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Young et al described the role of
2022-08-03
Young et al. [40] described the role of adenine monophosphate-activated protein kinase (AMPK) in the translocation of GLUT4 in the heart. The AMPK is activated during muscle contraction [74] by converting AMP to ATP. The adenosine analog, 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), is a c
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Optimization of the tetrahydroindazole series led to the dis
2022-08-03
Optimization of the tetrahydroindazole series led to the discovery of two moderately potent γ-secretase modulators, 2-cyclobutane and 2-hydroxy-2-methylpropane which were subsequently evaluated in a kinetic aqueous solubility assay. Unfortunately, neither analog demonstrated improved solubility ()
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Nicastrin is heavily glycosylated contributing KDa to the mo
2022-08-03
Nicastrin is heavily glycosylated, contributing 40–70KDa to the molecular weight of human γ-secretase. Among the 16 predicted N-linked glycosylation sites in the ECD, 11 have been unambiguously identified. The glycans appear to mostly stabilize the local structure, thus contributing to the folding a
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Some but not all GSIs inhibit signal peptide
2022-08-03
Some, but not all, GSIs inhibit signal peptide peptidases as well, though this has not been systemically studied [36], [41]. When considering biological activities of various GSIs this is an important and understudied caveat that could influence both biological response as well as potential toxiciti
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Berbamine hydrochloride australia The current gold standard
2022-08-03
The current gold standard for diagnosing BAM or BAD is the measurement of BA turnover rate with radiolabelled tauroselcholic (75selenium) Berbamine hydrochloride australia (also known as the SeHCAT retention test). SeHCAT test involves the use of a synthetic analogue of naturally occurring conjugate
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depicts the synthesis of series with a four step
2022-08-03
depicts the synthesis of series with a four-step sequence. First, the commercially available 4-hydroxybenzaldehyde () was condensed with 2-bromoethanol through Mitsunobu reaction to give the key intermediate (). Next, conventional nucleophilic substitution reaction with the privileged structures (
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br Conflict of interest br
2022-08-03
Conflict of interest Acknowledgments The research was funded by the Major Programs of Pharmaceutical research project of Jiangsu Province (Q2018044). Introduction Lipids are important regulators of cell death. In mammalian cells, both apoptotic and non-apoptotic cell death pathways can be
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Neuropathic pain NP is a
2022-08-03
Neuropathic pain (NP) is a chronic pain caused by lesion or disease affecting any part of the nervous system leading to clinical conditions ranging from painful neuropathy to poststroke central pain. Anticonvulsant drugs, Gabapentin and Pregabalin, acting on αδ subunit-containing voltage-dependent c
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SCH is a H R receptor
2022-08-03
SCH-497079 is a H3R receptor antagonist introduced by Schering-Plough, without any publicized pharmacological and structural information. A Phase II clinical trial assessment of SCH-497079 on weight has been completed in a multicenter, randomized, parallel-group and placebo-controlled study in obese
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Mapping PPI networks is challenging
2022-08-03
Mapping PPI networks is challenging, as it is difficult to express and purify large variaties of Terbinafine mg in sufficient quantities to allow the study of interactions between them. Membrane-bound proteins are particularly difficult to purify in functional form due to their amphiphilic nature. F
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The mode of action of
2022-08-02
The mode of action of m-Tyr has not been fully recognized. The primary/basic mechanism of action of m-Tyr is thought to be associated with the incorporation of this NPAA into the structure of proteins resulting in formation of dysfunctional proteins [11], [12]. m-Tyr is incorporated into proteins in
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Several studies have sought a
2022-08-02
Several studies have sought a cross-relationship between commensal bacteria-derived metabolites and the Gprs (Blad et al., 2012). Gpr81 is expressed primarily in adipocytes, and hence, lactate-Gpr81 interaction inhibits lipolysis (Cai et al., 2008, Liu et al., 2009). Lactate reduced inflammation by
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br Acknowledgments br Introduction Manipulating target prote
2022-08-02
Acknowledgments Introduction Manipulating target protein expression via either induction or suppression of gene expression is a powerful technology that has been widely used in the recent past in the field of neurobiology, both to study the pathophysiological significance of a target gene and
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12-O-tetradecanoyl phorbol-13-acetate To maintain low Glu co
2022-08-02
To maintain low Glu concentrations in the synaptic cleft below the affinity of its receptors, this amino 12-O-tetradecanoyl phorbol-13-acetate is rapidly removed from the extracellular space by a family of sodium-dependent high-affinity transport systems located mainly in the plasma membrane of per
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We also demonstrated that inhibition of NAAG hydrolysis to
2022-08-02
We also demonstrated that inhibition of NAAG hydrolysis to suppress glutamate production through a GCPII inhibitor is a viable target for cancer therapy. GCPII is also known as N-acetyl-L-aspartyl-L-glutamate peptidase I (NAALADase I) or NAAG peptidase (Pinto et al., 1996), and its increased express
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