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We also identified Ubc as a functional
2020-05-05
We also identified Ubc13 as a functional E2 for LNX1 and determined the complex structure of LNX1–Ubc13~Ub, which depicts the first step of the ubiquitination process (Fig. 3a.). Comparing structural alignment of the RNF4 RING: Ubc13~Ub: Ube2V2 complex (PDB code 5AIU) [33] and the RNF4:Ubc13~Ub comp
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br Acknowledgments br The design of polyaromatic molecules a
2020-05-05
Acknowledgments The design of polyaromatic molecules able to bind to DNA is of significant importance for the development of anticancer and fluorescent imaging agents. Among them, 1,8-naphthalimide derivatives have received significant attention and have been extensively investigated for their
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br Conclusion New series of thiazolo d pyridazine and
2020-05-05
Conclusion New series of thiazolo[4,5-d]pyridazine and imidazo[2′,1′:2,3]thiazolo[4,5-d]pyridazine were designed and synthesized using thiazole as scaffold based on its previously observed activity as DHFR inhibitor. Compounds 13 and 43 (Fig. 9) proved to be the most active DHFR inhibitors with I
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Within the BLA both CRF and the CRF receptor have
2020-05-05
Within the BLA, both CRF and the CRF1 receptor have been shown to functionally regulate synaptic activity. In vivo, CRF release into the BLA originates from projections from the CeA (Roozendaal, Brunson, Holloway, McGaugh, & Baram, 2002). Central administration of both CRF and CRF1 agonists has been
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Self Determination Theory SDT as described by Ryan and Deci
2020-05-05
Self-Determination Theory (SDT), as described by Ryan and Deci (2000) is “an approach to human motivation and personality that uses traditional empirical methods while employing an organismic metatheory highlighting the importance of humans\' evolved inner resources for personality development and b
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ERR induces the expression of
2020-05-05
ERRγ induces the expression of P450c17 in MA-10 cells and in mouse primary Leydig cells (Fig. 2). Deletion mutant analysis of putative ERRγ-binding sites in the P450c17 promoter suggested that only the proximal third site located between −269 bp and −136 bp within the P450c17 promoter is functional
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br Acknowledgments We thank Jon Clardy Juan Manuel
2020-04-30
Acknowledgments We thank Jon Clardy, Juan Manuel Domínguez, José Francisco García Bustos, and the GlaxoSmithKline (GSK) Plasmodium falciparum dihydroorotate dehydrogenase project team for their contributions, helpful advice, and discussions. Introduction Dihydroorotate dehydrogenase (DHODH) i
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Introduction Quassinoids are natural products formed through
2020-04-30
Introduction Quassinoids are natural products formed through the oxidative degradation of triterpene derivatives with anti-inflammatory, antimicrobial, antineoplastic, and antiplasmodial effects (Chakraborty and Pal, 2013; Houël et al., 2013). They are characteristic ingredients of the family Simar
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From the general synthetic route we first synthesized a dire
2020-04-30
From the general synthetic route, we first synthesized a directed set of analogues of general formula , keeping the synthesis simple by using a symmetrical pyrazole (R=R=Me). The SAR of a set of 30 compounds in the GTPγS binding assay turned out to be quite tight: only 4 (13%) compounds showed moder
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We thank Dr Hongqiang Qin at Dalian Institute
2020-04-30
We thank Dr. Hongqiang Qin at Dalian Institute of Chemical Physics, Chinese Academy of Sciences for technical assistance in mass-spectrometric analysis. We thank Prof. Quentin Liu at Dalian Medical University and Prof. Qiang Shen at M.D. Anderson Cancer Center for helpful discussion and comments. Dr
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br Theory br Method To test our hypotheses
2020-04-30
Theory Method To test our hypotheses as shown in Fig. 1, we conducted a survey at an international media company (hereafter referred to as ‘MediaCo’) headquartered in the UK. Its 5500 employees are dispersed throughout the world, partly due to massive acquisitions within the past decade. In ex
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(R,S)-Anatabine Otherwise ES cells express high level of
2020-04-30
Otherwise, ES (R,S)-Anatabine express high level of histone lysine specific demethylase 1 (LSD1) expression. In this context, it is proposed that LSD1 inhibition may block the function of EWS-ETS proteins [70]. Furthermore, checkpoint kinase 1 (CHK1), a modulator of cell survival under the conditio
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A decrease in heme levels enables the
2020-04-30
A decrease in heme levels enables the phosphorylation of eIF2α by HRI and thereby inhibition of eIF2α activity. Indeed, the relatively small change in cytosolic heme levels in SZ ras pathway showed downstream functional consequences manifested by almost 50% elevation in the phosphorylation of eIF2α
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Hedamycin isolated from Streptomyces griseoruber
2020-04-30
Hedamycin, isolated from Streptomyces griseoruber, belongs to the highly cytotoxic pluramycin class of AGN 194310 receptor (Figure 3(c)). It consists of a planar anthrapyrantrione chromophore attached to two amino sugar rings at one end and a bisepoxide-containing side-chain at the other end (Figure
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GDC-0199 Till date several predictive models have
2020-04-30
Till date, several predictive models have been developed by different research groups to speed up the process of library selection and drug optimization (Walters et al., 1999, Caldwell, 2000, Plewczynski et al., 2006, Wang and Ramnarayan, 1999, Pogorelcnik et al., 2015, Greenbaum et al., 2002, Sadow
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