Results 241 to 250 of about 148,826 (294)

The two faces of MyoD: repressor and activator of gene expression during myogenesis. [PDF]

Genes Dev
Birchmeier C.
europepmc   +1 more source

The potential for biased signalling in the P2Y receptor family of GPCRs

British Journal of Pharmacology, EarlyView.
The purinergic receptor family is primarily activated by nucleotides, and contains members of both the G protein coupled‐receptor (GPCR) superfamily (P1 and P2Y) and ligand‐gated ion channels (P2X). The P2Y receptors are widely expressed in the human body, and given the ubiquitous nature of nucleotides, purinergic signalling is involved with a plethora
Claudia M. Sisk, Simon Pitchford, Graham Ladds   +2 more
wiley   +1 more source

Structure of a Brochothrix thermosphacta bacteriophage reveals cell wall adsorption mechanism in Gram-positive infecting siphophages. [PDF]

Nat Commun
Peng Y, Pang H, Zheng J, Zhou J, Chen W, Yang F, Xiao H, Liu H.   +7 more
europepmc   +1 more source

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

British Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown, Alan Armstrong, David J. Mann   +2 more
wiley   +1 more source

Disrupting the ASH2L-DPY30 PPI in cancer: structure, function, and therapeutic opportunities in H3K4 methylation. [PDF]

Epigenetics Chromatin
Kamel EM, Allam AA, Rudayni HA, Alkhedhairi S, Ahmed NA, Alkhayl FFA, Lamsabhi AM.   +6 more
europepmc   +1 more source

Targeting protein–protein interactions with reversible covalent modalities: Non‐cysteine chemistries

British Journal of Pharmacology, EarlyView.
Abstract Protein–protein interactions (PPIs) are central to diverse cellular functions, and represent a rapidly expanding class of therapeutic targets. Advancements in covalent drug design have enabled small‐molecule drugs to overcome challenges associated with engaging these targets, such as limited durations of action and difficult‐to‐drug (expansive,
Ruchira Basu, Steven Fletcher
wiley   +1 more source

Modification of Whey Protein Isolate with Surfactants Based on Hofmeister Series and Interaction Parameter. [PDF]

ACS Omega
Lopes JS, Cosate de Andrade MF, Morales AR.   +2 more
europepmc   +1 more source

Defining AV2‐1 as a novel pharmacological probe to target human and rodent TRPV2

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Transient receptor potential vanilloid 2 (TRPV2) is a non‐selective cation channel implicated in immune cell functions. However, progress in understanding TRPV2 has been limited by a lack of potent and selective pharmacological tools, particularly those targeting the human variant. We aimed to identify and characterise a
Andrea Leipe, Julia A. Rocereta, Ruth A. Pumroy, Andreas Leffler, Michael Schaefer, Vera Moiseenkova‐Bell, Kerstin Hill   +6 more
wiley   +1 more source

Structural insight into IscB's RNA-lid-based inactivation mechanism. [PDF]

Nat Struct Mol Biol
Wang F, Guo R, Zhang S, Cui Y, Wang J, Hu T, Liu K, Wang Q, Liu Y, Nam KH, Zhao ZW, Ji Q, Xu X, Wang E, Zhu Y, Yang Y, Luo M, Ma P, Ma S, Xu C, Hu C.   +20 more
europepmc   +1 more source

The amino terminal domain of the human α7 nicotinic acetylcholine receptor subunit leads to the functional expression of human/insect receptors

British Journal of Pharmacology, EarlyView.
Human α7 receptors have been characterised in terms of pharmacological properties. Insertion of the N‐terminal domain of the human α7 subunit leads to honeybee and cockroach chimeric receptors activated by ACh and inhibited by α‐Bgt. Insertion of the human cys‐loop leads to cockroach chimeric receptors modulated by PNU.
Alison Cartereau, Chloé Veront, Alexandra Cremades, Priscilla Martin, Remi Gojard, Nicolas Galland, Emiliane Taillebois, Dieudonnée Togbé, Jean‐Yves Le Questel, Steeve H. Thany   +9 more
wiley   +1 more source