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Cell swelling stimulates the release of
2019-10-11
Cell swelling stimulates the release of certain amino acids, in particular the non-protein amino alpha-Endorphin taurine, via a pathway which has the characteristics of a channel rather than a carrier [54], [69]. Indeed, on the basis of pharmacological inhibition, it was suggested that volume-activa
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br Experimental methods br Results and discussion br Conclus
2019-10-10
Experimental methods Results and discussion Conclusion Rational design of highly selective fluorescent probes to detect G-quadruplexes is of profound importance for basic research. On this basis, we designed and synthesized a series of N-alkylated styrylquinolinium dyes Ls-1, Ls-2 and Ls-3.
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br Fragment based drug discovery FBDD is a powerful
2019-10-10
Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical nitric oxide synthase inhibitor space with libraries which are smaller in size, producing drug leads with high ligand-bi
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CYP A is involved in the metabolism
2019-10-10
CYP3A is involved in the metabolism of approximately 50% of all drugs that are currently prescribed to patients [1], [15], [16]. Marked interindividual variabilitity of the catalytic function for metabolizing CYP3A substrates has been demonstrated with variability exceeding 20-fold [1]. Levonorgestr
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To assess which export pathway is used by the
2019-10-10
To assess which export pathway is used by the iNOS mRNA, we inhibited CRM1 activity by incubation of DLD-1 dna stain with LMB. Since LMB covalently and exclusively binds to CRM1, it represents a potent and specific inhibitor of the CRM1 transport activity [38]. Inhibition of CRM1 activity as well a
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Although the phase I clinical trial of LMB was unsuccessful
2019-10-10
Although the phase I clinical trial of LMB was unsuccessful, the detailed review of this trial only mentions some malaise and anorexia as side effects, which are common for most effective chemotherapeutic drugs. These side effects may diminish if lower doses are administered. In view of the novel C
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Nicotine is the main psychoactive component of tobacco that
2019-10-10
Nicotine is the main psychoactive component of tobacco that causes addiction. Besides the regulation of the stress responses, CRF has been implicated in nicotine addiction based on several lines of evidence (Bruijnzeel and Gold, 2005, Sarnyai et al., 2001). First, acute administration of nicotine, l
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Kim et al reported for
2019-10-10
Kim et al. reported for bioactive compounds originating from the endemic species in Korea, the hexane and EtOAc fractions of the MeOH extracts from the roots of Dystaenia takeshimana (Nakai) Kitagawa (Umbelliferae) showed cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) dual inhibitory activity b
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br Acknowledgements This work was
2019-10-10
Acknowledgements This work was supported by the European Committee Fifth Framework Project QLK5-1999-01360. We are grateful to Dr. T.T. Hoang for the provision of plasmids pEX18Tc, pPS858 and pFLP2, Prof. B.L. Wanner for providing us with the plasmid pKD4 and related strains, and Prof. P. Soucail
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br Conclusion br Conflicts of interest br Acknowledgements
2019-10-10
Conclusion Conflicts of interest Acknowledgements This study was financially supported by The Science and Engineering Research Board (SERB), Department of Science & Technology (DST), Government of India under the Fast Track Scheme for Young Scientist to Dr. V. Dhananjayan (No: SB/FT/LS-140/
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Otherwise ES cells express high level of
2019-10-10
Otherwise, ES orbifloxacin express high level of histone lysine specific demethylase 1 (LSD1) expression. In this context, it is proposed that LSD1 inhibition may block the function of EWS-ETS proteins [70]. Furthermore, checkpoint kinase 1 (CHK1), a modulator of cell survival under the condition o
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After activation AKT phosphorylates target proteins involved
2019-10-10
After activation, AKT phosphorylates target proteins involved in cell growth, metabolism and survival (Manning and Cantley, 2007). For example, AKT phosphorylates the pro-apoptotic protein BAD, preventing it from binding to and inactivating Bcl-xL in mitochondria (Datta et al., 1997). In turn, Bcl-x
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In sum although it is reasonable
2019-10-10
In sum, although it is reasonable to assume that the activities of an enzyme on alternative (metabolically available) substrates may often depend on neutral drift, the point is difficult to prove because various types of selective pressures can be at play, and these will be different in different or
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br RING type E s and
2019-10-09
RING-type E3s and their substrates There is enormous diversity in substrate ubiquitination and its regulation, as the targets of RING-type E3s are incredibly varied. RING-type E3s are implicated as tumor suppressors, oncogenes, and mediators of endocytosis, and play critical roles in complex mult
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Interestingly Carver Johnson and Kim investigated a polymorp
2019-10-09
Interestingly, Carver, Johnson, and Kim (2016) investigated a polymorphism in the OPRM1 μ-opioid receptor gene for its role in sensitivity to social contexts. The G allele of this polymorphism was associated with higher levels of sensitivity. The authors found significant interactions, e.g. the nega
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