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Recently Bristol Myers Squibb and Merck reported
2022-03-12

Recently, Bristol-Myers Squibb and Merck reported their GPR40 agonist research focused on the modification of α,β-position of phenylpropionic Cy3.5 NHS ester (non-sulfonated) derivatives. For example, in recent published patent applications, Bristol-Myers Squibb claimed the pyrrolidine and dihydrop
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br Introduction In addition to
2022-03-12

Introduction In addition to glucose, which is the foremost stimulator of insulin secretion in beta-cells, other nutrients such as free fatty acids (also called non-esterified fatty acids, NEFA) contribute to glucose-stimulated insulin secretion (GSIS). Glucose triggers the processes leading to in
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As a part of our continuing efforts
2022-03-12

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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Curcumol receptor By measuring the accumulation of unprenyla
2022-03-12

By measuring the accumulation of unprenylated Rap1a as a surrogate marker for the inhibition of FPPS [8], [9], [10], [11], we found that upregulation of FPPS expression in Hela cells reduced the accumulation of unprenylated Rap1a in response to 24h' treatment with 0–50μM ZOL. As expected, cells cult
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In this investigation the NlVg relative transcript level
2022-03-11

In this investigation, the NlVg relative transcript level was also prompted by 1.3-fold compared to the untreated control in the TZP treatment, while there was a slight increase of 13.6% for NlVgR (Fig. 7A and B). One underlying molecular mechanism for the TZP-induced fecundity is the significant up
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Menadione sale Following our initial observation of an unexp
2022-03-11

Following our initial observation of an unexpected increase in the maximal rates of cGMP formation by NO-stimulated sGC in the presence of cytosolic PCA preparations [15], we attempted to purify, identify and characterize the responsible protein(s). The purification protocol described in the present
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br All platelet agonists acting
2022-03-11

All platelet agonists, acting through specific receptors and triggering different signaling pathways, activate phospholipases (PLCß or PLCγ) and the subsequent messengers inositol 1,4,5-trisphosphate (IP3) and 1,2 diacylglycerol which activate inositol 1,4,5-trisphosphate (IP3) receptors (IP3R) or
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The isoenzyme hGSTP is an attractive drug
2022-03-11

The isoenzyme hGSTP1-1 is an attractive drug target due to its high levels of disease association (target validation) and druggability (target tractability) properties [5,6,[17], [18], [19], [20], [21]]. hGSTP1-1 functions as a homodimer protein [18]. Each monomer has two domains, an α/β domain (N-t
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br GSNOR regulates SA synthesis and SA signalling The phenol
2022-03-11

GSNOR1 regulates SA synthesis and SA signalling The phenolic metabolite salicylic Calpain Inhibitor II, ALLM (SA) is a powerful immune activator in plants. Moreover, mutations that disable SA biosynthesis or transgenes that result in its depletion compromise both resistance (R) gene-mediated and
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Doxorubicin Strengths The primary feature of GPR
2022-03-11

Strengths The primary feature of GPR119 agonists resides in their dual mechanism of action in regulating blood glucose 1, 2, 3, 15. GPR119 agonists stimulate GLP-1 release from intestinal L Doxorubicin as well as glucose-dependent insulin secretion and insulin promoter activity enhancement in panc
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Proteinase K mg The inhibition of NSAIDs towards GLOI provid
2022-03-11

The inhibition of NSAIDs towards GLOI provides a direction for the development of novel effective GLOI inhibitors. Although the inhibitory activity of indomethacin was determined and the interactions between it Proteinase K mg and GLOI were probed by NMR titration experiments, no detailed inhibitor
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Memantine hydrochloride FPG had no consistent activity
2022-03-11

FPG-2 had no consistent activity in reducing G→T transversions. Gao and Murphy [2] earlier reported that FPG-2 had a limited amount of activity in vitro on depurinated, UV-treated, and methylene-blue-treated DNA (but not on 8-oxo-G-containing oligonucleotides). FPG-2 contains the N-terminal domain a
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br Conclusion Membrane transporters remain
2022-03-11

Conclusion Membrane transporters remain relatively understudied in human disease, especially TBI (Cesar-Razquin et al., 2015), and considerably less is known in terms of expression, function and substrates of membrane transporters in pediatric patients. However, their importance in maintaining Di
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br Author contribution br Declaration of interest br Acknowl
2022-03-11

Author contribution Declaration of interest Acknowledgements This work was supported by National Natural Science Foundation of China (Grants 81473093) and State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM1601ZZ-02). Introduction Diabetes represents a majo
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Boswellia papyrifera Del Hochst mostly grows in Sudanian and
2022-03-11

Boswellia papyrifera (Del.) Hochst., mostly grows in Sudanian and Sahelian regions and their oleo-gum resin is used medically in treatment of rheumatism, menorrhagia, amenorrhoea, vaginal infections, ulcers, sores, polyuria, syphilis, bronchitis, scrofulous affections, inflammations, asthma, diarrhe
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