Results 61 to 70 of about 13,155 (273)

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

Cell wall target fragment discovery using a low‐cost, minimal fragment library

FEBS Letters, EarlyView.
LoCoFrag100 is a fragment library made up of 100 different compounds. Similarity between the fragments is minimized and 10 different fragments are mixed into a single cocktail, which is soaked to protein crystals. These crystals are analysed by X‐ray crystallography, revealing the binding modes of the bound fragment ligands.
Kaizhou Yan, Mathew Stanley, Olawale Raimi, Andrew T. Ferenbach, Helge C Dorfmueller, Daan M. F. van Aalten   +5 more
wiley   +1 more source

Surface probing by fragment-based screening and computational methods identifies ligandable pockets on the von Hippel-Lindau (VHL) E3 ubiquitin ligase [PDF]

, 2018
Beyond the targeting of E3 ubiquitin ligases to inhibit protein homeostasis, E3 ligase binders can be repurposed as targeted protein degraders (PROTACs or molecular glues).
Ciulli, Alessio, Lucas, Xavier, van Molle, Inge   +2 more
core   +4 more sources

AAA+ protein unfoldases—the Moirai of the proteome

FEBS Letters, EarlyView.
AAA+ unfoldases are essential molecular motors that power protein degradation and disaggregation. This review integrates recent cryo‐electron microscopy (cryo‐EM) structures and single‐molecule biophysical data to reconcile competing models of substrate translocation.
Stavros Azinas, Marta Carroni
wiley   +1 more source

Plasmodium falciparum PfA-M1 aminopeptidase is trafficked via the parasitophorous vacuole and marginally delivered to the food vacuole [PDF]

, 2010
Background The Plasmodium falciparum PfA-M1 aminopeptidase, encoded by a single copy gene, displays a neutral optimal activity at pH 7.4. It is thought to be involved in haemoglobin degradation and/or invasion of the host cells.
Omid Azimzadeh, Cissé Sow, Marc Gèze, Julius Nyalwidhe, Isabelle Florent   +4 more
core   +1 more source

Multi‐omics and low‐input proteomics profiling reveals dynamic regulation driving pluripotency initiation in early mouse embryos

FEBS Open Bio, EarlyView.
Mouse pre‐implantation development involves a transition from totipotency to pluripotency. Integrating transcriptomics, epigenetic profiling, low‐input proteomics and functional assays, we show that eight‐cell embryos retain residual totipotency features, whereas cytoskeletal remodeling regulated by the ubiquitin‐proteasome system drives progression ...
Wanqiong Li, Xi Xiao, Lingbin Qi, Chanyi Li, Sirui Song, Jiaying Qin, Zhigang Xue, Jinfeng Xue, Huaifang Li   +8 more
wiley   +1 more source

PROteolysis TArgeting Chimeras (PROTACs) as emerging anticancer therapeutics

Oncogene, 2020
Using PROteolysis TArgeting Chimeras (PROTACs) to degrade proteins that are important for tumorigenesis has emerged as a potential therapeutic strategy for cancer. PROTACs are heterobifunctional molecules consisting of one ligand for binding to a protein of interest (POI) and another to an E3 ubiquitin (E3) ligase, connected via a linker.
Sajid Khan, Yonghan He, Xuan Zhang, Yaxia Yuan, Shaoyan Pu, Qingpeng Kong, Guangrong Zheng, Daohong Zhou   +7 more
openaire   +3 more sources

Engineering of Glioblastoma‐Derived Biomimetic Vesicles and Their Structural and Molecular Features

Advanced Healthcare Materials, EarlyView.
ABSTRACT Biomimetic nanosystems and vesicles have arisen as a novel approach to design vesicular transport systems with diverse therapeutic potential. The ‘biomimetic’ strategy involves the integration of cell membrane components into lipid bilayers, conferring them with biological properties originating from the cell of origin. Until now, most studies
Noelia Hernández‐Lobato, Hanan Abumanhal‐Masarweh, Martí de Cabo, Pablo Guerra, Marilena Hadjidemetriou, Neus Lozano, Kostas Kostarelos   +6 more
wiley   +1 more source

Deciphering the Roles of Multicomponent Recognition Signals by the AAA+ Unfoldase ClpX [PDF]

, 2015
ATP-dependent protein remodeling and unfolding enzymes are key participants in protein metabolism in all cells. How these often-destructive enzymes specifically recognize target protein complexes is poorly understood.
Baker, Tania, Ling, Lorraine, Montaño, Sherwin P., Rice, Phoebe A., Sauer, Robert T.   +4 more
core   +1 more source

Nanotherapies for Atherosclerosis: Targeting, Catalysis, and Energy Transduction

Advanced Healthcare Materials, EarlyView.
Atherosclerosis management is hindered by poor drug targeting and plaque heterogeneity. Nanotechnology overcomes these barriers via three core strategies: (1) target‐engineered nanocarriers that achieve lesion‐specific precision via ligand modification, biomimetic camouflage, stimuli‐responsive release, and self‐propelling nanomotors; (2) catalytic ...
Yuqi Yang, Jingguo Qu, Tonghuan Xiao, Xinyang Han, Michael Tin‐Cheung Ying   +4 more
wiley   +1 more source