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br Chemistry The methylsulfanyl dihydro H
2022-05-31

Chemistry The 8-methylsulfanyl-4,5-dihydro-1H-thieno[3,4-g]isothiadizaole scaffold was synthesized from commercially available 1,3-dioxolane-2,1′-cyclohexane-4-one 17 (Scheme 1). The isothiadizaole ring was formed with SOCl2 from N-carboxamide hydrazine imine 19, which was prepared from 17 and hy
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In mammals meiotic maturation is the process that couples co
2022-05-31

In mammals, meiotic maturation is the process that couples completion of MI with the acquisition of developmental competence to support fertilization (Figure 1). In females there are several hallmark maturation events that are linked to the cell cycle. First, meiosis is not continuous, it is initiat
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Protein structures determined in high resolution by X
2022-05-31

Protein structures determined in high resolution by X-ray crystallography and NMR techniques provide wealth of structural information on intra-domain and inter-domain protein interactions of small sized proteins. In addition, cryo-EM often provides low resolution structures of multi-component protei
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Studies utilising GPR mice however report different effects
2022-05-31

Studies utilising GPR55−/− mice, however, report different effects of GPR55 on body weight and insulin sensitivity. Genetic deletion of GPR55 appears to have no effect on overall body weight 5, 6, 7. However, one of these studies found increased fat deposition and insulin resistance in GPR55−/− mice
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Little is known about the role of GPR
2022-05-31

Little is known about the role of GPR35 in physiology and pathology. Using GPR35 knockout and wild-type mice showed that GPR35 activation by KYNA improves energy metabolism and inflammation, while demonstrated that GPR35 plays an important role in the development of angiotensin II-induced hyperten
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The differential tissue and ligand dependent signaling descr
2022-05-31

The differential tissue- and ligand-dependent signaling described here has important implications for the therapeutic potential of synthetic GPR109A agonists for the treatment of atherosclerosis. The failure of MK-0354, a biased, partial GPR109A agonist, to activate signaling pathways upstream of va
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Up to now many UDG assays have been reported based
2022-05-31

Up to now, many UDG assays have been reported based on the design of dU-containing substrate DNA, which can be roughly divided into two categories according to the sensing mechanisms. One type of UDG assays are simply based on the physical or chemical property changes of the substrate accompanied wi
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The typical pharmacophore for GPR
2022-05-31

The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors
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Pyrogallol is an organic gallic acid converting compound tha
2022-05-31

Pyrogallol is an organic gallic acid-converting compound that has three hydroxyl groups and belongs to the phenol family. Gallic Regorafenib hydrochloride synthesis is obtainable from the galls and barks of various trees, and a simple heating procedure can induce the decarboxylation of gallic acid t
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tcY-NH2 An important difference between glucokinase and the
2022-05-31

An important difference between glucokinase and the other hexokinases is that it has a much lower affinity for glucose, such that it is not saturated at physiological blood glucose concentrations (Wilson, 1995, Wilson, 1997, Wilson, 2003, Wilson, 2004, Cárdenas et al., 1998). In addition, glucokina
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Introduction Human pathogenic Leishmania protozoa comprise d
2022-05-31

Introduction Human pathogenic Leishmania protozoa comprise 20 different species that are distributed throughout the world and cause the disease leishmaniasis [1]. Transmission primarily occurs through the bite of a female sand fly and clinical manifestations of the disease span from cutaneous lesio
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The manner in which various residue side chains are oriented
2022-05-31

The manner in which various residue side chains are oriented in the active site of HsHxKIV was a driving factor for why glucosamine analogues could not bind, as we previously proposed [16]. These compounds would have difficulty managing access into the active site based on residue P153 in addition t
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One may carefully evaluate the concept
2022-05-31

One may carefully evaluate the concept ‘pancreas derived GLP-1′ as this may dependent on the specificity of the Cytidine 5-triphosphate used in immunohistochemistry or radiommunoassays. If either a side-viewing antibody or a C-terminal wrapping antibody raised against GLP-1 is applied one may also
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The potential therapeutic actions of GHSR in the central
2022-05-31

The potential therapeutic actions of GHSR in the central nervous system has been in the limelight lately. Peripheral administration of GHSR agonists have been shown to inhibit oxidative stress, apoptosis, proinflammatory cytokine production, microglia activation, mitochondrial dysfunction, and excit
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Data were collected using a Powerlab and
2022-05-31

Data were collected using a Powerlab and Chart 5 software (ADInstruments, Bella Vista, NSW, Australia) and were analysed using GraphPad Prism 5 (GraphPad Software, San Diego, CA). Responses to ghrelin receptor agonists in phenylephrine, methoxamine, endothelin-1, U46619 and 60mM [K+] contracted vess
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