Search Results - "Gilon, Chaim"
-
1
Intestinal Permeability of Cyclic Peptides: Common Key Backbone Motifs Identified
Published in Journal of the American Chemical Society (25-07-2012)“…Insufficient oral bioavailability is considered as a key limitation for the widespread development of peptides as therapeutics. While the oral bioavailability…”
Get full text
Journal Article -
2
The tripartite mechanism as the basis for a biochemical memory engram
Published in Journal of integrative neuroscience (30-06-2019)“…In this paper, we address the enigma of the memory engram, the physical trace of memory in terms of its composition, processes, and location. A neurochemical…”
Get full text
Journal Article -
3
Development of Clarstatin, a Novel Drug Lead for the Therapy of Autoimmune Uveitis
Published in Pharmaceutics (27-05-2024)“…We describe the design, synthesis, and activity of a potent thiourea-bridged backbone cyclic peptidomimetic known as Clarstatin, comprising a 5-amino acid…”
Get full text
Journal Article -
4
Synthesis of Novel Arginine Building Blocks with Increased Lipophilicity Compatible with Solid-Phase Peptide Synthesis
Published in Molecules (Basel, Switzerland) (25-11-2023)“…Arginine, due to the guanidine moiety, increases peptides' hydrophilicity and enables interactions with charged molecules, but at the same time, its presence…”
Get full text
Journal Article -
5
The Effect of Multiple N-Methylation on Intestinal Permeability of Cyclic Hexapeptides
Published in Molecular pharmaceutics (04-04-2011)“…Recent progress in peptide synthesis simplified the synthesis of multiple N-methylation of peptides. To evaluate how multiple N-methylation affects the…”
Get full text
Journal Article -
6
Enhancing Oral Bioavailability of Cyclic RGD Hexa-peptides by the Lipophilic Prodrug Charge Masking Approach: Redirection of Peptide Intestinal Permeability from a Paracellular to Transcellular Pathway
Published in Molecular pharmaceutics (06-08-2018)“…Hydrophilic peptides constitute most of the active peptides. They mostly permeate via tight junctions (paracellular pathway) in the intestine. This…”
Get full text
Journal Article -
7
Novel humanin analogs confer neuroprotection and myoprotection to neuronal and myoblast cell cultures exposed to ischemia-like and doxorubicin-induced cell death insults
Published in Peptides (New York, N.Y. : 1980) (01-12-2020)“…[Display omitted] •Humanin is a cytoprotective, 24-amino acid mitochondrial-derived peptide.•Humanin novel synthetic analogs HUJInin and c(D-Ser14-HN) were…”
Get full text
Journal Article -
8
Conversion of Protein Active Regions into Peptidomimetic Therapeutic Leads Using Backbone Cyclization and Cycloscan - How to Do it Yourself
Published in Current topics in medicinal chemistry (01-01-2018)“…Protein-protein Interactions (PPIs) are particularly important for controlling both physiologic and pathologic biological processes but are difficult to target…”
Get more information
Journal Article -
9
Deciphering Direct and Indirect Effects of Neurokinin B and GnRH in the Brain-Pituitary Axis of Tilapia
Published in Frontiers in endocrinology (Lausanne) (12-07-2019)“…Neurokinin B (NKB) and its cognate receptor (NK3R) are emerging as important components of the neuroendocrine regulation of reproduction. Unlike mammalian ,…”
Get full text
Journal Article -
10
Structure-Activity Relationship of Synthetic Linear KTS-Peptides Containing Meta-Aminobenzoic Acid as Antagonists of α1β1 Integrin with Anti-Angiogenic and Melanoma Anti-Tumor Activities
Published in Pharmaceuticals (Basel, Switzerland) (01-05-2024)“…To develop peptide drugs targeting integrin receptors, synthetic peptide ligands endowed with well-defined selective binding motifs are necessary. The snake…”
Get full text
Journal Article -
11
DMAP-assisted sulfonylation as an efficient step for the methylation of primary amine motifs on solid support
Published in Beilstein journal of organic chemistry (03-05-2017)“…Several multistep strategies were developed to ensure single methylation of amines on solid support. These strategies rely on the introduction of the -NBS…”
Get full text
Journal Article -
12
A small shared epitope-mimetic compound potently accelerates osteoclast-mediated bone damage in autoimmune arthritis
Published in The Journal of immunology (1950) (01-09-2013)“…We have recently proposed that the shared epitope (SE) may contribute to rheumatoid arthritis pathogenesis by acting as a ligand that activates…”
Get full text
Journal Article -
13
Treatment with αvβ3-integrin-specific 29P attenuates pressure-overload induced cardiac remodelling after transverse aortic constriction in mice
Published in Journal of Molecular and Cellular Cardiology Plus (Online) (01-06-2024)“…Heart failure remains one of the largest clinical burdens globally, with little to no improvement in the development of disease-eradicating therapeutics…”
Get full text
Journal Article -
14
The Molecular Basis of Neural Memory. Part 7: Neural Intelligence (NI) versus Artificial Intelligence (AI)
Published in AIMS medical science (01-01-2017)“…The link of memory to intelligence is incontestable, though the development of electronic artifacts with memory has confounded cognitive and computer…”
Get full text
Journal Article -
15
Cyclizing Painkillers: Development of Backbone-Cyclic TAPS Analogs
Published in Frontiers in chemistry (12-11-2020)“…Painkillers are commonly used medications. Native peptide painkillers suffer from various pharmacological disadvantages, while small molecule painkillers like…”
Get full text
Journal Article -
16
Backbone Cyclic Peptidomimetic Melanocortin-4 Receptor Agonist as a Novel Orally Administrated Drug Lead for Treating Obesity
Published in Journal of medicinal chemistry (28-02-2008)“…The tetrapeptide sequence His-Phe-Arg-Trp, derived from melanocyte-stimulating hormone (αMSH) and its analogs, causes a decrease in food intake and elevates…”
Get full text
Journal Article -
17
Allosteric inhibition of g-protein coupled receptor oligomerization: strategies and challenges for drug development
Published in Current topics in medicinal chemistry (01-01-2014)“…G-protein coupled receptors (GPCRs) mediate a large number of biological pathways and are major therapeutic targets. One of the most exiting phenomena of GPCRs…”
Get more information
Journal Article -
18
The effect of backbone cyclization on PK/PD properties of bioactive peptide-peptoid hybrids: The melanocortin agonist paradigm
Published in Bioorganic & medicinal chemistry (15-01-2010)“…General structure of peptides, peptoids, peptomers and backbone cyclic peptomers. A peptide–peptoid hybrid (peptomer) library was designed and synthesized,…”
Get full text
Journal Article -
19
Synthesis and Pharmacological Characterization of Visabron, a Backbone Cyclic Peptide Dual Antagonist of α4β1 (VLA-4)/α9β1 Integrin for Therapy of Multiple Sclerosis
Published in JACS Au (27-12-2021)“…Integrins α4β1/ α9β1 are important in the pathogenesis and progression of inflammatory and autoimmune diseases by their roles in leukocyte activation and…”
Get full text
Journal Article -
20
Oxytocin-Monolayer-Based Impedimetric Biosensor for Zinc and Copper Ions
Published in ACS omega (31-12-2017)“…Zinc and copper are essential metal ions for numerous biological processes. Their levels are tightly maintained in all body organs. Impairment of the Zn2+ to…”
Get full text
Journal Article