They include
its effects on endothelial cell «differentiation» to yield tubular - like structures, endothelial and tumor cell proliferation, apoptosis, and migration, as well as its effects on extracellular matrix remodelling enzyme activities of matrix metalloproteinase - 2 (MMP - 2) and urokinase - type plasminogen activator (uPA).
Not exact matches
Palmitate and oleate have distinct
effects on the inflammatory phenotype of human
endothelial cells.
Investigating the
effect of spatially varying wall shear stress
on lymphatic
endothelial cell alignment and transcriptional regulation Eleftheria Michalaki, Stanford University
Mechanotransduction The
effects of extracellular matrix stiffening
on endothelial cell health Cynthia Reinhart - King, Cornell University The
effects of membrane cholesterol and extracellular matrix elasticity
on vascular smooth muscle
cell mechanics and migration Zhongkui Hong, University of South Dakota
Figure 6 shows the
effects of 75 µM kahweol
on endothelial cell migration, as determined by the «wound healing» assay, after 8 and 24 h of treatment.
Therefore, it would be advisable to test the potential
effects of kahweol
on endothelial cell apoptosis.
Therefore, we studied the
effects of kahweol
on the growth of
endothelial cells.
Since invasion is dependent
on extracellular matrix remodeling capabilities, this inhibitory
effect strongly suggested that the two key extracellular membrane remodeling enzymes expressed by
endothelial cells, namely, MMP - 2 and uPA could be other main key targets of the pharmacological action of kahweol
on endothelial cells.
Different in vitro assays were carried out in order to test the specific
effects of kahweol treatment
on several key steps of the angiogenic process in both
endothelial and tumor
cells.
We also demonstrate the inhibitory
effect of kahweol
on the
endothelial cell potential to remodel extracellular matrix by targeting two key molecules involved in the process, MMP - 2 and uPA.
Data obtained
on the
effects of kahweol
on endothelial cell invasion (as determined by a continuous fluorescent assay) clearly show that kahweol induces an anti-invasive
effect in HUVEC in a dose - dependent manner (Figure 7).
Josin researchers made two major findings: They identified the mechanisms by which GLP - 1 can induce protective actions
on the glomerular (renal)
endothelial cells by inhibiting the signaling pathway of Ang II and its pro-inflammatory
effect; and demonstrated a dual signaling mechanism by which hyperglycemia, via PKCβ activation, can increase Ang II action and inhibit GLP - 1's protective
effects by reducing the expression of GLP - 1 receptors in the glomerular
endothelial cells.
Susan Amara, USA - «Regulation of transporter function and trafficking by amphetamines, Structure - function relationships in excitatory amino acid transporters (EAATs), Modulation of dopamine transporters (DAT) by GPCRs, Genetics and functional analyses of human trace amine receptors» Tom I. Bonner, USA (Past Core Member)- Genomics, G protein coupled receptors Michel Bouvier, Canada - Molecular Pharmacology of G protein - Coupled Receptors; Molecular mechanisms controlling the selectivity and efficacy of GPCR signalling Thomas Burris, USA - Nuclear Receptor Pharmacology and Drug Discovery William A. Catterall, USA (Past Core Member)- The Molecular Basis of Electrical Excitability Steven Charlton, UK - Molecular Pharmacology and Drug Discovery Moses Chao, USA - Mechanisms of Neurotophin Receptor Signaling Mark Coles, UK - Cellular differentiation, human embryonic stem
cells, stromal
cells, haematopoietic stem
cells, organogenesis, lymphoid microenvironments, develomental immunology Steven L. Colletti, USA Graham L Collingridge, UK Philippe Delerive, France - Metabolic Research (diabetes, obesity, non-alcoholic fatty liver, cardio - vascular diseases, nuclear hormone receptor, GPCRs, kinases) Sir Colin T. Dollery, UK (Founder and Past Core Member) Richard M. Eglen, UK Stephen M. Foord, UK David Gloriam, Denmark - GPCRs, databases, computational drug design, orphan recetpors Gillian Gray, UK Debbie Hay, New Zealand - G protein - coupled receptors, peptide receptors, CGRP, Amylin, Adrenomedullin, Migraine, Diabetes / obesity Allyn C. Howlett, USA Franz Hofmann, Germany - Voltage dependent calcium channels and the positive inotropic
effect of beta adrenergic stimulation; cardiovascular function of cGMP protein kinase Yu Huang, Hong Kong -
