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In anticipation of an approach based on modification
2019-09-25

In anticipation of an approach based on modification of the cyclohexylacetic Benzoylhypaconitine subunit of 1 as a means of improving permeability, a set of analogs were prepared to map out the optimum display of the acidic functionality. Homologated acids 25 and 26 were found to be equipotent to 1
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br Experimental methods br Results and
2019-09-25

Experimental methods Results and discussion Conclusions Here we describe the first reported method for high-yield Exendin-4 of active and soluble mature CPG2 (in the absence of the leader peptide) and its individual catalytic and dimerization domains in E. coli. Such a method is of key imp
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Stable carbon and nitrogen isotope ratios in bone collagen a
2019-09-25

Stable carbon and nitrogen isotope ratios in bone collagen and carbon isotope ratios in bone apatite data were obtained by the means of the techniques described in supplementary data (SD1). For collagen, standard indicators have been used to assess its preservation, such as collagen yield, carbon an
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The UI compo http www
2019-09-25

The UI components used in our proposal are called COTSgets, from COTS (Commercial Off-The-Shelf) [28] and gadgets (understood as any software that can work alone or as a piece of the architecture). A COTS component is any coarse-grained component developed by third parties available for building mor
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The crystal structure of full length CHK is still unsolved
2019-09-25

The crystal structure of full-length CHK is still unsolved. However, the close homology between CHK and Csk suggests that these kinases share a similar structure. Therefore, the engagement of the CHK SH2–kinase linker with the αC-helix could control the activity of the CHK kinase domain. Sequence al
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In summary A is a potent orally available
2019-09-25

In summary, A-216546 is a potent, orally available endothelin receptor antagonist with a high selectivity for the endothelin ETA receptor. The potency and bioavailability of A-216546 suggest that it will have important utility for preclinical evaluation of the pathophysiology of the endothelin syste
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Together the data suggests that more
2019-09-25

Together, the data suggests that more work needs to be done to establish the role of PARP inhibitors in Ewing sarcoma. As a single agent, there is some activity in Ewing sarcoma cell lines and a highly statistically significant relationship between olaparib sensitivity and EWS–FLI1 expression. Howev
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ERR is present early in the developing
2019-09-25

ERRβ is present early in the developing placenta in a subset of 795 in extra-embryonic ectoderm destined to make up the chorion.19, 20 ERRβ is likely essential for reproduction. ERRβ expression is essential for the maintenance of pluripotency and self-renewal potential in mouse embryonic stem cells
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Dp44mT br Materials and methods br Results br Discussion Inf
2019-09-25

Materials and methods Results Discussion Inflammatory signalling and in particular the arachidonic Dp44mT cascade have been suggested as targets for disease modification, optimization of the therapeutic response, and even restoration of pharmacosensitivity (Potschka, 2010). Recently, we dem
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Lavallee et al reported that PREG could be
2019-09-25

Lavallee et al. [30] reported that PREG could be esterified by lecithin:cholesterol acyltransferase (LCAT). LCAT uses cholesterol and phosphatidyl choline present in the newly formed high-density lipoprotein (HDL) as substrates and convert them into cholesteryl esters and lysophosphatidyl choline. T
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We should also note that although AOAA is
2019-09-25

We should also note that, although AOAA is not a specific H2S inhibitor, its inhibitory effect on l-cysteine-induced relaxations are related to H2S since addition of AOAA to another H2S inhibitor PAG did not provide a further inhibition of these relaxations in penile tissue [37]. In our study, the c
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Dual inhibition of ACE and NEP
2019-09-25

Dual inhibition of ACE and NEP as a strategy for treating hypertension has been extensively investigated, including contributions from these laboratories through the discovery of Sampatrilat . Given that both targets are related zinc metalloproteinases, dual enzyme inhibition can be achieved within
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br A brief history of
2019-09-25

A brief history of RBR E3s RBR E3s were originally defined based on sequence alignments that predicted a tripartite motif of three zinc (Zn)-binding domains: two RING domains (RING1 and RING2) connected via an in-between-RING (IBR) domain [28], [29]. The prediction together with initial observati
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In humans several different small ubiquitin related modifier
2019-09-25

In humans, several different small ubiquitin-related modifier (SUMO) paralogs can be conjugated to cellular proteins. The human genome codes for five SUMO paralogs (SUMO1–5); of these, SUMO1 and the almost identical SUMO2 and SUMO3 are ubiquitously expressed. Sumoylation is executed by an enzymatic
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br Introduction br Structure of the Ku
2019-09-25

Introduction Structure of the Ku heterodimer associated to DNA The atomic structure of the Ku heterodimer, alone and bound to a small DNA fragment, was recently determined (Walker et al., 2001) and has significantly improved our understanding of DNA recognition by DNA-PK holoenzyme (Fig. 3). B
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