• The gene SRD A encodes the reductase enzyme

  2024-05-06

  

  The gene SRD5A2 encodes the 5-α-reductase enzyme, which converts testosterone into dihydrotestosterone. Although dihydrotestosterone levels are considerably lower than testosterone, dihydrotestosterone has a five-fold stronger binding capacity to the androgen receptor and, thereby, a considerably mo

• exemplifies three of the compounds

  2024-05-06

  

  exemplifies three of the compounds investigated in the selection for a candidate drug (CD). Our first criteria was an IC XCT790 receptor as such did not show any genotoxicity in the SOS/umu assay, but this does not say anything about any possible genotoxicity of its metabolites or degradation prod

• br Experimental Procedures Additional information can

  2024-05-06

  

  Experimental Procedures Additional information can be found in Supplemental Experimental Procedures. Author Contributions Acknowledgments We thank all members of Lab of Health Chemistry for helpful discussions. This work was supported by Grant-in-Aid for Scientific Research (KAKENHI) from

• br Introduction The apelin receptor angiotensin receptor

  2024-05-06

  

  Introduction The apelin receptor (angiotensin receptor-like 1, APJ) is a seven transmembrane receptor (7TMR) that belongs to the class A peptidergic G protein-coupled receptors (GPCR) superfamily [1]. The endogenous ligands of APJ are the different isoforms of apelin (namely apelin-13, −17, and −

• br AMPK as a druggable

  2024-05-06

  

  AMPK as a druggable target AMPK signaling has attracted considerable attention within the past decades, owing to the capacity of pharmacological compounds (e.g., 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside [AICAR] and metformin) or natural compounds (e.g., resveratrol) to activate AMPK in

• To further demonstrate the significance of Nrf activation in

  2024-05-06

  

  To further demonstrate the significance of Nrf2 activation in the prevention of EGF-induced CRC growth by AR inhibitor, we examined the effect of fidarestat on EGF-induced cell viability in Nrf2-ablated cells. Our results suggest that AR inhibitor prevented the EGF-induced cell viability in control

• br Regulation of AHR Activity AHR activity

  2024-05-06

  

  Regulation of AHR Activity AHR activity is regulated in various ways. First, AHR protein levels are controlled via ubiquitin-mediated proteosomal degradation: Ligand binding induces AHR ubiquitination and subsequent degradation by the proteasome [5]. AIP, a component of the AHR chaperone complex,

• br ABCA and cancer drug response Overall the expression

  2024-05-06

  

  ABCA2 and cancer drug response Overall, the expression of ABC transporters has been linked with multidrug resistance phenotypes through the efflux of drugs via ATP-dependent transport. For example, 13 distinct transporters (ABCA2, ABCB1, ABCB4, ABCB11, ABCC1–6 ABCC10, ABCC11 and ABCG2) have been

• Mechanistically NAergic signaling in the VTA modulates neuro

  2024-05-06

  

  Mechanistically, NAergic signaling in the VTA modulates neuronal activity presumably via α1-AR. The majority of α1-ARs are found in the VTA are located presynaptically on unmyelinated clozapine-n-oxide and axon terminals of glutamatergic and GABAergic neurons. However, α1-ARs are also found on neur

• The direction of research then turned

  2024-05-06

  

  The direction of research then turned to investigating the long-term effects of adiponectin on insulin resistance. Adiponectin transgenic mice showed a reduction in insulin resistance and diabetes [5,6], while adiponectin-deficient mice showed mild insulin resistance with glucose intolerance, as wel

• Structure activity relationships biochemical metabolic and m

  2024-05-06

  

  Structure–activity relationships [23], [24], [25], [26], biochemical [24], [25], [26], [27], [28], [29], [30], [31], metabolic [19], [27], [28], [29], [30], [31], and molecular [32] investigations have demonstrated that the substrate specificity, as well as other characteristics of T. gondii adenosi

• Structure activity relationships biochemical metabolic and m

  2024-05-06

  

  Structure–activity relationships [23], [24], [25], [26], biochemical [24], [25], [26], [27], [28], [29], [30], [31], metabolic [19], [27], [28], [29], [30], [31], and molecular [32] investigations have demonstrated that the substrate specificity, as well as other characteristics of T. gondii adenosi

• br The cytochrome P enzyme hydroxylase lyase P is involved

  2024-05-03

  

  The cytochrome P450 enzyme 17α-hydroxylase/17,20-lyase (P450) is involved in the production of the C containing androgen precursors from the C containing steroids such as the pregnanes and progestins (). Steroids such as androstenedione (AD) and dehydroepiandrosterone (DHEA) are therefore synthesi

• In considering the roles of these enzymes in normal

  2024-05-03

  

  In considering the roles of these enzymes in normal physiology, given the importance of GLUT4-dependent glucose uptake and glucose-dependent fatty c-kit inhibitor synthesis for systemic metabolic homeostasis (Herman and Kahn, 2006, Herman et al., 2012), deletion of Acly in adipocytes results in a s

• AR is expressed in cell specific human ovarian follicles at

  2024-05-03

  

  AR is expressed in cell-specific human ovarian follicles at all stages of follicular development [25]. Administration of androgens in animals demonstrated initiation of follicular recruitment, stimulation of early stages of follicular growth, and increase in the number of growing follicles [26,27].

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