• Several dehidropregnenolone derivatives functionalized at C

  2024-10-12

  

  Several 16-dehidropregnenolone derivatives functionalized at C3, C4, C5 and C6 (Fig. 7) were prepared and evaluated as 5α-reductase inhibitors bearing in mind that after the formation of an enzyme-steroid complex a nucleophilic portion of the enzyme attacks the double bond of the steroid through Mic

• An alternative more rarely used electron microscopy based ap

  2024-10-12

  

  An alternative, more rarely used, electron microscopy-based approach exploits labeling of phagosomes with DAMP (3-(2,4-dinitroanilino)-30-amino-N-methyldipropylamine). DAMP is a weakly basic compound which is membrane-impermeable once it has been protonated. This way, DAMPH+ accumulates in acidic in

• br The role of LOX

  2024-10-12

  

  The role of 12/15-LOX plays in autophagy Autophagy is a process by which cellular material is delivered to lysosomal to degrade the damaged organelles and proteins to facilitate nutrient recycling (Towers and Thorburn, 2016). There has been characterized three types of autophagy-macroautophagy, m

• A third motif involves the

  2024-10-12

  

  A third motif involves the toggle switch and consists of the conserved FxxCWxP sequence in TM6 of class A GPCRs (Hofmann et al., 2009, Rosenbaum et al., 2009). Rotamerization of Trp in combination with a kink caused by Pro facilitates the outward movement of TM6 upon activation (Hofmann et al., 2009

• Coincident with APJ receptor several cell

  2024-10-12

  

  Coincident with APJ receptor, several cell types in the body can synthesize apelin protein. For example, the highest apelin concentrations in the body have been found in the rat central nervous system, pituitary gland, lungs, cardiac muscle, gastrointestinal tract and mammary glands, with lower valu

• br Materials and Methods br Results br

  2024-10-12

  

  Materials and Methods Results Discussion XHP is a traditional Chinese anti-cancer medicine that is widely used for the treatment and adjuvant treatment of breast cancer. XHP has been shown to induce apoptosis in various breast cancer Cytarabine in vitro, including Hs578T, MCF-7, and MDA-MB

• br Findings br Discussion br Conclusions Midwives were more

  2024-10-12

  

  Findings Discussion Conclusions Midwives were more likely to provide effective antimalaria services (including two doses of IPT during the second and third trimesters of pregnancy) to pregnant women if Conflict of interest Authors’ contributions Funding Acknowledgements Resea

• Some of the mechanisms that involve

  2024-10-11

  

  Some of the mechanisms that involve 12-LOX as a potential pathogenic enzyme are illustrated in Fig. 2. Direct β cell effects associated with the stimulation of 12-LOX activity include the activation of second messengers c-Jun N-terminal kinase and p38 MAPK, both of which show increased phosphorylati

• br LO synaptic integrity and memory Interestingly

  2024-10-11

  

  12/15LO, synaptic integrity, and memory Interestingly, several groups have found that 12/15LO directly modulates synaptic function. Normandin and colleagues reported that pharmacological inhibition of 12/15LO modulates rat hippocampal long-term depression (LTD), a process by which neuronal synapt

• Role of APPL in endosomal signaling pathways Endosomes consi

  2024-10-11

  

  Role of APPL in endosomal signaling pathways Endosomes consist of distinct membrane subdomains within individual organelles and assist in the translation of extracellular stimuli via cytoplasmic transduction cascades to the nucleus [3], [74]. Endosomal abnormalities are associated with the pathogen

• Since forskolin is known to act directly at the

  2024-10-11

  

  Since forskolin is known to act directly at the catalytic site of adenylate cyclases near the ATP binding (Tesmer et al., 1997), the synergistic and/or permissive effect of gonadotropins on FSK activity must occur at the level of AC itself or very near, at the level of one of its direct partner. The

• If overexpression of ADK is sufficient to

  2024-10-11

  

  If overexpression of ADK is sufficient to induce spontaneous seizures, then reduction of ADK in engineered mice should prevent epileptogenesis. The generation of mice with moderately reduced levels of ADK in brain rather than complete ADK deficiency seems to be essential, since several lines of evid

• br Functional consequences of ADK

  2024-10-11

  

  Functional consequences of ADK regulation on astrocyte function As outlined above (see introduction), ADK critically regulates the extracellular adenosine levels in caspase pathway (Boison, 2006, Etherington et al., 2009). Changes in the levels of adenosine, as a result of the regulation of ADK

• We further analyzed selected hit compounds for their

  2024-10-11

  

  We further analyzed selected hit compounds for their ability to inhibit human AdK in intact cells. Human 1321N1 astrocytoma BIIB021 were utilized which were found to express AdK. The whole cell assay was performed using a 96-well format. The standard AdK inhibitor 5-iodotubercidin was employed as a

• Since pyrrolopyrimidine dithiolanes and both displayed parti

  2024-10-11

  

  Since pyrrolopyrimidine dithiolanes and both displayed particularly excellent levels of ACK1 inhibition, these analogs were viewed as potential candidates for further investigation in tumor xenograft experiments. While in vitro metabolic studies indicated that pyrrolidine was predicted to be sign

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