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Molecular modelling studies were performed
2020-08-08
Molecular modelling studies were performed on the hDHFR inhibitors identified (1, 11, 13, 14, 16, 25 and 32) to explore the structural basis of the interaction between the mentioned compounds and the human enzyme. The docking studies were performed using the X-ray crystallographic structure of the h
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LPS is the major toxic component of
2020-08-08
LPS is the major toxic component of the outer membrane of gram-negative bacteria and high dose of LPS challenge in animal can induce a rapid systemic inflammatory response which resembles septic shock in clinical [15]. We demonstrated that administration of KPT330 significantly attenuated lung injur
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Hinokitiol possesses potent anti tumor effects
2020-08-08
Hinokitiol possesses potent anti-tumor effects by inducing cell apoptosis (Seo et al., 2017). Our present study also demonstrated that hinokitiol induced apoptosis effects (Fig. 1A, D) possibly through suppression of survivin expression in melanoma B16-F10 Immunology Compound Library (Fig. 2). Incr
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The structure of the HOIP RBR LDD module bound
2020-08-08
The structure of the HOIP RBR–LDD module bound to UbcH5~Ub reveals insights into an activated HOIP component [47]. Contacts between the E2~Ub and the non-cognate RBR module in the crystal suggest how a structure in which the active sites of the E2 and the E3 are in close proximity might look. In thi
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MK-8745 We did not performed MD simulations of the GAPDH int
2020-08-07
We did not performed MD simulations of the GAPDH interaction with α-synuclein modified by glyceraldehyde-3-phosphate since the products are unclear [38], and phosphate group might split off because of lability of the connection bond. Carboxymethyl lysine was chosen since it is considered to be the m
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br Experimental Procedures br Author Contributions br Acknow
2020-08-06
Experimental Procedures Author Contributions Acknowledgments A.M. is supported by NCI R01 104348 and is also supported by the Burroughs Wellcome Foundation and Chemotherapy Foundation. A.H. and D.G.G. are supported by NIH grants R01AI080850 and R21AI101704. This research was initially suppo
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Several antimalarial drugs in clinical studies target
2020-08-06
Several antimalarial drugs in clinical studies target pyrimidine nucleotide biosynthesis , because parasites rely on fast and large replication of DNA to infect during liver and blood stages. Dihydroorotate dehydrogenase (DHODH) catalyzes the oxidation of -dihydroorotate (L-DHO) to -orotate in the
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br A link between lipoprotein modification and
2020-08-06
A link between lipoprotein modification and inflammatory response A unique finding related to the HNE-induced COX-2 gene Acetazolamide sale is that the modified LDLs might be involved in the COX-2 induction. Kanayama et al. [18] found that HNE could induce COX-2 only in the presence of serum. Th
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Recent pharmacological and clinical studies suggested that
2020-08-06
Recent pharmacological and clinical studies suggested that estetrol (E4) should also be considered as an interesting candidate for MHT (Abot et al., 2014; Mawet et al., 2015). E4 is naturally produced from E2 and estriol (E3) via 15α- and 16α-hydroxylase by the human fetal liver during pregnancy and
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The process of ubiquitination is a
2020-08-05
The process of ubiquitination is a multi-step process ultimately leading to the covalent modification of a protein substrate with small molecule ubiquitin. There are three types of ubiquitination: 1) mono-ubiquitination in which single ubiquitin is attached to target 2) multi ubiquitination or poly-
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We used the conditions for covalent
2020-08-05
We used the conditions for covalent linkage of photoreactive THPs that were previously optimised for the integrin-binding THP, GFOGER [15], where, after 5 min of UV treatment and at a THP concentration of 5 μg/ml, maximal and specific covalent linkage of the photoreactive THP was observed. We antici
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BLAST analysis of BTA genes from C reinhardtii and K
2020-08-05
BLAST analysis of BTA1 genes from C. reinhardtii and K. lactis show that databases contain sequences of BTA1 orthologs from more than 30 species of basidiomycetes, all from fungal whole-genome projects. None of them has been functionally characterized. We demonstrated that BTA1 gene of basidiomycete
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Due to their ability to hydrolyze rhamnose from
2020-08-05
Due to their ability to hydrolyze rhamnose from natural flavonoids, α-RHAs are used in several biotechnological applications. Some examples include the hydrolysis of naringin to improve beverage quality by debittering grapefruit and citrus juices [12,13], and the removal of hesperidin crystals from
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Initial steps toward diubiquitin probes were published by
2020-08-04
Initial steps toward diubiquitin probes were published by Iphöfer et al. [49]. They developed the first chain-specific ubiquitin isopeptide probes in which HA-tagged ubiquitin is linked through its C-terminus to a lysine sidechain in a 13-amino casin peptide derived from ubiquitin. The C-terminal g
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Although the overall profile of was
2020-08-04
Although the overall profile of was encouraging, we pursued its optimization based on SAR studies imported from a novel class of compounds in which the sulfonamide moiety of MK-7246 was replaced by an amide group. Potential liabilities related to the presence of a sulfonamides group (i.e., allergic
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