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br Acknowledgments I thank Takeshi Sakaba
2021-10-11
Acknowledgments I thank Takeshi Sakaba for critical reading of the manuscript and helpful comments. This work was supported by JSPS/MEXT KAKENHI Grant Numbers 17K19466, 17H03548. Introduction The oral route of drug application is the main route in pharmacology since it is easy to handle and o
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In the Toc Regulator Mode Fig recognition of the transit
2021-10-11
In the “Toc34 Regulator Mode” (Fig. 6), recognition of the transit peptide by Toc159 monomer (step 4) leads to heterodimer-formation [18]. Subsequently, preprotein interaction with the Toc34G homodimer (step 1) regulates the Toc34G homodimer (step 2, 3). However, this mode requires a parallel induct
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The crystal structures of plant class ADH GSNOR
2021-10-11
The crystal structures of plant class ADH3/GSNOR from Arabidopsis thaliana (AtGSNOR) and Solanum lycopersicum cv. Amateur (SlGSNOR) with bound substrates and cofactors revealed important differences between plant and human enzyme, namely within the substrate-binding pocket. GSNOR are unusually homod
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Several studies have found that GPR possesses
2021-10-11
Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected Ki8751 expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (Rimon
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Strengths The primary feature of GPR agonists resides
2021-10-11
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 toll like receptor as well as glucose-dependent insulin secretion and insulin promoter activity enhancement
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Doripenem Hydrate synthesis As part of our discovery efforts
2021-10-11
As part of our discovery efforts searching for small molecule GPR119 agonists, we analyzed active pharmacophores of known agonists from the literature, and found that -methylsulfonylphenyl and substituted 4-hydroxyl piperidine are common fragments. In our initial efforts, we linked these two fragme
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As the material for in
2021-10-11
As the material for in silico experiments we used an amino Altretamine synthesis sequence of a fragment of HIV1 surface glycoprotein gp120 corresponding to its less mutable B-cellular epitope: NMWKNNMVEQMHEDIISLWDQ. This sequence is the same as the sequence of the NQ21 and the biotin-NQ21 peptides
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The HRTOF MS of showed a quasi molecular ion
2021-10-11
The HRTOF-MS of showed a quasi-molecular ion peak at / 525.3044 [M+Na], corresponding to a quasi-molecular formula of CHNONa (Calcd for CHNONa: 525.3053). IR absorptions at 1680 and 1522cm suggested the presence of amide functions. Based on an analysis of 1D and 2D NMR spectra, the presence of one
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Previous studies have demonstrated that cannabinoid
2021-10-11
Previous studies have demonstrated that cannabinoid potentiation of GlyR α3 subunits contributes to cannabinoid-induced analgesia. For instance, Dehydroxylcannabidiol (DH-CBD), a chemically modified cannabinoid, can alleviate acute pain and chronic inflammatory pain by targeting spinal α3 GlyRs (Xio
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br Regulation of Glu transporters The pivotal role of
2021-10-11
Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino somatostatin agonist calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These include
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However no reviews was focused
2021-10-11
However, no reviews was focused on all the glutamate heteroreceptor complexes and how to understand why some were formed and not others in the glutamate synapses and their extrasynaptic regions. These receptor complexes are present on the glutamate nerve terminals and the dendritic spines on which t
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The fine interplay among post translational
2021-10-11
The fine interplay among post-translational modifications and intersection with other pathways, such as PI3K–AKT, has a crucial role in the regulation of GLI activity and in the generation of their repressor forms 40, 41, 42. In addition to β-TrCP, for example, other E3 ligases belonging to the real
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br Materials and methods br Results
2021-10-11
Materials and methods Results shows serum FSH, LH, oestradiol and progesterone values in the two cycles from day 2 to day 10. Basal values of these hormones on day 2 (before any intervention) were similar in the two cycles. Thereafter, FSH values did not differ significantly between the two c
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Developmental studies have reported that some subunits
2021-10-09
Developmental studies have reported that some subunits of GABAA receptors like α2 and α3 are predominantly expressed during in-utero development, and then substituted for α1 around birth in the rat hippocampus (Brooks-Kayal et al., 2001; Fritschy et al., 1994; Golshani et al., 1997; Kapur and Macdon
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The ability to metastasize is the defining character of a
2021-10-09
The ability to metastasize is the defining character of a cancer and the leading cause for resultant mortality. It is hypothesized that a rare subset of cancer cells, often operationally referred to as “cancer stem cells” (CSCs), are responsible for sustaining cancer metastasis and recurrence [1]. T
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