Results 91 to 100 of about 19,199 (236)

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

open access: yesBritish 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

Development of peptidomimetic ligands of Pro-Leu-Gly-NH2 as allosteric modulators of the dopamine D2 receptor

open access: yesBeilstein Journal of Organic Chemistry, 2013
A variety of stable, small-molecule peptidomimetic ligands have been developed to elucidate the mechanism by which the neuropeptide Pro-Leu-Gly-NH2 (PLG) modulates dopaminergic neurotransmission.
Swapna Bhagwanth   +2 more
doaj   +1 more source

Cancer pain: current practice and emerging targets

open access: yesBritish Journal of Pharmacology, EarlyView.
Cancer pain (CP) arises from a complex interplay between the tumour and its microenvironment. Many patients experience a mixed pain phenotype that encompasses nociceptive, neuropathic and neuroinflammatory mechanisms, and vary across tumour type and disease stage. Despite decades of intensive research, the mainstay of cancer pain treatment is still non‐
Yi Ye   +5 more
wiley   +1 more source

Platelet-Induced Clumping of Plasmodium falciparum–Infected Erythrocytes from Malawian Patients with Cerebral Malaria—Possible Modulation In Vivo by Thrombocytopenia [PDF]

open access: yes, 2008
Platelets may play a role in the pathogenesis of human cerebral malaria (CM), and they have been shown to induce clumping of Plasmodium falciparum–parasitized red blood cells (PRBCs) in vitro.
Barnwell JW   +18 more
core   +1 more source

Targeting the noncatalytic activity of GSK3β modulates neuronal excitability in medium spiny neurons via Nav1.6 interactions

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Kinases phosphorylate ion channels, but their noncatalytic roles via protein–protein interactions (PPI) are less understood. Here, we identified the peptidomimetic ZL141 to characterize the PPI between GSK3β and Nav1.6, revealing a noncatalytic role for GSK3β in regulating Nav1.6 currents and neuronal excitability ...
Aditya K. Singh   +19 more
wiley   +1 more source

Synthesis of a [1,4]dioxane-2,5-dione based-peptidomimetic scaffold [PDF]

open access: yes, 2006
Copyright © ARKAT USA, Inc The document attached has been archived with permission from the publisher.(2S,3S)-3-[N-Cbz-L-Leucinyl]amino-2-hydroxy-4-phenylbutanoic acid 5 dimerised on treatment with EDCI and HOBT to give the symmetrical [1,4]dioxane-2,5 ...
Abell, A., Harvey, A.
core  

Hepatitis C virus molecular evolution: Transmission, disease progression and antiviral therapy [PDF]

open access: yes, 2014
Hepatitis C virus (HCV) infection represents an important public health problem worldwide. Reduction of HCV morbidity and mortality is a current challenge owned to several viral and host factors.
Carpio Pedroza, Juan Carlos   +10 more
core   +1 more source

PEGylated Chitosan Nanoparticles: Engineering Multifunctional Platforms for Targeted Cervical and Lung Cancer Treatment

open access: yesCancer Science, EarlyView.
Graphical representation of formation of self‐assembled PEGylated Chitosan Nanoparticles and their mechanism in tumor localization. ABSTRACT Polymer‐based nanocarriers have emerged as transformative platforms in cancer nanomedicine, enabling controlled and site‐specific delivery of therapeutic agents.
Prashant Kesharwani   +5 more
wiley   +1 more source

Pasireotide for the Medical Management of Feline Hypersomatotropism [PDF]

open access: yes, 2015
BACKGROUND: Feline hypersomatotropism (HST) is a cause of diabetes mellitus in cats. Pasireotide is a novel multireceptor ligand somatostatin analog that improves biochemical control of humans with HST.
Abraham   +45 more
core   +2 more sources

A guide to the types, structures, and multifaceted functions of matrix metalloproteinases in cancer

open access: yesThe FEBS Journal, EarlyView.
Matrix metalloproteinases (MMPs) orchestrate cancer progression and metastasis through proteolytic and non‐proteolytic actions. By remodeling the tumor microenvironment, enhancing growth factor availability, and modulating cell behavior, MMPs promote proliferation, migration or invasion, and epithelial‐to‐mesenchymal transition. Alongside extracellular
Zoi Piperigkou   +4 more
wiley   +1 more source

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