• AG957 The Liver X Receptor and LXRs

  2021-02-20

  

  The Liver X Receptor-α and -β (LXRs, NR1H3 and NR1H2, respectively) are members of the nuclear receptor superfamily that play a central role in controlling cholesterol homeostasis [9], [10]. In macrophages, LXRs can decrease the cellular sterol burden by inducing expression of the cholesterol efflux

• Methods br Results br Discussion In

  2021-02-20

  

  Methods Results Discussion In this study we make the novel observation that villin-1 and gelsolin are down-regulated in response to diverse cellular stressors, including bacteria associated with the pathogenesis of CD. The high plasticity and dynamics of the brucine cytoskeleton are exploite

• br Activity based probes br Characterization of coronavirus

  2021-02-19

  

  Activity-based probes Characterization of coronavirus-encoded DUBs with activity-based probes To study the activity of specific DUBs, investigators frequently take advantage of the ~10kDa (monoUb or Ubl ABP) or ~20kDa (DiUb ABP) increase in MW on probe labeling. SDS-PAGE analysis or blotting f

• Although elevated production of cysLTs

  2021-02-19

  

  Although elevated production of cysLTs is characteristic of rhinosinusitis of diverse etiology, patients with aspirin-sensitive rhinosinusitis show even higher levels of cysLTs in the nasal mucosa, which are further enhanced by aspirin challenge., Elevated production of cysLTs in these patients may

• Several highly potent CysLT receptor

  2021-02-19

  

  Several highly potent CysLT1 receptor antagonists with large structural the have been developed. Beyond antagonists with structures analogous to cysteinyl leukotrienes, other subclasses comprise: (a) hydroxyacetophenones, (b) indoles and indazoles, (c) quinolines, benzothiazoles, and thiazoles. On

• ARA metabolites which are produced

  2021-02-19

  

  ARA metabolites, which are produced through cytochrome P450 (CYP450) enzymes influence cardiovascular homeostasis. Human CYP4A11 and CYP1A2 metabolize ARA to 20-hydroxyecostearonic directly (20-HETE) [11], which is a vasoconstrictor [12], platelet activator [13] and naturetic in the kidney [14]. On

• br CDK Regulators as Coactivators of NF B and

  2021-02-19

  

  CDK Regulators as Coactivators of NF-κB and STAT CDK regulating proteins also have the ability to control the inflammatory response. The p21CIP1 protein binds to and inhibits the activity of cyclin–CDK4/6 and cyclin–CDK1/2 complexes. Consistent with its ability to inhibit CDK activity, deletion o

• CRF and urocortin produce marked effects on the cardiovascul

  2021-02-19

  

  CRF and urocortin 1 produce marked effects on the AMG 487 when administered both i.v. or directly into the CNS (Parkes et al., 2001). Systemic i.v administration of CRF and urocortin 1 cause a marked and long-lasting reduction in mean arterial blood pressure in rats Briscoe et al., 2000, Lawrence e

• Alternatively procedural factors may have contributed to

  2021-02-19

  

  Alternatively, procedural factors may have contributed to the conflicting results. For instance, in order to have a more circumscribed area of drug diffusion, a volume of 0.05μl was injected in experiment 1b, which is four times lower than the one used in the mentioned plus-maze investigation. Besid

• br Criteria for ER targeted

  2021-02-19

  

  Criteria for ER-targeted fluorescent probes Survey of fluorescent probes Proposed approach to high affinity fluorescent steroidal ER probes Our proposed approach to the development of a new generation of fluorescent estrogen receptor imaging agents employs many of the elements present in th

• CM AVM and VOGM are thought to be two distinct

  2021-02-19

  

  CM-AVM and VOGM are thought to be two distinct disorders, with CM-AVM characterized by atypical CMs, with or without AVM in variable body parts, while VOGM is a type of cerebral AVM [16]. The fact that VOGM is infrequently reported as the AVM in CM-AVM patients, and CMs are quite often identified in

• Our previous high throughput screening

  2021-02-19

  

  Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based XEN445 assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21], [22], [23],

• br Materials and methods br Results br

  2021-02-19

  

  Materials and methods Results Discussion The EP4 mk 801 for PGE2 is similar to the EP1, EP2 and EP3 receptors in that they all have seven transmembrane segments and are coupled to Gα subunits of heterotrimeric G proteins, with a different Gα subunit for each receptor (Sugimoto and Narumiya

• br Methods br Results br Discussion The findings of

  2021-02-18

  

  Methods Results Discussion The findings of this study indicate that an ET system including ET-1 and ET-2 as well as ET receptors are present in the retina and RPE/choroid, and are up-regulated by both hypertension and diabetes. Specifically, individual antagonism of the ETRA or ETRB deliver

• br Experimental Procedures br Author Contributions M B with

  2021-02-18

  

  Experimental Procedures Author Contributions M.B., with input and help from T.T.H., conceived the project, designed and performed the experiments, analyzed the data, and wrote the manuscript. B.B.B. and F.D.M. synthesized the wild-type and (nonhydrolyzable, NH) Ub tetramers and contributed Fig

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