Results 31 to 40 of about 11,341 (256)

SPR-measured dissociation kinetics of PROTAC ternary complexes influence target degradation rate [PDF]

, 2019
Bifunctional degrader molecules, known as proteolysis-targeting chimeras (PROTACs), function by recruiting a target to an E3 ligase, forming a target/PROTAC/ligase ternary complex.
Ciulli, Alessio, Farnaby, William, Galant, Michael, Hughes, Scott J, Roy, Michael, Rumpel, Klaus, Whitworth, Claire, Winkler, Sandra   +7 more
core   +3 more sources

Enhanced thrombin generation in patients with cirrhosis-induced coagulopathy [PDF]

, 2010
BACKGROUND: Prothrombin time (PT) and the international normalized ratio (INR) are still routinely measured in patients with liver cirrhosis to 'assess' their bleeding risk despite the lack of correlation with the two. Thrombin generation (TG) assays are
Agarwal, Auzinger, Bellest, Besser, Brodin, Caldwell, Clauss, Collins, Dargaud, Dielis, Ewe, Gatt, Grant, Haidl, Hemker, Hezard, Hron, Kamath, Lincz, Northup, Quick, Sogaard, Tripodi, Tripodi, Tripodi, Tripodi, Van Veen, Van Veen   +27 more
core   +1 more source

Inhibition of bromodomain and extra-terminal (BET) proteins increases NKG2D ligand MICA expression and sensitivity to NK cell-mediated cytotoxicity in multiple myeloma cells. role of cMYC-IRF4-miR-125b interplay [PDF]

, 2016
Background: Anticancer immune responses may contribute to the control of tumors after conventional chemotherapy and different observations have indicated that chemotherapeutic agents can induce immune responses resulting in cancer cell death and immune ...
Abruzzese, MARIA PIA, Bilotta, MARIA TERESA, Borrelli, Cristiana, Cippitelli, Marco, Fionda, Cinzia, Molfetta, Rosa, Paolini, Rossella, Petrucci, MARIA TERESA, Ricciardi, Maria Rosaria, Santoni, Angela, Soriani, Alessandra, Vulpis, Elisabetta, Zingoni, Alessandra, Zitti, Beatrice   +13 more
core   +15 more sources

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

PROTACs: A novel strategy for cancer drug discovery and development

MedComm, 2023
Proteolysis targeting chimera (PROTAC) technology has become a powerful strategy in drug discovery, especially for undruggable targets/proteins. A typical PROTAC degrader consists of three components: a small molecule that binds to a target protein, an ...
Xin Han, Yi Sun
doaj   +1 more source

Non-small molecule PROTACs (NSM-PROTACs): Protein degradation kaleidoscope

Acta Pharmaceutica Sinica B, 2022
The proteolysis targeting chimeras (PROTACs) technology has been rapidly developed since its birth in 2001, attracting rapidly growing attention of scientific institutes and pharmaceutical companies. At present, a variety of small molecule PROTACs have entered the clinical trial.
Sinan Ma, Jianai Ji, Yuanyuan Tong, Yuxuan Zhu, Junwei Dou, Xian Zhang, Shicheng Xu, Tianbao Zhu, Xiaoli Xu, Qidong You, Zhengyu Jiang   +10 more
openaire   +3 more sources

Structural basis of PROTAC cooperative recognition for selective protein degradation [PDF]

, 2017
Inducing macromolecular interactions with small molecules to activate cellular signaling is a challenging goal. PROTACs (proteolysis-targeting chimeras) are bifunctional molecules that recruit a target protein in proximity to an E3 ubiquitin ligase to ...
A Illendula, A Thompson, A Whitty, AC Lai, AC Lai, AJ McCoy, Alessio Ciulli, Andrea Testa, AW Schüttelkopf, BR Brooks, C Galdeano, CE Stebbins, DM Duda, Douglas J Lamont, DP Bondeson, E Bulatov, E Krissinel, E Nicodeme, EF Douglass Jr., ES Fischer, ES Fischer, G Lu, G Petzold, GE Winter, GN Murshudov, J Frost, J Krönke, J Lu, J Zuber, J-H Min, JC Phillips, JM Roberts, K Raina, K Vanommeslaeghe, KM Sakamoto, Kwok-Ho Chan, LB Sheard, LL Manza, M Gilar, M Tanaka, M Toure, M Zengerle, M Zhou, MD Winn, ME Matyskiela, Michael Zengerle, MJ Waring, Morgan S Gadd, NM Glykos, P Emsley, P Filippakopoulos, P Filippakopoulos, P Thiel, PP Chamberlain, PR Evans, RA Laskowski, RJ Deshaies, RM Eglen, T Ito, VB Chen, W Humphrey, W Kabsch, W-C Hon, Wenzhang Chen, X Huang, X Tan, Xavier Lucas, Y Pommier   +67 more
core   +3 more sources

Protacs for Treatment of Cancer [PDF]

Pediatric Research, 2010
Protein degradation is the cell's mechanism of eliminating misfolded or unwanted proteins. The pathway by which proteins are degraded occurs through the ubiquitin-proteasome system. Ubiquitin is a small 9-kD (kDa) protein that is attached to proteins. A minimum of four ubiquitins are required for proteins to be recognized by the degradation machinery ...
openaire   +2 more sources

PROTACs– a game-changing technology [PDF]

Expert Opinion on Drug Discovery, 2019
Introduction: Proteolysis - targeting chimeras (PROTACs) have emerged as a new modality with the potential to revolutionize drug discovery. PROTACs are heterobifunctional molecules comprising of a ligand targeting a protein of interest, a ligand targeting an E3 ligase and a connecting linker.
Konstantinidou, Markella, Li, Jingyao, Zhang, Bidong, Wang, Zefeng, Shaabani, Shabnam, Ter Brake, Frans, Essa, Khaled, Dömling, Alexander   +7 more
openaire   +2 more sources

Ubistatins Inhibit Proteasome-Dependent Degradation by Binding the Ubiquitin Chain [PDF]

, 2004
To identify previously unknown small molecules that inhibit cell cycle machinery, we performed a chemical genetic screen in Xenopus extracts. One class of inhibitors, termed ubistatins, blocked cell cycle progression by inhibiting cyclin B proteolysis ...
Coffino, Philip, D'Onofrio, Mariapina, Deshaies, Raymond J., Fushman, David, King, Randall W., Peters, Noel R., Sakamoto, Kathleen M., Tochtrop, Gregory P., Varadan, Ranjani, Verma, Rati, Zhang, Mingsheng   +10 more
core   +2 more sources