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We next examined the effects of substituents around
2021-02-01

We next examined the effects of substituents around the carboxylic 6206 moiety on CRTH2 binding (Table 4). The carboxylic acid moiety shared by the representative CRTH2 antagonists and is essential for the CRTH2 activity. Germinal dimethylation of the methylene moiety next to the carboxylic acid re
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Under conditions of energy scarcity or nutritional restricti
2021-02-01

Under conditions of energy scarcity or nutritional restriction, AMPK, a critical energy sensor, is activated in response to the increased ratio of AMP to ATP. Various kinases may phosphorylate AMPK, leading to its activation. For example, AMPK phosphorylation by liver kinase B 1 (LKB1) at Thr172 res
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DASA-58 Natural progestogens play an important
2021-01-30

Natural progestogens play an important role in the stimulation of oocyte growth and maturation as well as in spermatogenesis and sperm maturation, and they act as sex pheromones in teleost fish (Kime, 1990, Kobayashi et al., 2002, Nagahama and Yamashita, 2008, Scott et al., 2010). A complex series o
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First of all two assumptions just as in
2021-01-30

First of all, two assumptions just as in Ref. [30] are need to simplify the penetration process: (1) The crater phases is short and the Amiloride HCl dihydrate of EFP is consumed little; thus, the influence of crater on penetration can be ignored; (2) the initial stagnation radial pressure is equal
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Walrycin B In terms of its protease activity
2021-01-30

In terms of its protease activity, MME has a broad range of substrates being able to target glucagon, bradykinin, GLP1, and several other Walrycin B of circulating small molecules [25]. MME has been shown to target free insulin B-chain [32], although whether MME could target and degrade the insulin
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Imatinib STI is a first line tyrosine kinase
2021-01-30

Imatinib (STI-571) is a first-line tyrosine kinase inhibitor (TKI) targeted at breakpoint cluster region-Abelson kinase (ABL) for the treatment of chronic myeloid leukemia (CML) [26]. As a type II inhibitor, imatinib achieves significant selectivity by binding to an inactive DFG-out conformation (DF
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br Experimental Procedures br Acknowledgments br Introductio
2021-01-30

Experimental Procedures Acknowledgments Introduction The ability of the affiliative and nurture hormone oxytocin (OT) to attenuate stress has been observed across psychological, neurological, and physiological levels [1], [2]. We and others have demonstrated that, in the gut, OT can lessen
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Here we report that ILC s
2021-01-30

Here, we report that ILC3s sensed oxysterols through GPR183, which was highly expressed by LTi-like ILC3s. 7α,25-OHC-synthesizing enzymes were produced by fibroblastic stromal Nemadectin found in intestinal lymphoid structures, and the GPR183 ligand 7α,25-OHC acted as a chemoattractant for ILC3s. GP
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Another important issue in biosensors is to design a
2021-01-30

Another important issue in biosensors is to design a simple and potable detection strategy to meet the requirement of the point-of-care (POC) test applications. According to the recent research, by using invertase Defactinib for hydrolyzing sucrose into glucose, the range of personal glucometer has
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br Conclusions In conclusion we identified and overexpressed
2021-01-29

Conclusions In conclusion, we identified and overexpressed DGAT2 in fast growing, oleaginous N. oceanica for the first time. The engineered N. oceanica overexpressing DGAT2 resulted in enhanced neutral lipid accumulation and altered fatty gaba agonist composition. Altogether, our findings demons
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In vitro work by us
2021-01-29

In vitro work by us and others revealed that high affinity interaction with collagen requires dimerization and/or pre-oligomerization of DDR1 (Agarwal et al., 2007, Abdulhussein et al., 2008, Leitinger, 2003). It has also been reported that a significant percentage of the DDR1 population forms ligan
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br Estrogen receptors activate mGluR
2021-01-29

Estrogen receptors activate mGluR signaling pathways In order to distinguish the opposing effects of estradiol on CREB phosphorylation, we turned to a “bottom-up” approach, working backwards from CREB phosphorylation to pharmacologically isolate the two signaling pathways (Boulware et al., 2005).
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We recently employed a functional drug screening
2021-01-29

We recently employed a functional drug screening approach to identify mithramycin as an inhibitor of EWS–FLI1. In our study, we employed a stepwise approach involving a luciferase primary screen and a novel multiplex PCR screen to evaluate over 50,000 compounds to identify mithramycin as an inhibito
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br Results br Discussion Fetal development
2021-01-29

Results Discussion Fetal development occurs under conditions of low oxygen tension and steady maternal glucose such that physiologic systems including the pancreas are functionally poised in the prenatal state. Postnatally, oxidative metabolism becomes dominant and intermittent feeding exposes
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br Results br Discussion The ubiquitin system has in recent
2021-01-29

Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i
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