Endothelial and Metabolic Dysfunction, and Novel Biomarkers in Diabetes, Hypertension, Dyslipidemia and Estrogen Deficiency, Endothelium - derived Contracting Factors in the Regulation of Vascular Tone, Adipose Tissue Regulation of Vascular Function in Obesity, Diabetes and Hypertension, Pharmacological Characterization of New Anti-diabetic and Anti-hypertensive Drugs, Hypotensive and antioxidant Actions of Biologically Active Components of Traditional Chinese Herbs and Natural Plants including Polypehnols and Ginsenosides Adriaan P. IJzerman, The Netherlands - G protein - coupled receptors; allosteric modulation; binding kinetics Michael F Jarvis, USA - Purines and Purinergic Receptors and Voltage-gated ion channel (sodium and calcium) pharmacology Pain mechanisms Research Reproducibility Bong - Kiun Kaang, Korea - G protein - coupled receptors; Glutamate receptors; Neuropsychiatric disorders Eamonn Kelly, Prof, UK - Molecular Pharmacology of G protein - coupled receptors, in particular opioid receptors, regulation of GPCRs by kinasis and arrestins Terry Kenakin, USA - Drug receptor pharmacodynamics, receptor theory Janos Kiss, Hungary - Neurodegenerative disorders, Alzheimer's disease Stefan Knapp, Germany - Rational design of highly selective inhibitors (so call chemical probes) targeting protein kinases as well as protein interaction inhibitors of the bromodomain family Andrew Knight, UK Chris Langmead, Australia - Drug discovery, GPCRs, neuroscience and analytical pharmacology Vincent Laudet, France (Past Core Member)- Evolution of the Nuclear Receptor / Ligand couple Margaret R. MacLean, UK - Serotonin, endothelin, estrogen, microRNAs and pulmonary hyperten Neil Marrion, UK - Calcium - activated potassium channels, neuronal excitability Fiona Marshall, UK - GPCR molecular pharmacology, structure and drug discovery Alistair Mathie, UK - Ion channel structure, function and regulation, pain and the nervous system Ian McGrath, UK - Adrenoceptors; autonomic transmission; vascular pharmacology Graeme Milligan, UK - Structure, function and regulation of G protein - coupled receptors Richard Neubig, USA (Past Core Member)- G protein signaling; academic drug discovery Stefan Offermanns, Germany - G protein - coupled receptors, vascular / metabolic signaling Richard Olsen, USA - Structure and function of GABA - A receptors; mode of action of GABAergic drugs including general anesthetics and ethanol Jean - Philippe Pin, France (Past Core Member)- GPCR - mGLuR - GABAB - structure function relationship - pharmacology - biophysics Helgi Schiöth, Sweden David Searls, USA - Bioinformatics Graeme Semple, USA - GPCR Medicinal Chemistry Patrick M. Sexton, Australia - G protein - coupled receptors Roland Staal, USA - Microglia and neuroinflammation in neuropathic pain and neurological disorders Bart Staels, France - Nuclear receptor signaling in metabolic and cardiovascular diseases Katerina Tiligada, Greece - Immunopharmacology, histamine, histamine receptors, hypersensitivity, drug allergy, inflammation Georg Terstappen, Germany - Drug discovery for neurodegenerative diseases with a focus
on AD Mary Vore, USA - Activity and regulation of expression and function of the ATP - binding cassette (ABC) transporters
This
effect on cell survival was not
endothelial cell - specific, since IC50 values for kahweol treatment of several human tumoral
cell lines were similar to those obtained for HUVEC (results not shown).
Concerning the apoptosis assay, the negative
effect on endothelial (HUVEC)
cells is in agreement with our results in quail CAM.
Three recent experimental studies focused
on low consumption / exposure.949596 In one study, 29 smokers each consumed a single cigarette, immediately after which they had a significant decrease in blood vessel output power and significant increase in blood vessel ageing level and remaining blood volume 25 minutes later, as markers of atherosclerosis.94 In another study, human coronary artery
endothelial cells were exposed to the smoke equivalent to one cigarette, which led to activation of oxidant stress sensing transcription factor NFR2 and up - regulation of cytochrome p450, considered to have a role in the development of heart disease.95 These
effects were not seen when heart
cells were exposed to the vapour from one e - cigarette.95 A study exposed adult mice to low intensity tobacco smoke (two cigarettes) for one to two months and found adverse histopathological
effects on brain
cells.96
We show for the first time that kahweol is an anti-angiogenic compound with inhibitory
effects in two in vivo and one ex vivo angiogenesis models, with
effects on specific steps of the angiogenic process:
endothelial cell proliferation, migration, invasion and tube formation
on Matrigel.
In this prospective, open and non-randomized study, the
effect of alpha - lipoic acid
on the progression of
endothelial cell damage and the course of diabetic nephropathy, as assessed by measurement of plasma thrombomodulin and urinary albumin concentration (UAC), was evaluated in 84 patients with diabetes mellitus over 18 months.
Effect of Alpha - lipoic Acid
on the Progression of
Endothelial Cell Damage and Albuminuria in Patients with Diabetes Mellitus: An Exploratory Study Diabetes Res Clin Pract 2001 (Jun); 52 (3): 175 — 183 Oxidative stress plays a central role in the pathogenesis and progression of late microangiopathic complications (diabetic nephropathy) in diabetes mellitus.