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Aude Sylvain, Natacha Stoehr, Fupeng Ma, Artiom Cernijenko et autres
ch, us, de, cn (code pays fourni par la source)
Antonin V. Tutter, Dennis L. Buckley, Andrei A. Golosov, Xiaolei Ma et autres
us, ch, cn (code pays fourni par la source)
Aude Sylvain, Natacha Stoehr, Fupeng Ma, Artiom Cernijenko et autres
Summary The NLRP3 (NACHT-, leucine-rich repeat [LRR]- and pyrin domain [PYD]- containing protein 3) inflammasome is a cytoplasmic signaling complex that promotes inflammation in response to signals from infection and cellular damage. Increased activation of the NLRP3 inflammasome is linked to numerous …
ch, cn, us, de (code pays fourni par la source)
Antonin V. Tutter, Dennis L. Buckley, Andrei A. Golosov, Xiaolei Ma et autres
Abstract The Von Hippel-Lindau Tumor Suppressor gene product (pVHL) is an E3 ligase substrate receptor that binds proline-hydroxylated HIF1-α, leading to its ubiquitin-dependent degradation. By using protein arrays, we identified a small molecule that binds the HIF1-α binding pocket on pVHL and …
us (code pays fourni par la source)
Sarah C. Moser, Jane S.A. Voerman, Dennis L. Buckley, Georg E. Winter et autres
nl, ch, cn, us, at (code pays fourni par la source)
Benika J. Pinch, Dennis L. Buckley, Scott Gleim, Scott M. Brittain et autres
ch, cn, us (code pays fourni par la source)
Ryosuke Shirasaki, Geoffrey M. Matthews, Sara Gandolfi, Ricardo De Matos Simoes et autres
Heterobifunctional proteolysis-targeting chimeric compounds leverage the activity of E3 ligases to induce degradation of target oncoproteins and exhibit potent preclinical antitumor activity. To dissect the mechanisms regulating tumor cell sensitivity to different classes of pharmacological "degraders" of oncoproteins, we performed genome-scale CRISPR-Cas9-based …
us, nl (code pays fourni par la source)
Behnam Nabet, Fleur M. Ferguson, Bo Kyung A. Seong, Miljan Kuljanin et autres
Abstract Chemical biology strategies for directly perturbing protein homeostasis including the degradation tag (dTAG) system provide temporal advantages over genetic approaches and improved selectivity over small molecule inhibitors. We describe dTAG V -1, an exclusively selective VHL-recruiting dTAG molecule, to rapidly degrade …
us (code pays fourni par la source)
Benika J. Pinch, Dennis L. Buckley, Scott Gleim, Scott M. Brittain et autres
ABSTRACT Targeted protein degradation is a rapidly developing therapeutic modality that promises lower dosing and enhanced selectivity as compared to traditional occupancy-driven inhibitors, and the potential to modulate historically intractable targets. While the well-characterized E3 ligases CRBN and VHL have been successfully …
ch (code pays fourni par la source)
Hailemichael O. Yosief, Shuai Liu, Dennis L. Buckley, Justin M. Roberts et autres
Polo-like kinase 1 (PLK1) and BRD4 are two different therapeutic targets in cancer drug discovery. Recently it has been reported that PLK1 inhibitor, BI-2536, is also a potent inhibitor of BRD4. The simultaneous inhibition of PLK1 and BRD4 by a single drug …
Ting Chen, Xiangpeng Dai, Andrew H. Beck, Lorenz Buser et autres
The bromodomain and extra-terminal (BET) family of proteins, comprised of four members including BRD2, BRD3, BRD4 and the testis-specific isoform BRDT, largely function as transcriptional co-activators 1–3 and play critical roles in various cellular processes, including cell cycle, apoptosis, migration and invasion …
us (code pays fourni par la source)
Behnam Nabet, Fleur M. Ferguson, Bo Kyung A. Seong, Miljan Kuljanin et autres
ABSTRACT Chemical biology strategies for directly perturbing protein homeostasis including the degradation tag (dTAG) system provide temporal advantages over genetic approaches and improved selectivity over small molecule inhibitors. We describe dTAG V -1, an exclusively selective VHL-recruiting dTAG molecule, to rapidly degrade …
us (code pays fourni par la source)
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