Abstract:
:Inhibition of angiogenesis involves blocking of tyrosine kinases (TK) implicated in signalling of vascular endothelial growth factor receptors (VEFGR). The inhibition of TK results in a disruption of Ras/Raf/MEK/ERK1/2 and PI3K/Akt signalling pathways. We evaluated recently developed TK inhibitor 22SYM and compared its anti-angiogenic effects with an approved multitargeted TK inhibitor sunitinib L-malate (sunitinib). Both compounds significantly inhibited migration and proliferation of human umbilical vein endothelial cells and ERK1/2 and Akt phosphorylation induced by VEGF. The lower inhibitory activity of 22SYM probably reflects its lower bioavailability and higher specific binding to VEGFR2 TK, which may decrease its potential side effects and toxicity in comparison with sunitinib.
journal_name
Gen Physiol Biophysjournal_title
General physiology and biophysicsauthors
Moravčík R,Stebelová K,Boháč A,Zeman Mdoi
10.4149/gpb_2015055subject
Has Abstractpub_date
2016-10-01 00:00:00pages
511-514issue
4eissn
0231-5882issn
1338-4325journal_volume
35pub_type
杂志文章abstract::Charcot-Marie-Tooth disease (CMT) and related peripheral neuropathies are the most commonly inherited neurological disorders in humans, characterized by clinical and genetic heterogeneity. The most prevalent clinical entities belonging to this group of disorders are CMT type 1A (CMT1A) and hereditary neuropathy with l...
journal_title:General physiology and biophysics
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doi:10.4149/gpb_2011_04_379
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journal_title:General physiology and biophysics
pub_type: 杂志文章,评审
doi:
更新日期:1996-10-01 00:00:00
abstract::7,8-Dihydroxyflavone (7,8-DHF) is a natural flavonoid compound that act as Trk-B agonist. 7,8-DHF is also a potent antioxidant. When applied systematically, 7,8-DHF can pass through blood-brain barrier and exhibit potential therapeutic effects in several animal models of neurodegenerative disorders. This study investi...
journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:10.4149/gpb_2020022
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abstract::Phosphorylation of P-glycoprotein (PGP) by some protein kinases may play an important role in the regulation of its drug transport activity, and may also be important for the development of multidrug resistance (MDR) phenotype. In the present study we investigated the expression of three groups of mitogen-activated pr...
journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:
更新日期:1999-03-01 00:00:00
abstract::Aquaporin attracted attention not only of physiologists and biophysicists, but also of chemical engineers. Here we critically analyze a paper describing aquaporin-based artificial membranes, suggested for forward osmosis-based water purification (Wang et al. 2012, Small 8, pp. 1185-1190). Related papers published late...
journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:10.4149/gpb_2013058
更新日期:2013-12-01 00:00:00
abstract::We studied the involvement of O2, pH and low molecular thiols in H2S-induced decomposition of S-nitrosoglutathione (GSNO). The GSNO decomposition - •NO release was evaluated by UV-VIS spectroscopy and Griess assay. The H2S donor Na2S was used. O2 slightly increased, but was not necessary for the H2S-induced GSNO decom...
journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:10.4149/gpb_2013026
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journal_title:General physiology and biophysics
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doi:10.4149/gpb_2017020
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journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:
更新日期:2007-06-01 00:00:00
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journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:
更新日期:1986-06-01 00:00:00
abstract::The character of structural changes in thylakoid membranes caused by temperature variation was investigated. Experiments were performed on maize leaf segments in vivo and in a closed temperature cycle 24-50-24 degrees C. Two biophysical methods were used for detection: luminescence and EPR. Arrhenius plots of delayed ...
journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:
更新日期:1993-02-01 00:00:00
abstract::Voltage-activated calcium channels can be divided into two subgroups based on their activation threshold, low-voltage-activated (LVA) and high-voltage-activated (HVA). Auxiliary subunits of the HVA calcium channels contribute significantly to biophysical properties of the channels. We have cloned and characterized mem...
journal_title:General physiology and biophysics
pub_type: 杂志文章,评审
doi:
更新日期:2005-06-01 00:00:00
abstract::Low-conductance chloride channel from skeletal muscle SR vesicles of the crayfish Astacus fluviatilis was incorporated into planar lipid bilayers and its basic characteristics were investigated. The channel has a relatively low unitary conductance of 26 pS in symmetrical 160 mmol/l choline-chloride. The dependence of ...
journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:
更新日期:1991-12-01 00:00:00
abstract::Results of studies on the modulation of skeletal muscle contraction by phosphorylation of myosin regulatory light chains and by exchange of magnesium for calcium in myosin heads were reviewed. The polarized fluorescence method was used in these studies, and conformational changes of contractile proteins accompanying m...
