• Since the cloning of ARs in

  2024-09-06

  

  Since the cloning of ARs in the beginning of the 1990s, the efforts to characterize them have led to the accumulation of a substantial amount of experimental data. Decades of site-directed mutagenesis (SDM; Box 1) studies, in combination with pharmacological data and computational modeling, have pav

• Telatinib In conclusion two novel series of furo pyrimidin

  2024-09-06

  

  In conclusion, two novel series of furo[2,3-]pyrimidin4-amines and 7-pyrrolo[2,3-]pyrimidin-4-amines which exhibit potent in vitro inhibitor activity against ACK1 have been identified and evaluated. 1,3-Dithiolane-substituted pyrrolopyrimidine displays excellent ACK1 cellular inhibition, good kinas

• Regarding androgens it is known that they

  2024-09-06

  

  Regarding androgens, it is known that they are also essential for reproductive success (Walters et al., 2010). At the molecular level, their effects are produced mainly by dihydrotestosterone (DHT), arising from the conversion of testosterone by the enzyme 3-oxo-5-alpha-steroid-4-dehydrogenase (enco

• LO is a soluble kDa enzyme composed of an

  2024-09-06

  

  5-LO is a soluble 78 kDa enzyme, composed of an α-helix-rich catalytic domain and a regulatory β-sheet-rich C2-like domain. Depending on the cell type, 5-LO may be located in the cytosol, in the nucleoplasm, or in both compartments (Werz, 2002). Upon cell stimulation by agents that elevate intracell

• Mesoridazine Besylate A review has recently been published t

  2024-09-06

  

  A review has recently been published to evaluate the potential effects of food, alcohol and Mesoridazine Besylate juices on the pharmacokinetics and pharmacodynamics of the drugs for BPH. The authors reviewed the PubMed database during the years 1991–2015. In addition, a digital version of Stockley

• Ac-IETD-pNA synthesis Materials and methods br Results br

  2024-09-06

  

  Materials and methods Results Discussion ATX plays a significant role in initiating and sustaining tumor metastasis [43]. LPA stimulates cell proliferation, migration and survival by acting on its cognate G-protein-coupled receptors. Aberrant LPA production, receptor Ac-IETD-pNA synthesis an

• If the lack of specificity

  2024-09-06

  

  If the lack of specificity and the high pleiotropy may represent a problem in view of the potential chemotherapeutic features of autophagy-inducing agents, it TMP269 may switch into an advantage in the case of chemopreventive strategies. In fact, as non-pharmacologic interventions such as limited ca

• br The future of cancer therapeutics with

  2024-09-06

  

  The future of cancer therapeutics with Aurora kinase inhibitors Involvement of Aurora kinases in deregulating multiple tumor suppressor and oncogenic pathways together with the preclinical findings on the efficacy of Aurora kinase inhibitors in attenuating growth of tumor FSLLRY-NH2 suggests tha

• br Materials and methods br Results br

  2024-09-05

  

  Materials and methods Results Discussion The current treatment modalities for colorectal cancer are hampered by various issues such as high acquired resistance, long-term complication with potential of cancer recurrence, severe side-effects and poor therapeutic index [50], [51], [52]. Compl

• Apelin is a peptide hormone and an endogenous ligand

  2024-09-05

  

  Apelin is a peptide hormone and an endogenous ligand for a G protein-coupled receptor named APJ [7], [8], and apelin and APJ are widely expressed in human organs including hypothalamus, heart, lungs, kidneys, adipose tissue, muscles, and others [9]. Apelin is initially synthesized as a 77-amino-acid

• Apelin is involved in various

  2024-09-05

  

  Apelin is involved in various physiological functions, including corticotropin releasing factor contraction (Ashley et al., 2005), vasodilatation (Jia et al., 2007), feeding control (Valle et al., 2008), and metabolic homeostasis (Higuchi et al., 2007, Dray et al., 2008, Attane et al., 2010). Its p

• Intriguingly androgens may also have

  2024-09-05

  

  Intriguingly androgens may also have an indirect effect on AR gene expression through inhibition of the GATA2 transcription factor gene (He et al., 2014) (Table 1). Using ChIP-seq, GATA2 was found to bind to a regulatory element 5.5 kb upstream of the TSS of the AR gene and enhanced transcription, w

• The reactions and the control mechanisms described are

  2024-09-05

  

  The reactions and the control mechanisms described are all supported by observations. For example the reactions require that different compounds are formed in different groups of NAD+ cells and this has been observed [15]. Intravenous injection of glycine results in reduced utilisation of glucose b

• cgk br Discussion The patient presented initially only with

  2024-09-05

  

  Discussion The patient presented initially only with parietal symptoms in the form of acalculia, visuo-spatial deficits, and visuo-perceptual deficits and dressing apraxia. He also had simultognosia as early symptoms. Later when the disease progressed he had recent memory deficits and language in

• Within the PARP family TIPARP is most evolutionarily

  2024-09-05

  

  Within the PARP family, TIPARP is most evolutionarily conserved with PARP12 (ARTD12) and PARP13 (ARTD13) [27,28,41]. All three proteins contain at least one RNA-type CCCH zinc finger domain, a poly-ADP-ribose binding WWE domain and a PARP catalytic domain (Fig. 1). PARP13 is catalytically inactive,

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