Results 31 to 40 of about 464,369 (258)

Targeted Strategies for Degradation of Key Transmembrane Proteins in Cancer

BioTech, 2023
Targeted protein degradation is an attractive technology for cancer treatment due to its ability to overcome the unpredictability of the small molecule inhibitors that cause resistance mutations.
Vehary Sakanyan, Nina Iradyan, Rodolphe Alves de Sousa   +2 more
doaj   +1 more source

Salmonella lipopolysaccharide‐containing supported lipid bilayers as platforms to study bacteriophage interactions

FEBS Letters, EarlyView.
We present robust protocols for the preparation of supported lipid bilayers (SLBs) incorporating either Salmonella smooth LPS or outer membrane vesicles (OMVs). We use a combination of quartz crystal microbalance with dissipation (QCM‐D) and fluorescence microscopy to both characterize the SLBs of various compositions and to probe their interactions ...
Hudson P. Pace, Alyssa Borges, Charles Arnaud, Tove Karlsson, Nina K. Bröker, Stefanie Barbirz, Marta Bally   +6 more
wiley   +1 more source

Research advances in targeted protein degradation technologies [PDF]

Yixue xinzhi zazhi
Targeted protein degradation (TPD) technologies leverage the body’s innate protein degradation systems to selectively eliminate protein of interest (POI).
PI Chuan, HAO Xuanrun, XIAO Haiting, LUO Xing, ZHANG Qixiong   +4 more
doaj   +1 more source

Microbiome−host proteostasis crosstalk—An emerging perspective on mechanisms and interventions toward healthy longevity

FEBS Letters, EarlyView.
Proteostasis and the gut microbiota play a key role in shaping host physiology. Microbiota‐derived metabolites, vitamins, and RNA modulate host proteostasis. Findings from model systems, including C. elegans, indicate microbes can either stabilize or disrupt host proteostasis.
Abhishek Anil Dubey, Maria Ermolaeva
wiley   +1 more source

Induced ubiquitination of the partially disordered estrogen receptor alpha via a 14-3-3 directed molecular glue-PROTAC

Nature Communications
Proteins lacking defined ligandable pockets remain challenging drug targets. Here, we develop a molecular glue-based PROTAC (MGPROTAC) approach that chemically conjugates a molecular glue stabilizer to a VHL-recruiting ligand to capture and ubiquitinate ...
Carlo J. A. Verhoef, Charlotte Crowe, Mark A. Nakasone, Aitana DeLaCuadra-Basté, Tessa Harzing, Naomi A. S. Span, Gajanan Sathe, Laura C. Demmers, Kentaro Iso, Christian Ottmann, Luc Brunsveld, Alessio Ciulli, Peter J. Cossar   +12 more
doaj   +1 more source

Targeted Protein Degradation: Principles and Applications of the Proteasome

Cells, 2023
The proteasome is a multi-catalytic protease complex that is involved in protein quality control via three proteolytic activities (i.e., caspase-, trypsin-, and chymotrypsin-like activities).
Yosup Kim, Eun-Kyung Kim, Yoona Chey, Min-Jeong Song, Ho Hee Jang   +4 more
doaj   +1 more source

Modelling stem cell differentiation related processes—A practical overview for biologists

FEBS Letters, EarlyView.
Stem cell differentiation is complex and difficult to control experimentally. This review introduces suitable computational modelling approaches that can support stem cell research, from mechanistic ODE and abstract models to multiscale and deep learning methods.
Ricco Zeegelaar, Xinqi Yan, Lucas F. Jansen Klomp, Stefano Schivo, Janine N. Post   +4 more
wiley   +1 more source

Discovery of a CNS active GSK3 degrader using orthogonally reactive linker screening

Nature Communications
Bifunctional targeted protein degraders, also known as Proteolysis Targeting Chimeras (PROTACs), are an emerging drug modality that may offer a new approach for treating neurodegenerative diseases. Identifying chemical starting points for PROTACs remains
Andreas Holmqvist, Nur Mehpare Kocaturk, Christina Duncan, Jennifer Riley, Steven Baginski, Graham Marsh, Joel Cresser-Brown, Hannah Maple, Kristiina Juvonen, Gajanan Sathe, Nicola Morrice, Calum Sutherland, Kevin D. Read, William Farnaby   +13 more
doaj   +1 more source

PROTAC-induced protein structural dynamics in targeted protein degradation

eLife
PROteolysis TArgeting Chimeras (PROTACs) are small molecules that induce target protein degradation via the ubiquitin-proteasome system. PROTACs recruit the target protein and E3 ligase; a critical first step is forming a ternary complex.
Kingsley Y Wu, Ta I Hung, Chia-en A Chang   +2 more
doaj   +1 more source

From classic medicinal chemistry to state‐of‐the‐art interdisciplinary medicine: Recent advances in proteolysis‐targeting chimeras technology

Interdisciplinary Medicine, 2023
Proteolysis‐targeting chimeras (PROTACs) is a targeted protein degradation (TPD) technique effected by hijacking the ubiquitin‐proteasome system (UPS) of the cells.
Xuyang Zhao, Yifan Chen, Huang Su, Liqin Zhang   +3 more
doaj   +1 more source