journal_title:General physiology and biophysics
pub_type: 杂志文章,评审
doi:
更新日期:1991-06-01 00:00:00
abstract::The plasma membrane H(+)-ATPase of Neurospora has been reconstituted into planar lipid bilayer membranes by means of the vesicle-fusion technique described by Finkelstein and his collaborators (Zimmerberg et al., 1980; Cohen et al., 1980, 1984; Akabas et al., 1984). Enzyme was first transferred from isolated plasma me...
journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:
更新日期:1993-10-01 00:00:00
abstract::A model for the dynamics of quasi-1D lipid structures in biological membranes is proposed. The model takes into account interactions between the lipid heads and hydro-carbon chains, the description of their relaxation dynamics being based on the phenomenological Ginzburg-Landau approach. It is shown that in lateral li...
journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:
更新日期:1997-12-01 00:00:00
abstract::Semiserial sections of lung capillaries of seven rabbits were examined for megakaryocytes. Triads of serial sections of each lobe were examined, and megakaryocyte counts per cm2 were determined. Median megakaryocyte count was determined for each lobe. The lobal values were used to calculate the was determined for each...
journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:
更新日期:1987-08-01 00:00:00
abstract::Hyperglycemia impairs oxidative capacity in skeletal muscle. Muscle oxidative capacity is regulated by peroxisome proliferator-activated receptor-γ co-activator-1α (PGC-1α). Transcutaneous carbon dioxide (CO2) enhances PGC-1α expression in skeletal muscle. Therefore, the aim of this study was to clarify the effects of...
journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:10.4149/gpb_2018048
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journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:
更新日期:2006-09-01 00:00:00
abstract::In this study possible connection between radiofrequency exposure (RF) and development of oxidative stress was investigated by measuring impairment in cellular oxidation-reduction balance immediately after RF exposure. Fibroblast cells V79 were exposed for 10, 30 and 60 minutes to 1800 MHz RF radiation. Electric field...
journal_title:General physiology and biophysics
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doi:10.4149/gpb_2017007
更新日期:2017-10-01 00:00:00
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journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:10.4149/gpb_2009_04_371
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abstract::Various techniques have been used (UV absorbance and fluorescence spectroscopy, polarised UV fluorescence microscopy, viscosimetry, electrophoresis and isoelectric focusing, superprecipitation, etc.) As suggested by several parameters, denervation interferes with the structure of actin by producing local conformation ...
journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:
更新日期:1987-06-01 00:00:00
abstract::Effects of six thiol reagents with different physico-chemical properties were tested on the Na+-dependent 45Ca2+ transport into the rat brain microsomal membrane vesicles. The mercurials p-chlormercuribenzoate and Mersalyl effectively inhibited 45Ca2+ uptake with IC50 values in the order of 10(-4) mol X l-1 in the med...
journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:
更新日期:1987-04-01 00:00:00
abstract::A mechanical model of heart muscle is proposed which includes rheological equations and equations for Ca-troponin interaction, for the dependences of the number of myosin cross-bridges on the length of sarcomere and on the speed of motion. The main assumption of the model is the dependence of the troponin affinity to ...
journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:
更新日期:1990-06-01 00:00:00
abstract::Malate dehydrogenases (MDH, L-malate:NAD oxidoreductase, EC 1.1.1.37), catalyze the NAD/NADH-dependent interconversion of the substrates malate and oxaloacetate. This reaction plays a key part in the malate/aspartate shuttle across the mitochondrial membrane, and in the tricarboxylic acid cycle within the mitochondria...
journal_title:General physiology and biophysics
pub_type: 杂志文章,评审
doi:
更新日期:2002-09-01 00:00:00
abstract::Aiming at making the Münch model more adequate to the biological reality we introduce certain modifications and complements. Considering the model within the framework of so-called integrated system of long-distance water transport in plants we present a quantitative analysis based on the Kedem-Katchalsky formalism. A...
journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:
更新日期:2001-06-01 00:00:00
abstract::Although high-intensity electric fields (HEF) application is currently the only effective therapy available to terminate ventricular fibrillation, it may cause injury to cardiac cells. In this study we determined the relation between HEF pulse length and cardiomyocyte lethal injury. We obtained lethality curves by sur...
journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:10.4149/gpb_2015047
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journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:
更新日期:2003-12-01 00:00:00
abstract::Mitochondrial nucleoids (hereafter nucleoids) contain genetic information, mitochondrial DNA, prerequisite for mitochondrial functioning, particularly information required for mitochondrial electron transport. To understand nucleoid functioning, it is imperative to know its ultrastructure and dynamics in the context o...
journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:10.4149/gpb_2016008
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journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:
更新日期:2006-06-01 00:00:00
abstract::Although numerous studies have shown the existence of various types of ion conductance in antral part of gastric fundus mucosa epithelia of amphibian, practically no data are available on ion conductance in higher animal species. Present experiments were undertaken to check the possible existence of ion conductance in...
journal_title:General physiology and biophysics
pub_type: 杂志文章
doi:
更新日期:1995-12-01 00:00:00