, Siao, Sole, Sottrup, Sternlicht, Strongin, Sukhova, Suzuki, Suzuki, Svedin, Tsuji, Turner, Van, Vogel, Wang, Wang, Webersinke, Yepes, Ying, Zhang, Zhang, Zhang, Zhao   +91 more
core   +1 more source

Targeting Protein Kinases Degradation by PROTACs

Frontiers in Chemistry, 2021
Kinase dysregulation is greatly associated with cell proliferation, migration and survival, indicating the importance of kinases as therapeutic targets for anticancer drug development.
Fei Yu, Ming Cai, Liang Shao, Jihong Zhang   +3 more
doaj   +1 more source

Modulation of microtubule acetylation by the interplay of TPPP/p25, SIRT2 and new anticancer agents with anti-SIRT2 potency [PDF]

, 2017
The microtubule network exerts multifarious functions controlled by its decoration with various proteins and post-translational modifications. The disordered microtubule associated Tubulin Polymerization Promoting Protein (TPPP/p25) and the NAD ...
Adél Szabó, Attila Lehotzky, Judit Oláh, Judit Ovádi, Manfred Jung, Marianna Csaplár, Matthias Schiedel, Péter Lőw, Sándor Szunyogh, Tibor Szénási   +9 more
core   +2 more sources

Targeted degradation of LRG1 to attenuate renal fibrosis

Asian Journal of Pharmaceutical Sciences
Leucine-rich α-2 glycoprotein 1 (LRG1), a secreted glycoprotein, has been identified as significantly upregulated in renal fibrosis, potentially exacerbating the condition by enhancing TGF-β-Smad3-dependent signaling pathways.
Linyao Fan, Yingqiu Qi, Xi Yang, Yarui Xu, Yana Zhang, Longdi Wang, Anying Zhu, Lirong Zhang, Jian Song, Shengnan Du, Guangjun Nie, Huan Min   +11 more
doaj   +1 more source

Molecular architecture of human polycomb repressive complex 2. [PDF]

, 2012
Polycomb Repressive Complex 2 (PRC2) is essential for gene silencing, establishing transcriptional repression of specific genes by tri-methylating Lysine 27 of histone H3, a process mediated by cofactors such as AEBP2.
Aebersold, Ruedi, Ciferri, Claudio, Herzog, Franz, Lander, Gabriel C, Maiolica, Alessio, Nogales, Eva   +5 more
core   +1 more source

Molecular recognition of ternary complexes:a new dimension in the structure-guided design of chemical degraders [PDF]

, 2017
Molecular glues and bivalent inducers of protein degradation (also known as PROTACs) represent a fascinating new modality in pharmacotherapeutics: the potential to knockdown previously thought ‘undruggable’ targets at sub-stoichiometric concentrations in
Alessio Ciulli, Bartlett, Beddell, Blundell, Bohacek, Bondeson, Brown, Buckley, Buckley, Chamberlain, Chan, Choi, Crew, Cyrus, Cyrus, Dhanaraj, Erlanson, Fischer, Fischer, Frost, Gadd, Galdeano, Gray, Griffith, Ho, Ito, Itoh, Itoh, Jin, Kissinger, Kronke, Kronke, Lai, Lebraud, Lipinski, Lipkowitz, Lopez-Girona, Lu, Lu, Lucas, Maniaci, Marriott, Matyskiela, Milroy, Navia, Ohh, Ottis, Paul Workman, Perutz, Petzold, Pommier, Rahuel, Raina, Renaud, Rob L.M. van Montfort, Sakamoto, Schiedel, Schneekloth, Scott J. Hughes, Sheard, Soares, Tan, Thiel, Ulane, Van Molle, Winter, Wurz, Yu, Zengerle   +68 more
core   +2 more sources