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As a part of our continuing efforts
2022-07-21

As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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Free fatty acids FFAs which are
2022-07-21

Free fatty acids (FFAs), which are obtained from dietary fat or endogenous synthesis, function as nutrients and signaling molecules. Studies have shown that free fatty BRD-6125 mg receptors 1–4 which are G-protein coupled receptors, bind free fatty acids and serve as receptors for these FFAs. Short
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We have presented evidence that only muscle FBPase is
2022-07-21

We have presented evidence that only muscle FBPase is detectable within HL-1 cells. This is consistent with past findings of the Eschrich's group, which showed that in rat heart AP1903 expression of FBPase is almost exclusively limited to the muscle isozyme [3]. Results of our preliminary experimen
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In the past two decades studies of the
2022-07-21

In the past two decades, studies of the non-B cell-derived Ig, including cancer cell-derived IgG, have been predominately facilitated by general anti-human Ig antibodies, which do not distinguish the non-B Ig from classical Ig derived from B cells. Due to this caveat, it remains obscure about whethe
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br Introduction Stroke is the second
2022-07-20

Introduction Stroke is the second cause of death worldwide and the first cause of acquired motor disability in adults [1], [2]. In sub-Saharan Africa, stroke is the first cause of admission in neurology departments [3]. In Cameroon, the in-hospital mortality of stroke is estimated at 26.8% [4]. A
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Histamine which was used as the agonist
2022-07-20

Histamine, which was used as the agonist, had low potencies in our functional experiments when compared to its affinity from binding studies (e.g. Lim et al., 2005). This phenomenon is related to the fact that the coupling of the presynaptic receptor to the transduction machinery and the final funct
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Saikosaponin A synthesis Furthermore we observed a striking
2022-07-19

Furthermore, we observed a striking difference between BR 11257 and activators from the dicarboxylic Saikosaponin A synthesis type in thermofluor measurements on thermostability. The dicarboxylic acids cinaciguat [30] and BAY 60-2770 (see Fig. 3) induced a significant melting temperature increase o
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Accessibility and physico chemical features of cysteine resi
2022-07-19

Accessibility and physico-chemical features of cysteine residues define their redox-reactivity and the 3-dimensional structure of GSNOR allows to identifying such surface-exposed, redox-sensitive cysteine residues. GSNOR crystal structures are available from human (Protein Data Bank code: 1MP0), tom
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The difference in the expression of functional
2022-07-19

The difference in the expression of functional FFARs between neutrophils and monocytes/macrophages suggests that the role of FFA2R may be restricted to the very early phase of acute inflammation where neutrophils are dominating players called into action, whereas GPR84 may have a broader functional
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Introduction The onset of uterine labor is the
2022-07-19

Introduction The onset of uterine labor is the culmination of a gradual uterine activation wherein physiological inflammation induces a common prolabor pathway characterized by increased myometrial contractility, weakening of fetal membrane integrity, and cervical ripening. Pathological proinflamma
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The opposite modulation observed for circulating LPI levels
2022-07-19

The opposite modulation observed for circulating LPI levels and WAT GPR55 Arylquin 1 receptor by nutritional status suggests that increased levels of LPI may down-regulate the expression of its receptor in WAT, whereas in conditions of low serum LPI levels, the expression of GPR55 is stimulated. Ho
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Propylthiouracil Armed with this knowledge we looked at
2022-07-19

Armed with this knowledge, we looked at ways to reduce the log of through nitrogen incorporation while still maintaining potency via installation of ortho substituents such as chloro, methyl, bromo, and thiomethyl (). In general, pyridine analogs were less active ( vs ; vs ; vs ) than their simpl
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br Materials and Methods br Results br Discussion
2022-07-19

Materials and Methods Results Discussion A model of seizure and excitotoxicity induced by neonatal MSG administration was described recently (19) in which extracellular glutamate increased after the first and second MSG administrations were observed, the greatest increase seen following the
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Tolvaptan Transmembrane AMPA receptor regulatory proteins TA
2022-07-19

Transmembrane AMPA receptor regulatory proteins (TARPs) are a relatively newly discovered protein family. Prototypic TARP, stargazin, was found by a spontaneous mutation in ataxic stargazer mouse line as a homologous protein to γ1 calcium channel subunit (Letts et al., 1998). The role of stargazin i
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br SMO antagonists pitfalls and
2022-07-19

SMO antagonists: pitfalls and limitations The first Hh inhibitor discovered was cyclopamine, a naturally occurring alkaloid isolated from Veratrum californicum[21], which inactivates SMO by directly binding to its hepathelical bundle. Nevertheless, cyclopamine has shown several limitations as a d
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