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This review focuses on the atomic basis of CRM
2021-02-03
This review focuses on the atomic basis of CRM1-mediated nuclear export. There are now 27 crystal structures of CRM1 in the Protein Data Bank (PDB) (www.rcsb.org) [64]. Collectively, this large body of work explains various aspects of CRM1 function. Here we summarize the structure–function studies t
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The synthesis of tricyclic analogs is described
2021-02-03
The synthesis of tricyclic analogs 28–33 is described in Scheme 3. Oxidative C–C bond cleavage of the terminal olefin of 39i afforded a tricyclic product 52 without isolation of an aldehyde expected as an intermediate. Aminolysis of the chloride 52 with optionally substituted anilines afforded 28–30
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br Materials and methods br
2021-02-03
Materials and methods Results Discussion Consistent with previous reports (Barr et al., 2010, Vuong et al., 2010), the current study demonstrates that rats treated with amphetamine exhibit heightened anxiety states during withdrawal. Furthermore, icv. infusion of a CRF2 receptor antagonist
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Based on the finding described above the present study was
2021-02-03
Based on the finding described above, the present study was designed to investigate the effects of specific CRF receptors, CRF1 and CRF2, in the BLA and CeA on the duration of TI in guinea pigs (Cavia porcellus). To this end, we evaluated whether administration of the CRF1 8-CPT-2Me-cAMP, sodium sal
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It should be noted that the
2021-02-03
It should be noted that the long-lifetime binding-responsive luminescence of ARC-1528 and ARC-1530 becomes evident only upon illumination with radiation at near-UV range where the excitation of ATB or ASB moiety is possible. At higher wavelength range (visible light), the fluorophore (5-TAMRA) can b
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Another important consideration with respect to drug conditi
2021-02-03
Another important consideration with respect to drug conditioning suggested by the present findings is the observation of an attenuated (R)-(+)-Etomoxir sodium salt receptor on the second extinction trial. Seemingly, if ERK measurements were made following a partial reduction in the conditioned res
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To develop antagonists selective for the mouse EP receptor
2021-02-03
To develop antagonists selective for the mouse EP1 receptor, we started with compound (), synthesized as previously described (). Diethyl dipicolinic ponceau stain mg () was reduced with NaBH to . Parikh–Doering oxidation of with sulfur trioxide–pyridine complex and DMSO produced the unstable aldehy
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ELUXA HM EMSI is an ongoing
2021-02-03
ELUXA 1 (HM-EMSI-202) is an ongoing pivotal Phase II global clinical trial, designed to further investigate the efficacy and safety of Olmutinib in patients T790M-positive NSCLC with acquired resistance after first-line EGFR TKIs. Primary endpoint is ORR according to RECIST 1.1, while secondary endp
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Mulan is one of three E ubiquitin ligases that
2021-02-02
Mulan is one of three E3 ubiquitin ligases that are present in the mitochondria along with MARCH5/MITOL (membrane associated RING-CH5) and RNF185 [14], [15], [16], [17]. Mulan is a 352-residue polypeptide that crosses the mitochondrial outer membrane (OMM) twice, its amino-terminus, which includes t
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br Introduction In most of
2021-02-02
Introduction In most of the angiosperms, sexual reproduction requires a process called double fertilization where the specialized cell division called meiosis produces haploid gametes combine to form diploid (2n) embryo. In phospholipase a2 inhibitor to this, apomixis, naturally occurs in at leas
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br Conclusion br Acknowledgements This work is supported by
2021-02-02
Conclusion Acknowledgements This work is supported by the National Natural Science Foundation of China (41806151, 41706144), the National Natural Science Foundation of China (31330082). We would like to thanks the support of young science and technology talents training fund of South China Agr
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Our structures also provide new insights into
2021-02-02
Our structures also provide new insights into CRTH2 drug development. The ligand binding pocket revealed by our structures comprises many aromatic residues and a few polar residues at the distal end. Correspondingly, most CRTH2 antagonists share a similar structural feature characterized by an aceta
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Recent studies have shown that the extracellular regulated
2021-02-02
Recent studies have shown that the extracellular regulated protein kinase 1 and 2 (ERK1 and ERK2), commonly referred to collectively as ERK 1/2, are members of the mitogen-activated protein kinase (MAPK) family. This family of kinases transport signals from the surface of the cell to the nucleus, th
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Although MMP might be a
2021-02-02
Although MMP-9 might be a downstream target of Src kinase signaling (Liu and Sharp, 2011), a direct connection has not been established. We showed for the first time that, in the collagenase-induced ICH model, Src kinase signaling regulates MMP-9 activity and mediates EP1R toxicity. Consistent with
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As a support chitosan presents interesting
2021-02-02
As a support, chitosan presents interesting characteristics that reinforce its great potential for enzyme immobilization [18,19]. Firstly, it is produced from renewable natural sources in addition to being biodegradable and water insoluble [20,21]. Also, the main peculiarity in the chitosan structur
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