• br Antioxidative stress and anti inflammation Oxidative

  2024-11-13

  

  Antioxidative stress and anti-inflammation Oxidative stress is a major cause of reduced endothelial NO bioavailability in hypertension, and inflammatory response is thought to play an important role in these processes (Blake and Ridker, 2001, Landmesser et al., 2006). Reactive oxygen species (ROS

• Finasteride has been shown to be

  2024-11-13

  

  Finasteride has been shown to be a mechanism-based inhibitor of 5AR-2 [9]. Finasteride acts as an alternate substrate for 5AR-2 and is initially bound in an extremely stable enzyme-bound NADP-dihydrofinasteride adduct which is ultimately processed to dihydrofinasteride. The NADP-dihydrofinasteride

• br ARIs in the prevention of

  2024-11-13

  

  5ARIs in the prevention of prostate cancer Prostate cancer continues to be a leading cause of male deaths worldwide. In 2009, it was estimated there would be 192,280 new cases of prostate cancer with a predicted 27,360 deaths [25]. Because androgens, and specifically DHT, play a large role in bot

• In an effort to determine if one ARI was more

  2024-11-13

  

  In an effort to determine if one 5ARI was more effective than the other, the Enlarged Prostate International Comparator Study (EPICS) [17] compared treatment with finasteride and dutasteride in 1630 men over the age of 50 and concluded that after one year of treatment, both groups had statistically

• The benzimidazole group seems to be a key feature for

  2024-11-13

  

  The benzimidazole group seems to be a key feature for the excellent anti-tumor activity of galeterone (159), which motivated the synthesis of new steroidal inhibitors containing N-heterocyclic groups structurally related to benzimidazole. Thus, several 1H- and 2H-indazole derivatives of dehydroepian

• LPA binds to six specific cell surface GPCR receptors

  2024-11-13

  

  LPA binds to six specific cell surface GPCR receptors. The receptors LPA1 (lysophosphatidic receptor 1, formerly, Edg2), LPA2 (Edg4) and LPA3 (Edg7) belong to the endothelial differentiation gene family (EDG) and share sequence homology (50–60% amino cki synthesis homology) An et al., 1997, An et a

• In this paper we described synthesis

  2024-11-13

  

  In this paper, we described synthesis, biological evaluation and docking study of 3-aroyl-1-(4-sulfamoylphenyl)thiourea derivatives 4a–o as 15-lipoxygenase inhibitors. Results and discussion Conclusion We designed and synthesized a novel of thiourea derivatives containing phenylsulfonamide mo

• Calcineurin has been established to be a ubiquitous Ca activ

  2024-11-13

  

  Calcineurin has been established to be a ubiquitous Ca2+-activated serine phosphatase in the nervous system (Pyrzynska et al., 2001). It has been reported that the activation of calcineurin protects aromatase from autophagy-mediated protein degradation, implying that calcineurin-dependent dephosphor

• The contractility index showed positive inotropic effects of

  2024-11-12

  

  The contractility index showed positive inotropic effects of apelin in both doses at min 5 (Fig. 3, Fig. 5). Although the mean arterial pressure did not recover to the baseline, the contractility index increased, the relaxation index (tau) and ±dp/dt max returned back to their baseline, and left ven

• br Nanoparticle Conjugated Topoisomerase Inhibitors The safe

  2024-11-12

  

  Nanoparticle-Conjugated Topoisomerase Inhibitors The safety and efficacy of topotecan administered as LDM or MTD have been evaluated in several preclinical studies and a few clinical trials whose results showed that there can be significant adverse effects likely precluding its use in patients [5

• Breast Cancer Although androgens have been considered to be

  2024-11-12

  

  Breast Cancer: Although androgens have been considered to be a risk factor in prostate cancer they have been recommended to treat breast cancers. Even before the discovery of SERMs and aromatase inhibitors, steroidal androgens such as medroxyprogesterone and fluoxymesterone were used to treat breast

• Our research group has been

  2024-11-12

  

  Our research group has been involved by many years in the synthesis of new 2,3-benzodiazepin-4-ones (e.g. 1, Fig. 1) and in the characterization of their mechanism of action.15, 16, 17 Within the development of these compounds, we demonstrated that an improvement of AMPAR antagonism by 2,3-benzodiaz

• Imaging QTL studies may have several potential

  2024-11-12

  

  Imaging QTL studies may have several potential advantages over case-control studies, including increased power . Imaging endophenotypes of disease in QTL studies can separate patients and normal subjects more accurately and therefore limit the confound of including asymptomatic subjects in the contr

• Liver plays a pivotal role in

  2024-11-12

  

  Liver plays a pivotal role in metabolism of xenobiotic compounds, such as environmental contaminants and drugs. Some of these compounds generate hepatic damage and impair its function. It was well-known that 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) could induce pathological changes in mouse and ra

• br Acknowledgments br Introduction Within the classical secr

  2024-11-12

  

  Acknowledgments Introduction Within the classical secretory pathway, transmembrane and soluble cargos travel via the endoplasmic reticulum (ER) and Golgi apparatus en route to their final destinations [1]. However, at a post-Golgi level, trafficking routes can diverge. In this context, the tra

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