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Because of the important role of the
2020-12-28
Because of the important role of the DDB1-CUL4B interaction for CUL4B-based E3 ligases, disruption of the DDB1-CUL4B interaction could be an effective approach to treat cancer. Therefore, we developed an in vitro HTS assay based on yeast cell growth inhibition to identify compounds that could disrup
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Structure similarity searches were conducted using the stand
2020-12-28
Structure similarity searches were conducted using the standalone version of the DALI program with the query structures scanned against a local current version of the PDB that has all chains as separate entries (Holm and Sander, 1995). The structural hits for each query were collected, even if the D
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A structural explanation for how RBR RING
2020-12-28
A structural explanation for how RBR RING1s handle their bound E2~Ubs differently from canonical RINGs has not been readily apparent. Only a few residue positions are strongly conserved in RING and RING1 domains, most of which are zinc-coordinating Cys and histidine residues. A key position in canon
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The roles of ginsenoside in
2020-12-28
The roles of ginsenoside in E1 and 26S proteasome inhibition are shown in Table 2. The nitro substitute on the furan ring may be important for PYR-41 inhibition of the E1 enzyme (Yang et al., 2007). The macrocycle core and aliphatic tail of Largazole are responsible for inhibiting E1 activity (Unger
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br Roles of TLS polymerases outside DNA damage tolerance br
2020-12-28
Roles of TLS polymerases outside DNA damage tolerance Preparing the ground for more DNA damage: adaptive responses through gene induction Conclusions and perspectives Although known for many decades, the relevance of TLS in genome stability is normally considered secondary to mechanisms tha
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br Conflict of Interest br Acknowledgements Marques F was su
2020-12-28
Conflict of Interest Acknowledgements Marques F. was supported by the Foundation for Science and Technology (FCT), Portugal, Grant UMINHO/BI/35/2012. This work was supported by FCT by the Project PTDC/AGR-AAM/70418/2006. Introduction β-methylamino-l-alanine (BMAA) exposure has long been as
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The first transcription factor TF known to interact
2020-12-28
The first transcription factor (TF) known to interact with one of the cis-acting GAREs is GAMYB protein, the expression of which is induced by GA in the aleurone AKT inhibitor VIII australia of barley (HvGAMYB) (Gubler and Jacobsen, 1992). GAMYB is an important regulator of endosperm functions duri
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eg5 Similar to Bdnf acute administration of
2020-12-28
Similar to Bdnf4, acute administration of RG108 did not alter gene expression of Gria1 and Hdac2, despite their relevance for the task. Gria1 belongs to the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic eg5 receptor (AMPAR) family that is known to be crucial for LTP and the strengthening of synap
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bupropion hydrochloride br Discussion This study characteriz
2020-12-28
Discussion This study characterized longitudinal changes of cholinesterase and PON1 enzyme activities in greenhouse workers over two periods of a crop season with different levels of pesticide exposure. Although study participants were not exposed to OP insecticides, because they worked under in
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As for the molecular mechanism Ferguson BD
2020-12-28
As for the molecular mechanism, Ferguson BD suggested that EphB4/EphrinB2 stimulation induced topoisomerase I activity in small cell lung cancer cell lines. Treatment of Caspase Inhibitor Set I synthesis with EphrinB2/Fc induced topoisomerase activity as assessed by DNA relaxation in cells with hig
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It is well established that a number of
2020-12-26
It is well established that a number of intracellular signaling pathways mediate sensitization of sensory neurons (Gold and Gebhart, 2010, Richardson and Vasko, 2002). This redundancy could be advantageous since it provides diversity in initiating and maintaining hypersensitivity in response to inju
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The compounds listed in Table Table Table Table Table
2020-12-26
The compounds listed in Table 1, Table 2, Table 3, Table 4, Table 5 were biologically evaluated for their inhibition of the specific binding of a radiolabeled ligand [3H]PGE2 to membrane fractions prepared from cells stably expressing each mouse prostanoid receptor. The EP1 antagonist activity of th
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br Assessing DUB activity The Ub field has
2020-12-25
Assessing DUB activity The Ub field has benefited greatly from the past efforts of biochemists and chemical biologists who have reconstituted Ub signals in vitro and generated tools for capturing or measuring DUB activities, many of which can be readily produced or are commercially available (Ekk
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The synthesis of compounds a and b are
2020-12-25
The synthesis of compounds 7a and 7b are outlined in Scheme 2. Compound 5 was obtained by di-tert-butyl pyrocarbonate protection of Paxilline receptor 4a. Then, compounds 6a and 6b were obtained by amination of the fluoride with a morpholino and dimethylamine, respectively. Target compounds 7a and
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corticotropin releasing factor Like compound substitution on
2020-12-25
Like compound substitution on compound () contains amino and carboxamide groups attached to adjacent ring positions. These groups have similar interactions as compound with the protein backbone and Glu114. The triazole core is coordinated with Lys291. The triazole ring core π-stacks with Tyr226. The
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