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Next we elucidated that the Mtb enolase binds to
2021-02-27
Next, we elucidated that the Mtb enolase binds to host plasminogen with a high affinity. The KD value of 360nM for this interaction suggested an avid binding between the two proteins in vivo. This observation is also in conciliation with the observed KD values for enolase-plasminogen interactions in
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Ritonavir Modulating protein stability specifically inhibiti
2021-02-27
Modulating protein stability, specifically inhibiting ubiquitin E3 ligases, provides potential advantages over other druggable targets given the presence of biochemically multiple, unique pharmacophores within complexes that can bind a variety of small molecules [12]. The FBXO3 inhibitors used here
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BRD-9424 mg br Ubiquitylation of the TGF BMP pathway compone
2021-02-27
Ubiquitylation of the TGFβ/BMP pathway components Ubiquitylation is a reversible post-translational modification that is essential in many cellular regulatory mechanisms [20], [21]. During the ubiquitylation cascade, ubiquitin is attached to target proteins through the concerted actions of an E1-
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Because stimulation and blockade of
2021-02-26
Because stimulation and blockade of dopamine D2 receptor all cause a similar disruption of maternal behavior, one critical question is whether they do so through the same or different behavioral mechanisms. One idea is that stimulation or blockade of D2 receptors similarly suppresses maternal motiva
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Introduction Mycobacterium leprae the causative agent of
2021-02-26
Introduction Mycobacterium leprae, the causative agent of leprosy, affects skin, peripheral nerves and upper respiratory tract [1]. Although leprosy has been eradicated from most of the countries, it still affects approximately a quarter of a million people from India [2]. Details of many bacteriol
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The aniline R group was extensively explored and
2021-02-26
The aniline R2 group was extensively explored and a large variety of substitution was tolerated at several positions on the aryl ring (). Notably, substitution at the 3-position often gave increased potency. Increasing lipophilic bulk at this position gave increasing potency within an ether series (
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Primary human GBM neurospheres expressed high levels of the
2021-02-26
Primary human GBM neurospheres expressed high levels of the metabolic enzyme fatty acyl-CoA synthetase VL3 (ACSVL3) that were associated with CSCs self-renewal and tumorigenic capacity. ACSVL3 knockdown significantly decreased ALDH levels, indicating its contribution to cell metabolism and maintenan
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GMX1778 br How does DDR receptor activated to induce Osteoar
2021-02-26
How does DDR2 receptor activated to induce Osteoarthritis Alternation of joints by mechanical stress produces microcracks and deterioration of natural pores in subchondral bone provides GMX1778 for cross talk through diffusion of small molecules [26,27]. At early stage of OA, chondrocytes in the
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The pharmacokinetics properties of compound were evaluated i
2021-02-26
The pharmacokinetics properties of compound were evaluated in male Sprague Dawley rats following IV (0.7mg/kg) and oral (2.0mg/kg) dosing. The total body clearance and the terminal half-life were 0.73 L/h/kg and 5.1h, respectively. After oral administration the compound showed good bioavailability
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Recently it was reported that Crm is linked to
2021-02-26
Recently, it was reported that Crm1 is linked to spindle pole body (SPB) by Spc72 in Monastrol australia yeast [9]. Spc72 and Spc110 are two specific receptors of γ-tubulin complex (Tub4), which target Tub4 to SPB and mediate the nucleation of microtubules from SPB [20]. It was found that disrupting
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LY3023414 The anxiolytic like responses produced by anti SVG
2021-02-26
The anxiolytic-like responses produced by anti-SVG-30 suggests that CRF2 receptors mediate not only the elicitation of anxiety behavior induced by prior stress, i.e. conditioned freezing, but also unconditioned anxiety behavior induced by exposure to the unfamiliar environment of the elevated plus m
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ClC is a member of the voltage gated
2021-02-26
ClC-3 is a member of the voltage-gated chloride channel superfamily and has many roles in cell proliferation, apoptosis, TBCA progression and so on (Dai et al., 2005). A growing number of studies showed that ClC-3 encoded a volume-regulated Cl− channel (ICl,Vol) in heart, that could contribute to th
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Not all of the biological activities
2021-02-26
Not all of the biological activities exhibited by progestogens (Table 1) are mediated via binding to SRs. For example, the anti-estrogenic action of progestogens in the STAT5 Inhibitor synthesis is due to the progestogen-bound PR suppressing ER gene expression, and consequently the ability of the c
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br Genomic and non genomic signaling crosstalk As
2021-02-26
Genomic and non-genomic signaling crosstalk As exemplified in the previous sections, it is evident that the mechanisms of action of estrogen in the various cell targets represent a combination of complex multifactorial processes. Besides the independent genomic and non-genomic pathways described
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br STAR Methods br Acknowledgments
2021-02-26
STAR★Methods Acknowledgments We are grateful to Amaia Lujambio, James Fagin, and Ramon Parsons for providing cell lines and Evripidis Gavathiotis for critical reading of the manuscript. We would like to thank Saboor Hekmaty for providing expertise with RNA-seq analysis. P.I.P. would like to ac
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