• br AR signals and chemosensitivity

  2024-11-08

  

  AR signals and chemosensitivity in urothelial cancer A significant amount of patients with urothelial cancer fail to respond to cisplatin-based systemic chemotherapy, although it remains the mainstay of successful management of advanced disease. However, underlying mechanisms for chemoresistance

• In vivo CA mediate hypoxic nutritional and neurologic stress

  2024-11-08

  

  In vivo CA mediate hypoxic, nutritional, and neurologic stress responses. Stimulation of ADRα2A by these hormones to reduce β-cell metabolism has an obvious role in suppressing insulin secretion (Arun, 2004). Since β-cell metabolism and insulin secretion are linked, mechanisms that inhibit metabolis

• br Transparency document br Introduction G protein coupled

  2024-11-08

  

  Transparency document Introduction G protein-coupled receptors (GPCRs) comprise a diverse family of seven transmembrane domain-containing receptors represented by over 800 genes in humans. GPCRs respond to a range of stimuli, including peptides, hormones, growth factors, lipids, odorants, and

• Involvement of Adiponectin in the regulation of

  2024-11-08

  

  Involvement of Adiponectin in the regulation of imatinib resistance in human CML cells has not been hitherto examined. Therefore, in this study, we first established imatinib-resistant K562 CML cells, and then evaluated the effect of Adiponectin in reversing imatinib resistance. The data presented h

• In the past few years several experimental

  2024-11-08

  

  In the past few years, several experimental findings have demonstrated a pivotal involvement of adenosine also in driving the phenotypic switch of macrophages. In particular, the stimulation of A2A and A2B receptors seems to play a critical role in switching macrophages from M1 to M2 phenotype [37,6

• br Acknowledgements MC and PD were funded by the Michael

  2024-11-08

  

  Acknowledgements MC and PD were funded by the Michael J Fox Foundation (Grant ID 9969). We would like to thank Pierluigi Saba, Francesco Traccis and Barbara Tuveri for their technical assistance. Introduction In the prostate, androgens play a crucial role in normal, BPH and cancerous growth b

• SGI-1027 The introduction of a pyrazole

  2024-11-08

  

  The introduction of a pyrazole moiety into any position of the sterane core by cross-coupling reactions [13] or by Knorr construction from a CCC bis-electrophilic sterane precursor and an N,N binucleophile building block [17], [19] may serve as an example. Very few reports are to be found, however,

• Fig summarizes the oxidative metabolism of arachidonic acid

  2024-11-07

  

  Fig. 1 summarizes the oxidative metabolism of arachidonic Busulfan by lipoxygenases cyclooxygenases and cytochrome P450. Lipoxygenases in humans are expressed in a tissue-specific fashion: 5-LOX is mainly expressed in leukocytes, 12-LOX in platelets, and 15-LOX-1 in reticulocytes, eosinophils, and

• Receptors containing an x y subunit interface where

  2024-11-07

  

  Receptors containing an αx/γy subunit interface, where x=1, 2, 3, 5 and y=1–3, form a high-affinity binding site for benzodiazepines (Figure 1A), for the later developed Z-drugs of different chemotypes, and for a large number of chemically distinct research compounds 17, 18 (Box 1 for examples). For

• Thus phosphorylation of p was used

  2024-11-07

  

  Thus, phosphorylation of p38 was used to measure the intracellular potency of ASK1 inhibitors. In this assay, HEK293/AP-1luc indocid expressing human full-length ASK1 were incubated with compound for 18 h and then lysed and the level of phospho-p38 was quantified using the HTRF assay [33]. Resul

• br Angiotensin receptor neprilysin inhibitors Sacubitril

  2024-11-07

  

  Angiotensin receptor-neprilysin inhibitors Sacubitril/valsartan is the first-in-class ARNI, comprising of molecular moieties of valsartan (ARB) and a neprilysin inhibitor prodrug, sacubitril (AHU377) [51]. Upon ingestion, sacubitril is rapidly metabolised into an active neprilysin inhibitor, sacu

• We also found that the size of mEPSC amplitude was

  2024-11-07

  

  We also found that the size of mEPSC amplitude was reduced in unc-43 mutants, consistent with the decrease in synaptic GLR-1/GLR-2 heteromeric receptors. The decrease in mEPSC amplitude was not as great as that observed when measuring current in response to pressure application of glutamate. These d

• Recently Kamoshita et al evaluated a

  2024-11-07

  

  Recently, Kamoshita et al. (2016) evaluated a mouse model of retinal neuronal disturbance with the intraperitoneal injection of LPS and found that treatment with AICAR suppressed the reduction of conical function and decreased mRNA levels of TNF-α as well as improved mRNA levels of the mitochondrial

• br Experimental methods br Acknowledgments br

  2024-11-07

  

  Experimental methods Acknowledgments Introduction Long-term potentiation (LTP) and long-term depression (LTD) at excitatory synapses are thought to underlie experience-dependent learning and memory. These synaptic plasticity mechanisms are best characterized at hippocampal CA1 synapses, whe

• A candidate protein for the regulation

  2024-11-07

  

  A candidate protein for the regulation of AMPAR transport is CaMKII, a Ca2+-dependent kinase with diverse cellular functions. With respect to synaptic transmission, CaMKII is recognized as a key synaptic protein that is required to modify the number of synaptic AMPARs in response to LTP and LTD stim

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