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The role of ETB clearing receptors has been studied in
2020-01-13
The role of ETB clearing receptors has been studied in detail in endothelial cell–specific ETB knock-out mice. In these animals, clearance of an intravenous Bay 11-7085 of labeled ET-1 was reduced significantly compared with wild-type controls. Importantly, functioning ETB were retained on all other
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Preliminary studies suggest that dimerization of the
2020-01-13
Preliminary studies suggest that dimerization of the AT1 receptor occurred during the biosynthesis in the endoplasmic reticulum before surface expression [27,40], which may explain the presenece of these Protease Inhibitor Cocktail (100X in DMSO, EDTA plus) before the addition of any ligand. Our re
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The isomeric phenyloxazole not only exhibited increased pote
2020-01-13
The isomeric 5-phenyloxazole not only exhibited increased potency against NEP, but also a decreased ACE inhibition thus providing encouraging selectivity. Changing the P1 group from an -propyl to a more polar methoxyethyl at the left hand adenosine receptor antagonist (as seen in compound pairs – an
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Collagen type is the most
2020-01-13
Collagen type 1 is the most abundant extracellular matrix (ECM) protein found in vertebrates. Collagen exerts its role as a load bearing structure and regulator of cell function, only after it has assembled into fibrils., The equilibrium between the synthesis and degradation of collagen fibrils and
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br Significance Our understanding of the
2020-01-13
Significance Our understanding of the ubiquitin biology has been rapidly expanding. The role of the ubiquitin system in the pathogenesis of numerous disease states has increased the interest in finding new strategies to pharmacologically interfere with the enzymes responsible of the ubiquitinatio
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br Materials and Methods br Acknowledgements Authors would l
2020-01-13
Materials and Methods Acknowledgements Authors would like to thank Mr. Pritam Naskar and Mr. Dibya Mukherjee for their help. Authors also acknowledge the help of Mr. Barun Mahata and Dr. Kaushik Biswas, Division of Molecular Medicine, Bose Institute, for human cDNA samples. P.A.B. and A.B.D. w
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A spectrum of therapies came in
2020-01-13
A spectrum of therapies came in order to counter this misfortune, some of them are discussed below. However, the common problem faced by most of these drugs is their emerging resistance after a span of time. Some of the important drugs reported so far are as: Quinine-based antimalarial drugs (Fig. 1
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Introduction DHFR is an important enzyme in both
2020-01-13
Introduction DHFR is an important enzyme in both mammals and microorganism including Mycobacterium tuberculosis (Mtb). It catalyzes folic am 580 conversion to dihydro and tetrahydro folic acid which is a crucial step in folate pathway [1]. Inhibition of folate pathway leads to interruption of thym
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C527 Unlike the CRF receptor the CRF a receptor
2020-01-13
Unlike the CRF1 receptor, the CRF2(a) receptor binds and is activated by agonists with a broad range of potencies. Therefore, we assessed the ability of strong and weak ligands to desensitize retinoblastoma CRF2(a) receptors. Although stresscopin\'s N-terminus is two C527 longer than the N-terminus
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In the current study although
2020-01-11
In the current study, although EP4 agonist was the most effective in relaxing corpus cavernosum, it did not affect the neuronally-mediated relaxation. On the other hand, both alprostadil and iloprost, which were less effective as direct relaxants, potentiated EFS-induced relaxation of rat corpus cav
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N6-Cyclopentyladenosine Crystallographic and NMR based analy
2020-01-11
Crystallographic and NMR-based analyses have revealed that RINGs and U-boxes have a common mode of interaction with E2s (Fig. 2A). The key structural elements are two loop-like regions, which, in the case of RINGs, coordinate Zn. The loops surround a shallow groove formed by the central α-helix. Tog
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These findings further extend our
2020-01-11
These findings further extend our knowledge of how P4 and/or E2 can mediate anxiety and fear responses. Female rats in behavioral estrous and ovx rats administered systemic P4 and/or E2 demonstrated significantly less anxiety in the open field and/or elevated plus maze, compared to diestrous rats, a
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In our previous research we
2020-01-11
In our previous research, we have focused on the discovery of novel VEGFR-2 inhibitors as anti-angiogenesis agents. Numbers of biphenyl-aryl urea incorporated with salicylaldoxime including BPS-7 have been developed as potent and selective VEGFR-2 inhibitors (Fig. 3) [12], [13], [14], [15], [16], [1
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PGE exerts its functions by binding
2020-01-11
PGE2 exerts its functions by binding to different receptors. Four different subtypes of PGE2 receptors are found in mammals and are designated as EP1-4. These are G-protein coupled receptors that belong to a family of seven rhodopsin-like transmembrane spanning receptors. They are structurally diffe
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CFTRinh-172 br Experimental Procedures br Author
2020-01-11
Experimental Procedures Author Contributions Acknowledgments Introduction The intestinal mucosal barrier surface is constantly exposed to food antigens, beneficial microbes, pathogens, and a multitude of other environmental stimuli (Turner, 2009). Innate lymphoid CFTRinh-172 (ILCs) are k
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