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IC is a rat mAb specifically binding to insulin
2021-12-20
IC2 is a rat mAb specifically binding to insulin granula [127,128]. Although this mAb was discovered 30 years ago, it has only recently been used for β-cell imaging in vivo. Moore et al. used this mAb for β-cell imaging in 2001 [129]. After DTPA conjugation, IC2 was labeled with 111In. Both in vitro
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Based on work from our labs with mGlu
2021-12-20
Based on work from our labs with mGlu NAMs, and the ability of [3.3.0] systems, such as the octahydropyrrolo[3,4-]pyrrole, to effectively mimic piperazines, we focused our attention on the potential bioisoteric replacement of the [3.1.0] system of and , as well as the piperidine of , with a [3.3.0]
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FPG had no consistent activity
2021-12-20
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 Materials methods br Results FAS
2021-12-20
Materials & methods Results FAS c.-671AA, AG and GG genotypes and A and G dopamine receptor antagonist frequencies were similar in both patients with FMF and healthy control groups, and no significant difference was found (P>0.05, Table 1). The frequency of TC genotype in FASLG in the healthy
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Together the epigenetic interplay revealed in this study ena
2021-12-20
Together, the epigenetic interplay revealed in this study enabled us to expand the therapeutic potential of EZH2is from hematological malignances to solid tumors. In solid tumors, EZH2i-driven transcriptional changes are shown to be dispensable of H3K27me-regulated transcriptional network. Instead,
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br An approach for the key challenges facing forensic
2021-12-18
An approach for the key challenges facing forensic science One of the key challenges for forensic science is to avoid being side-tracked by one of the louder narratives in the media that the big problem forensic science faces is ‘junk science’ and ‘rogue scientists’. These are clearly important i
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The selection of mutations in vivo with antivirals
2021-12-18
The selection of mutations in vivo with antivirals is a complex process involving, among other things, the frequency of a given mutation prior to treatment, the effect of that mutation on viral protein function, and the interplay of a given mutation pattern with host immune mechanisms. Investigation
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In summary we have designed and optimized a new
2021-12-18
In summary, we have designed and optimized a new series of 1,4-dioxycyclohexane GPR119 agonists. SAR studies led to the discovery of the preferred molecule that has potent and efficacious GPR119 activity across species. This lead compound exhibited an excellent ADME and safety profile, and demonstr
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Results indicated that superfusion of orexin alone glutamate
2021-12-18
Results indicated that superfusion of orexin alone, glutamate alone or orexin-glutamate co-administration significantly increases the spontaneous discharge rate of LC neurons in both morphine dependent and non-dependent rats (Fig. 2, Fig. 3). However, co-application of orexin and glutamate resulted
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Cy5.5 maleimide (non-sulfonated) In this study we present th
2021-12-18
In this study, we present the synthesis and structure–activity studies of a structurally distinct series possessing high potency and selectivity in HEK cell lines together with a potentially promising overall biopharmacological profile. Focusing on creating sufficient structural dissimilarity with g
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Moreover the ubiquitous expression of the OTR and GHSR
2021-12-18
Moreover, the ubiquitous mechlorethamine mg of the OTR and GHSR was also observed in hippocampal and hypothalamic primary culture, indicating that this expression pattern is likely due to basal activity of these receptors. GPCR trafficking under control conditions has been linked to biased signalli
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Some but not all GSIs inhibit signal
2021-12-17
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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We have isolated various bioactive peptides acting by
2021-12-17
We have isolated various bioactive ipa chemical acting by binding to the receptors of endogenous bioactive peptides such as opioid, bradykinin, neurotensin, and complements C3a and C5a etc. [24]. Rubimetide is the first example of an agonist peptide of the FPR2 of exogenous origin. Anxiolytic-like
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Receptor activator of NF B ligand RANKL
2021-12-17
Receptor activator of NF-κB ligand (RANKL) and macrophage colony-stimulating factor (M-CSF) stimulate the generation of osteoclast cyproheptadine hcl australia [10], [11], [12], [13]. In response to sphingosine 1-phosphate (S1P) signaling, osteoclasts then attach to regions of bone undergoing resor
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The Ala to Leu substitution would reduce the
2021-12-17
The Ala116 to Leu110 substitution would reduce the size of the active-site cavity disfavoring the production of longer allylic compounds as a result of steric hindrance, according to the observations of Poulter and co-workers [29], [30]. However, this explanation appears to be unlikely since several
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