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Much is known about FPPS
2021-11-25
Much is known about FPPS structure and function, with over 120 FPPS crystal structures being currently available. This wealth of information is largely the consequence of human FPPS serving as a drug target for the treatment and/or prevention of pathologies such as osteoporosis, hypercalcemia and Pa
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The progression of HIV varies from patient to patient
2021-11-25
The progression of HIV varies from patient to patient, with some who progress slowly and others who progress much faster. However, CD4+ and CD8+ cell counts are intimately linked in those that are able to suppress the HIV infection (Walker et al., 1986; Saez-Aninon et al., 2007). Depletion of these
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In this paper we demonstrate a diatomaceous earth based
2021-11-25
In this paper, we demonstrate a GSK 4716 based TLC-SERS sensing technique combined with machine learning analysis to quantitatively detect seafood allergen in real spoiled tuna samples. We fabricate a diatomaceous earth TLC plate as a separable SERS-active substrate to detect histamine in artificia
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br HER proto oncogene The erbB gene located on
2021-11-25
HER2 proto-oncogene The erbB2 gene, located on the short arm of chromosome 17, was discovered and cloned in 1983 (Fig. 1) (Sato et al., 1983). The product of this gene, HER2, is a transmembrane glycoprotein of 185 KDa that consists of three main domains: an extracellular, a transmembrane and an i
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HDAC enzymes oppose the effects of HATs by reversing
2021-11-25
HDAC enzymes oppose the effects of HATs by reversing lysine acetylation, an action that restores the positive charge of the lysine thus stabilizing the local chromatin structure. By removing acetyl groups from ε-amino lysines of proteins, HDACs not only alter transcription, but also promote either t
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A repertoire of cytotoxic payloads is increasing
2021-11-25
A repertoire of cytotoxic payloads is increasing; among those, MMAE has been utilized for the highly effective ADC brentuximab vedotin. However, the ADCs which utilized MMAE to target GCC in solid tumors have shown a poor efficacy suggesting that various tumor types respond differently to a given to
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Our observations with RBC in human
2021-11-25
Our observations with RBC8 in human platelets suggested a more wide-ranging role for Rals in platelet function compared to our observations in Ral deficient mouse platelets. Using lumi-aggregometry, 10 μM RBC8 significantly reduced platelet aggregation and ATP secretion responses in both WT and DKO
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GPR GPR GPR GPR and GPR all shared identities to
2021-11-24
GPR80, GPR81, GPR82, GPR93 and ψGPR79 all shared identities to P2Y GPCRs or P2Y-like oGPCRs. Previously, at least three different nucleotide receptor phenotypes have been observed in mammalian tissue, including GPCRs activated by Maprotiline HCl nucleotides (e.g. P2Y1 and P2Y11), uridine nucleotide
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br Acknowledgements This work was supported by
2021-11-24
Acknowledgements This work was supported by the National Key Research and Development Program of China [2017YFD0400106]; Innovation of modern Project[F18R02-03]. Introduction The Vesiculovirus genus is one of the six genera of the rhabdovirus family. The prototype vesiculovirus is vesicular s
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Hepatic drug metabolizing enzymes and transporters
2021-11-24
Hepatic drug-metabolizing Cefpodoxime Proxetil synthesis and transporters expression were regulated by nuclear receptors [19], [20], [21]. The effects of HFD-induced fatty liver on drug metabolizing enzymes in mice were recently studied, and the results provided a systematic evaluation of the chang
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The MeO CFO phen yl group
2021-11-24
The 1-MeO-4-CFO-phen-2-yl group was then selected for the C-3 position when we investigated the aryl substituents at the C-6 position of indazole. As shown in , C-6 position seems to be more tolerant than the C-3 position, as all the aryl groups examined exhibited potent hGCGR activity. Interestingl
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The patterns of Fig Fig emerge at
2021-11-24
The patterns of Fig. 1, Fig. 2 emerge at the multicellular level; their dynamics can only be understood by integrating different magnitudes and feedback loops in networks incorporating the coupling between biochemical and bioelectrical signals (see Fig. 6, Fig. 8). Interestingly, this might also be
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Formyl peptide receptors FPRs are a family
2021-11-24
Formyl peptide receptors (FPRs) are a family of surface-expressed, G protein-coupled receptors [7]. The three members, FPR1, FPR2 and FPR3, share significant sequence homology, but have different functional properties [7]. While FPRs are mainly expressed by innate leukocytes, they are also found on
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Considering the conformational preferences of the SRSRY
2021-11-24
Considering the conformational preferences of the SRSRY sequence in the x-ray structures of soluble uPAR (SuPAR) [18], [19], [20], [50], [51], it is included in a quite flexible linker delimited by Cys76 and Cys95 residues. The SRSRY sequence adopts either α-turned or β-extended conformation. In any
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The objective of this study
2021-11-24
The objective of this study is to design and synthesize drug-like molecules with agonistic activity on both receptors; PPARγ and FFAR1. These agents would act as insulin sensitizers and insulin secretagogues through their action on PPARγ and FFAR1, respectively. The design of drugs with dual mode of
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