Systems analysis of drug-induced receptor tyrosine kinase reprogramming following targeted mono- and combination anti-cancer therapy [PDF]
The receptor tyrosine kinases (RTKs) are key drivers of cancer progression and targets for drug therapy. A major challenge in anti-RTK treatment is the dependence of drug effectiveness on co-expression of multiple RTKs which defines resistance to single ...
Goltsov, Alexey +26 more
core +1 more source
Gut microbiome and aging—A dynamic interplay of microbes, metabolites, and the immune system
Age‐dependent shifts in microbial communities engender shifts in microbial metabolite profiles. These in turn drive shifts in barrier surface permeability of the gut and brain and induce immune activation. When paired with preexisting age‐related chronic inflammation this increases the risk of neuroinflammation and neurodegenerative diseases.
Aaron Mehl, Eran Blacher
wiley +1 more source
Probing Cortical Sites of Antipsychotic Drug Action with in vivo Receptor Imaging
Imaging receptors using radioactive ligands has allowed direct determination of the sites of action of antipsychotic drugs. Initial studies relating antipsychotic drug efficacy to action at striatal dopamine D2-like receptors have recently been ...
P. Shaw, L. S. Pilowsky
doaj +1 more source
Ascidian Ciona larvae initially show strong clockwise tail twisting, which is largely corrected during development. However, a small residual twist remains. This study shows that organized helical myofibrils in tail muscles mechanically stabilize this residual asymmetry, preventing complete restoration of bilateral symmetry and revealing how embryos ...
Yuki S. Kogure +3 more
wiley +1 more source
Drug targeting to tumors using HPMA copolymers [PDF]
Copolymers based on N-(2-hydroxypropyl)methacrylamide (HPMA) are prototypic and well-characterized polymeric drug carriers that have been broadly implemented in the delivery of anticancer agents.
Dep Farmaceutische wetenschappen +2 more
core +1 more source
Adhesion GPCRs are widely expressed throughout the subsections of the gastrointestinal tract [PDF]
Background: G protein-coupled receptors (GPCRs) represent one of the largest families of transmembrane receptors and the most common drug target. The Adhesion subfamily is the second largest one of GPCRs and its several members are known to mediate ...
Schiöth, Helgi B, +20 more
core +2 more sources
Septin 9 polybasic domains couple phosphoinositide‐rich membrane binding to centrosome positioning, Golgi organization, and microtubule acetylation to control epithelial polarity. Their loss disrupts this axis, causing centrosome mispositioning, Golgi fragmentation, reduced microtubule acetylation, and polarity inversion via upregulation of the ...
Ting ting Cai +4 more
wiley +1 more source
Identification of class-determining residues in G protein-coupled receptors by sequence analysis
G protein-coupled receptors (GPCRs) form a large superfamily of receptors that are characterised by a seven transmembrane helical motif, The functions they perform, such as binding ligands and G proteins, are related to the presence of certain amino ...
Ijzerman, Adriaan P. +3 more
core
Receptor for activated C kinase-1 facilitates protein kinase C-dependent phosphorylation and functional modulation of GABA(A) receptors with the activation of G-protein-coupled receptors [PDF]
GABA(A) receptors are the principal sites of fast synaptic inhibition in the brain. These receptors are hetero-pentamers that can be assembled from a number of subunit classes: alpha(1-6), beta(1-3), gamma(1-3), delta(1), epsilon, theta, and pi, but the ...
Trevor G Smart +7 more
core
Muscarinic acetylcholine receptors as targets for drug development [PDF]
Muscarinic acetylcholine receptors (mAChRs) are a subfamily of G protein-coupled receptors that have been identified as promising targets for drug development. Five different mAChR subtypes regulate various fundamental functions.
Stojković Maja +2 more
doaj +1 more source

