• br Materials and methods br Results

  2021-03-23

  

  Materials and methods Results Discussion Cisplatin, as one member of a class of platinum-containing anti-cancer drugs, which displays a great deal of clinical activity on a wide variety of solid tumors. In addition, cisplatin often used in combination with other chemotherapy drugs to treat

• Interest in the PGE EP pathway

  2021-03-23

  

  Interest in the PGE2/EP4 pathway is increasing given its diverse capability of regulating central nervous system activity [13]. EP4 has a protective function by reducing cerebral injury and improving functional outcome after stroke [14], and in suppressing Nifedipine mg inflammation [15]. The EP4 r

• Given its high frequency it is not

  2021-03-23

  

  Given its high frequency, it is not surprising that different strategies have been developed to restore the sensitivity of EGFR T790M-mutant formyl peptide receptors to EGFR inhibition. To date, several different strategies have been evaluated in both preclinical and clinical models, but only few ha

• br Ubiquitin Capture by the Mobile APC

  2021-03-23

  

  Ubiquitin Capture by the Mobile APC11 RING Domain Contributes to Processive Substrate Ubiquitylation Although the rules of Ub-mediated proteolysis are only beginning to emerge, the rate and order in which different APC/C substrates are degraded during the ion channel correlates with processivity

• We propose two different pathways for the production of this

  2021-03-23

  

  We propose two different pathways for the production of this species: either that described by Dooley [24], where the phenol ring is first activated by binding of its oxygen to copper, or one where a copper-peroxo species would directly react with an active site tyrosine residue (Scheme 1B). This se

• br Rationale Recently we have shown that the nasal

  2021-03-23

  

  Rationale Recently we have shown that the nasal CysLT2 receptor localized exclusively in blood vessels and the expression level of the CysLT2 receptor in patients with nasal allergy was higher than that in patients with non-allergic rhinitis (Shirasaki et al. Allergol Int 2013). We hypothesized t

• br Materials and methods br

  2021-03-23

  

  Materials and methods Results and discussion In the present work, we have applied two methodologies, CoMFA and CoMSIA to build 3D-QSAR models. There is no crystal structure available; therefore, an indirect method i.e., a ligand-based approach is the method of choice. The highly active molecul

• Benzoylmesaconitine br Acknowledgments This research was sup

  2021-03-22

  

  Acknowledgments This research was supported by grants from the Ministerio de Ciencia e Innovación (Grants SAF/FEDER 2010-17907; 2013-49076-P), Spain, Red de trastornos adictivos (RETICS RD12/0028//0003, Instituto de Salud Carlos III, Spain) and Fundación Séneca (15405/PI/10, Región de Murcia, Spa

• br Introduction Prostaglandins are important local mediators

  2021-03-22

  

  Introduction Prostaglandins are important local mediators in a host of reproductive processes including ovulation, fertilization, embryonic development, luteal regression, and parturition (Ushikubi et al., 2000). Prostaglandin E2 (PGE2) is among the more versatile prostanoids, and its effects app

• The action of pt PGE as an

  2021-03-22

  

  The action of 17-pt-PGE2 as an EP1 receptor agonist [34] was demonstrated in several experimental settings, including cancer, neurons, vascular system, kidney and was confirmed by application of EP1 receptor selective antagonists [35], [36], [37], [38], [39], [40], [41]. Receptor binding studies in

• Introduction Pain is frequently the first clinical

  2021-03-22

  

  Introduction Pain is frequently the first clinical symptom of head and neck carcinoma. Indeed, pain is the initial reason leading ∼70% of cancer patients to seek professional assistance (Lam & Schmidt, 2011; Rettig & D’Souza, 2015; Schmidt, 2014). Clinically, cancer-induced facial pain can be evoke

• Inappropriate heme metabolism has been linked to several neu

  2021-03-22

  

  Inappropriate heme metabolism has been linked to several neuropsychiatric disorders. In the hippocampi of Alzheimer's disease (AD) patients, for example, heme was found to binds intracellular amyloid β (Aβ), resulting in reduced heme bioavailability and its functional deficiency (Atamna and Frey, 20

• The development of novel approaches to

  2021-03-22

  

  The development of novel approaches to study GPCR-mediated transactivation in live Kif15-IN-1 is important, and this study describes a unique BRET-based quantification of Grb2 recruitment to the EGFR as a direct readout of GPCR-mediated transactivation. We have previously used the recruitment of Gr

• br E Ubiquitin Ligases Regulate Central and Peripheral T

  2021-03-22

  

  E3 Ubiquitin Ligases Regulate Central and Peripheral T Cell Tolerance During the random process of somatic recombination, T cell receptors (TCRs; see Glossary) that recognize self-antigens are commonly generated. Notably, meticulously precise filtering mechanisms, termed tolerance, are necessary

• Currently much effort has been made

  2021-03-22

  

  Currently, much effort has been made to design and synthesize ThDP analogs (such as ThTDP, ThTTDP, and triazole-ThDP in Fig. 2)8, 9, 10, 11, 12 as PDHc E1 inhibitors. These ThDP analog inhibitors, such as ThTDP and ThTTDP, can block the ThDP binding site, and exhibit significantly stronger binding a

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