• Under some pathological conditions AT R internalization is d

  2023-03-11

  

  Under some pathological conditions, AT1R internalization is decreased when agonist exposure is prolonged. This weakens or removes the AT1R desensitization effect and leads to AT1R and downstream signal overactivation. AT1R overactivation can result in continued biological effects such as sustained v

• Evidence from basic science studies suggests that Cd may

  2023-03-11

  

  Evidence from basic science studies suggests that Cd may play a role in prostate cancer through disruption of the androgen receptor (AR). AR, a hormone-activated transcription factor, is the key driver of prostate cancer progression [6]. Ironically, the AR is also required for normal prostate growth

• Perforation of the surface membrane however is

  2023-03-11

  

  Perforation of the surface membrane, however, is not the only mechanism of calcium dysregulation by Aβ at the presynaptic terminals. When in excess, both monomers and oligomers modulate biophysical properties of voltage-activated calcium receptor tyrosine kinase as well as calcium release from the

• Here we provide evidence that

  2023-03-11

  

  Here, we provide evidence that NO contributes to changes in synaptic strength, but also offer an explanation as to why previous attempts to link NO to LTP have often failed. Our results describe a model by which cycling AMPARs, held in intracellular pools, are rapidly delivered to the membrane surfa

• In this study we designed and synthesized

  2023-03-11

  

  In this study, we designed and synthesized two ALK PROTACs (degraders), 5 (MS4077) and 6 (MS4078), by linking ceritinib and pomalidomide [45] through two different linkers. Using human ALCL and NSCLC cells, we characterized both compounds in a battery of assays to demonstrate their effects on reduci

• In a recent series of studies from

  2023-03-11

  

  In a recent series of studies from our laboratory, to characterize the contractile systems within the rat l-name synthesis wall, three conditions were identified that led to detrusor activity: spontaneous micro-contractions, electrical field stimulated (EFS) contractions and muscarinic agonist induc

• The excellent potencies selectivities and improved PK associ

  2023-03-11

  

  The excellent potencies, selectivities and improved PK associated with the piperazine class triggered more extensive off-target screenings of the highlighted compounds. A screen of more than 100 enzymes, receptors, and ion channels resulted in activity at the norepinephrine transporter (NET). This

• Our studies suggest that AdipoR and

  2023-03-11

  

  Our studies suggest that AdipoR1 and AdipoR2 genes are expressed in multiple tissues in the chicken wherein both receptors are likely to mediate the physiological effects of adiponectin. We determined the relative expression of AdipoR1 and AdipoR2 mRNA in various tissues and found that skeletal musc

• The reduced IFN production seen with BPAL

  2023-03-11

  

  The reduced IFNγ production seen with BPAL10-primed splenocytes could potentially be attributed to the impaired intracellular survival of B. pertussis, thereby leading to a weakened induction of cell-mediated immunity. Earlier studies have suggested an antimicrobial role of IFNγ in mediating the eli

• Toxicity is the main reason

  2023-03-11

  

  Toxicity is the main reason for the failure at all stages of the new drug development process. The major part of safety-related attrition occurs at preclinical phases while predicting preclinical safety liabilities earlier in the drug development process. This strategy enables the design and/or sele

• Specifically equity injections in a multinational affiliate

  2023-03-11

  

  Specifically, equity injections in a multinational affiliate X located in an ACE country can be passed on as lending to another group member Y located in a different country with a high corporate income tax rate. For the group member Y, the interest on the loans is tax deductible, and at the same ti

• Another topic for research will be the combination of other

  2023-03-11

  

  Another topic for research will be the combination of other cytotoxic agents with Aurora kinase inhibitors. Particularly interesting might be the combination of Aurora kinase inhibitors and agents that depend on the spindle checkpoint for their activity, such as the taxanes, given the importance of

• Aurora A or B selective and pan aurora inhibitors have

  2023-03-11

  

  Aurora -A or -B selective and pan-aurora inhibitors have demonstrated different preclinical and clinical therapeutic efficacies [2,[19], [20], [21], [22], [23]]. For example, clinical trials for a pan-Aurora inhibitor VX-680 (developed by Vertex) were halted at phase II for toxicity reasons (one cas

• There is limited information regarding

  2023-03-11

  

  There is limited information regarding hyperargininemia incidence or prevalence. Reports of incidence vary by an order of magnitude: 0.5 to 5.0 per million [5], [6]. A relatively large U.S. study estimated 1.1 cases per million births [7], but it used an indirect methodology that introduces uncertai

• Immunohistochemistry in tissue samples showed the expression

  2023-03-09

  

  Immunohistochemistry in tissue samples showed the expression of several nuclear receptor co-activators, including NCOA1, NCOA2, NCOA3, CREBBP, and EP300, in 85–100% of Norfloxacin hydrochloride tumors even some of which lacked AR expression (Boorjian et al., 2009). Knockdown of each co-activator als

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