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Compounds and were evaluated for their
2022-01-07
Compounds and were evaluated for their pharmacokinetic properties in rats and the results are summarized in . Following intravenous (IV) administration, both compounds displayed low clearance (CL), short half-lives (t) and low volumes of distribution (V). When dosed orally as a solution, exposure
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Our results further indicate that low expression of
2022-01-07
Our results further indicate that low expression of p300/CBP in CRC is directly associated with poor clinical therapeutic outcome of 5-FU treatment, potentially providing a new set of biomarkers to predict chemo-sensitivity. Although the ability of low expression of p300/CBP to predict poor prognosi
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n-acetyl-l-cysteine Glycine released from astrocytes as well
2022-01-07
Glycine released from astrocytes as well as neurons is also known as a co-agonist of NMDAR (Roux and Supplisson, 2000). Neuronal glycine in mouse hippocampus might be released from glutamatergic terminals (Muller et al., 2013) that express functional n-acetyl-l-cysteine receptors (Rodriguez et al.,
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To efficiently develop bioactive ligands even if the
2022-01-07
To efficiently develop bioactive ligands even if the structural information of the target protein is unknown, we have presented a three-dimensional structural diversity-oriented strategy based on structural properties of a chiral cyclopropane. Our strategy has allowed us to design and synthesize a s
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Allergic rhinitis characterized by inflammation
2022-01-07
Allergic rhinitis, characterized by inflammation of the nasal membrane, results from an over-activated immune system exposed to N6-Cyclopentyladenosine in sensitized individuals, and is associated with nasal congestion, rhinorrhea, sneezing, and pruritus. As histamine is a key mediator in triggerin
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In addition to acting as the gatekeeper for
2022-01-07
In addition to acting as the gatekeeper for the metabolic and antioxidant roles of glucose, HKs have also been found to regulate mPTP opening directly. First described in the cancer field, the high-affinity HK isoforms HK1 and HK2 are strongly anti-apoptotic when bound to the outer mitochondrial mem
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Importantly recent in vivo results demonstrated that combini
2022-01-07
Importantly, recent in vivo results demonstrated that combining an HDACi and a IKK inhibitor significantly reduced ovarian tumor growth compared with either inhibitor alone [26]. The slowest tumor growth in the HDACi/IKK inhibition combination group was associated with the lowest CXCL8 tumor and pla
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sc4 library sale Mapping PPI networks is challenging as it i
2022-01-07
Mapping PPI networks is challenging, as it is difficult to express and purify large variaties of sc4 library sale in sufficient quantities to allow the study of interactions between them. Membrane-bound proteins are particularly difficult to purify in functional form due to their amphiphilic nature
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It is interesting that SEC significantly inhibited
2022-01-07
It is interesting that SEC significantly inhibited cell migration and EMT in PC3 cells expressing a low RKIP level and HEK293T RKIP−/− cells, while had no effect on HEK293T RKIP+/+ cells. These observations can be interpreted that the RKIP-ANXA7 association may block SEC-induced ANXA7 GTPase activat
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In addition to gonadotropes GnRHRs have also been
2022-01-06
In addition to gonadotropes, GnRHRs have also been detected on somatotropes, lactotropes, thyrotropes, melanotropes, somatolactin (SL) cells, and/or corticotropes using immunohistochemical, radioligand-binding, or mRNA expression approaches across species; including fishes, rats, and humans (La Rosa
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In the present study co administration
2022-01-06
In the present study, co-administration of TM (AT1 receptor blocker) and PD (AT2 receptor blocker) were made in ischemic mice to explore the significance of AT2 receptors in cerebral ischemia while blocking central AT1 receptors. Also to prove that AT2 receptors should be free after ischemic injury
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Recently unimolecular multi functional peptides that combine
2022-01-06
Recently, unimolecular, multi-functional peptides that combine GLP-1RA activity with AZD2932 and/or GIP activity have been suggested as new therapeutic agents for glycaemic and weight control. In rodents, dual GIP and GLP-1 receptor agonists achieve significantly better glucose control and weight lo
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br Conclusions There are a number of factors that affect
2022-01-06
Conclusions There are a number of factors that affect the transit of solutes through gap junction channels. Fig. 4 provides a simplified illustration of those factors. First is the cytoplasmic vestibule through which all permeable solutes must pass to gain access to the pore. In an equivalent cir
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br Therapeutic approaches exploiting Cx function Due to
2022-01-06
Therapeutic approaches exploiting Cx43 function Due to their potential role in cancer metastasis, attempts have been made to alter connexin function to inhibit cancer growth. Therapeutic approaches include Cx43 peptide mimetics, Cx43 inhibitors, chemical agents capable of enhancing Cx43 function,
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As with the GSIs there are again major concerns that
2022-01-06
As with the GSIs, there are again major concerns that GSM therapy in patients with symptomatic AD is almost certain to fail, unless the compound has additional mechanism of action not linked to Aβ that prove to beneficial [52]. Although Aβ1–42 or other longer Aβ peptides are critical for initiating
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