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The interferences between thapsigargin and forskolin
2021-07-13
The interferences between thapsigargin- and forskolin-induced Ca release indicate that these drugs deplete the same intracellular stores in RASMC. In fact, after partial depletion of thapsigargin-sensitive stores, the forskolin-induced increases in [Ca]c were significantly reduced. Similarly, a prev
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An Emerging Role for the EphrinB EphB
2021-07-13
An Emerging Role for the EphrinB2-EphB4-RASA1 Signaling Axis in Human Congenital Cerebrovascular Disorders Normal vascular development includes de novo blood vessel formation from endothelial cells (ECs) (vasculogenesis) 1, 2, expansion of the network through vessel sprouting, splitting, and remode
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Historically covalent drugs have had great
2021-07-12
Historically, covalent drugs have had great success (e.g., aspirin and penicillin), and covalent drugs have become a focus in anticancer and antiviral drug discovery (Kalgutkar and Dalvie, 2012, Singh et al., 2011). These compounds contain low reactivity warheads that allow covalent adducts to form
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The biological significance of DNA ligases is attributed to
2021-07-12
The biological significance of DNA ligases is attributed to their function in DNA replication, recombination and/or DNA repair [1], [2]. In vertebrates, three different DNA ligases I, III and IV are recognized. DNA ligase I is essential for the Okazaki fragments’ ligation during lagging-strand DNA s
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br Fragment based drug discovery FBDD is a powerful
2021-07-12
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 atm inhibitor space with libraries which are smaller in size, producing drug leads with high ligand-binding efficiency.
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The synthetic route of R changed
2021-07-12
The synthetic route of R-changed derivatives is shown in . Compounds – were prepared from commercially available 4-nitro-1-indazole (). After same two steps with , the N-substituted indazole of was produced using the Suzuki reaction in a good yield (85%). Reduction of was performed using Pd/C, and
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br Experimental section br Results br Discussion In our prev
2021-07-12
Experimental section Results Discussion In our previous work (Rashidi et al., 2018) we isolated a novel glucarpidase whose raised WEHI-539 hydrochloride did not cross-react with the one in clinical use. In principle, therefore, it would be possible to delay the production of antibodies in a
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br The LSCP model and
2021-07-12
The LSCP model and its properties In this section, we first introduce the LSCP model in Section 2.1. Some examples of the model are presented in Section 2.2 and basic properties of the model are presented in Section 2.3. Finally, Section 2.4 introduces finite dimensional approximations necessary
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The present study sought to determine if chlorodifluoroaceto
2021-07-12
The present study sought to determine if chlorodifluoroacetophenones, such as 3 and 4, were amenable to a radiolabelling methodology to generate potential 18F imaging agents with high cholinesterase affinity. A number of procedures have been reported for the synthesis of trifluoromethyl ketones, inc
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br Introduction The cervix is a poorly studied
2021-07-12
Introduction The hyPerFUsion™ high-fidelity DNA polymerase mg is a poorly studied component of the mare’s reproductive tract. It has anatomical and biological defense mechanisms involved in the delicate balance between immunological tolerance, sperm transport and biological defense. Anatomically
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The ESC update emphasizes the need for implementing
2021-07-12
The 2017 ESC update emphasizes the need for implementing strategies to minimize PCI-related complications, including risk stratification for ischemia and bleeding, keeping triple antithrombotic therapy to the shortest possible duration with dual antithrombotic therapy as an alternative, using non–vi
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stavudine receptor Additionally both in vitro and in vivo st
2021-07-12
Additionally, both in vitro and in vivo studies showed that a Ca2+ influx is closely related to apoptosis (Rizzuto et al., 2003). Calmodulin (CaM) is a multifunctional intermediate calcium-binding messenger protein expressed in all eukaryotic cells, which senses intracellular calcium levels by bindi
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For the current studies we used the
2021-07-12
For the current studies, we used the selective Epac agonist 8CPT-AM to directly activate the proteins. We chose this pharmacological approach since it allows a direct activation of Epacs rather than using receptor agonists such as PGE2 which could introduce confounding variables. One potential conce
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br Methods Ventricular cardiomyocytes from adult
2021-07-12
Methods Ventricular cardiomyocytes from adult male Wistar rats were isolated using a standard enzymatic digestion [11]. Cells were incubated at 37°C for 4 to 6h with Tyrode solution (in mM: 140 NaCl, 4 KCl, 1.1 MgCl2, 10 HEPES, 10 glucose, 1.8 CaCl2; pH7.4, with NaOH) supplemented or not with 10μ
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br Chemistry The test compounds listed in
2021-07-12
Chemistry The test compounds listed in Table 1, Table 2, Table 3, Table 4, Table 5, were synthesized as outlined in Scheme 1, Scheme 2, Scheme 3, Scheme 4, Scheme 5. Synthesis of 2–5 is described in Scheme 1. N-Sulfonylation of the aniline 26 with benzenesulfonyl chloride afforded the sulfonamide
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