Results 91 to 100 of about 5,903,465 (247)

Multivalent sialic acid binding proteins as novel therapeutics for influenza and parainfluenza infection [PDF]

open access: yes, 2014
In nature, proteins with weak binding affinity often use a multivalency approach to enhance protein affinity via an avidity effect. Interested in this multivalency approach, we have isolated a carbohydrate binding module (CBM) that recognises sialic ...
Alias, Nadiawati
core   +2 more sources

Paclitaxel induces NM2‐dependent cellular contraction through GEF‐H1 dissociation from microtubules and RhoA/ROCK activation in cancer cells

open access: yesMolecular Oncology, EarlyView.
Taxanes are widely used chemotherapeutics whose effects on cellular mechanics remain poorly understood. We show that paclitaxel induces rapid cellular contraction by promoting GEF‐H1 dissociation from microtubules and non‐muscle myosin II activation through RhoA/ROCK.
Gloria Asensio‐Juárez   +5 more
wiley   +1 more source

Enabling target-aware molecule generation to follow multi objectives with Pareto MCTS

open access: yesCommunications Biology
Target-aware drug discovery has greatly accelerated the drug discovery process to design small-molecule ligands with high binding affinity to disease-related protein targets.
Yaodong Yang   +9 more
doaj   +1 more source

Studies and analysis of drug-target interactions by affinity chromatography and related techniques: A review

open access: yesJournal of Pharmaceutical Analysis
The characterization of drug-target interactions is a key component of drug discovery, testing, and development. Affinity chromatography is one approach that can be used for this type of analysis.
David S. Hage   +7 more
doaj   +1 more source

SPHINX31 acts as a SRPK1 inhibitor targeting the ATR/DNA‐PKcs/CHK1 replicative checkpoint to inhibit cell growth in non‐small cell lung cancer

open access: yesMolecular Oncology, EarlyView.
The kinase SRPK1 directly interacts with the protein TOPBP1 and regulates the pre‐mRNA splicing of WIZ thereby contributing to the activation of the ATR/CHK1 replicative checkpoint in response to replicative stress. This allows cancer cells' genomic stability and survival.
Amani Shreim   +17 more
wiley   +1 more source

Probing the druggability of the Notch1 ankyrin domain using a fragment-based approach [PDF]

open access: yes, 2011
Notch signalling is a highly conserved pathway that is important in the developmental processes that control cell differentiation and cell fates. This canonical pathway involves binding of a transmembrane ligand in one cell to the extraceullular domain ...

core   +2 more sources

Versatile vector tools for efficient protein screening across multiple expression systems

open access: yesFEBS Open Bio, EarlyView.
A unified vector toolkit enables rapid protein expression screening across E. coli, insect, and mammalian cells. A single primer pair amplifies the target gene, which is inserted into any vector via a standardized interface. This streamlined workflow eliminates repeated cloning steps, accelerating the identification of optimal expression conditions for
Zhimin Zhu   +5 more
wiley   +1 more source

Delivering bioactive cyclic peptides that target Hsp90 as prodrugs

open access: yesJournal of Enzyme Inhibition and Medicinal Chemistry, 2019
The most challenging issue facing peptide drug development is producing a molecule with optimal physical properties while maintaining target binding affinity.
Yuantao Huo   +7 more
doaj   +1 more source

Cyclic azapeptide CD36 ligand attenuates cardiac injury and reduces long‐chain fatty acid accumulation after myocardial ischemia–reperfusion in mice

open access: yesFEBS Open Bio, EarlyView.
In a murine model of myocardial ischemia and reperfusion (MI/R), the CD36 azapeptide ligand MPE‐298 reduces cardiac injury and transiently lowers left ventricular long‐chain fatty acids (LCFAs) accumulation 3 h after reperfusion, accompanied by a decrease of oxidative stress and inflammation‐associated genes' expression in the heart and adipose tissue.
Jade Gauvin   +12 more
wiley   +1 more source

Relative affinity constants by electrospray ionization and Fourier transform ion cyclotron resonance mass spectrometry: calmodulin binding to peptide analogs of myosin light chain kinase [PDF]

open access: yes, 2003
Synthetic RS20 peptide and a set of its point-mutated peptide analogs have been used to analyze the interactions between calmodulin (CaM) and the CaM-binding sequence of smooth-muscle myosin light chain kinase both in the presence and the absence of Ca2+.
Lafitte, Daniel   +3 more
core   +1 more source

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