• Derivatives of M that possess either

  2024-01-13

  

  Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these mithramycin to maintain 5-HTR antagonist properties as (+)-M100907 was demonstr

• cyp3a inhibitors br In patients with spina

  2024-01-13

  

  In patients with spina bifida and spinal cord injury, fecal incontinence is a serious issue that can impair activities of daily living and patient self-esteem. To address this Malone et al. first described the Antegrade Continence Enema (ACE) procedure in 1990 [1], which achieves continence by all

• Another significant group of reductase inhibitors is the ste

  2024-01-13

  

  Another significant group of 5α-reductase inhibitors is the steroidal 3-carboxylic Cy3.5 NHS ester (non-sulfonated) derivatives (relevant examples in Fig. 5), which were designed to mimic the putative enzyme-bound enolate intermediate. This was achieved by introducing sp2-hybridized centers at C3 an

• Drug resistance development often involves structurally un

  2024-01-13

  

  Drug resistance development often involves structurally un-related drugs and, specifically both conventional and targeted agents. IGROV-1/Pt1 Aloperine are characterized by resistance to cisplatin and reduced sensitivity to inhibitors of EGF-R and MEK, the up-stream activator of ERK1/2, associated w

• ATX LPA signaling in cancer is also well known

  2024-01-13

  

  ATX/LPA signaling in cancer is also well known to promote chemotherapy and radiotherapy resistance [7]. Furthermore, others have recently shown that endothelial-derived ATX activity in renal cell carcinoma promotes renal tumorgenesis and acquired resistance to sunitinib through an IL-8-mediated mech

• br Results and discussion br Conclusion In summary a series

  2024-01-13

  

  Results and discussion Conclusion In summary, a series of indazole-based derivatives were synthesized and SAR studies conducted, with view to the development of a novel Aurora kinases inhibitor. The carboxylic 7ACC1 receptor group extending from the C-3 position of the aniline and substituted

• Preliminary results of studies sponsored by the manufacturer

  2024-01-13

  

  Preliminary results of studies sponsored by the manufacturer of ETC-1002 have also shown positive results for monotherapy in statin-intolerant patients and for the combined use of the ACL inhibitor plus other cholesterol-reducing agents. In patients with a documented history of intolerance to statin

• climbazole In this study we found

  2024-01-13

  

  In this study, we found that ACL silencing is sufficient to impair myoblast differentiation and that this effect is accompanied by a decrease in MYOD early in the myogenic process and by a subsequent decline in fast MyHC protein climbazole at a later stage of differentiation (Figure 4J). Furthermor

• It has also been reported

  2024-01-13

  

  It has also been reported that defects in ATM or ATR signalling are synthetically lethal with PARP inhibition (Turner et al., 2008, Peasland et al., 2011, Yap et al., 2011, Michels et al., 2014), suggesting that combined inhibition of PARP and ATM or ATR may be an effective therapeutic strategy. In

• Receptor Subtypes and Their Function Critical Appraisal

  2024-01-13

  

  Receptor Subtypes and Their Function – Critical Appraisal Largely unselective ligands of the benzodiazepine binding site, such as diazepam, are known to elicit a wide range of in vivo effects including hypnosis, sedation, anxiolysis, and muscle relaxation. Genetically modified mice were introduced

• It is well known that neurosteroids such as testosterone

  2024-01-13

  

  It is well-known that neurosteroids such as testosterone and their metabolites endogenously modulate neural excitability in animals and humans. Testosterone has protective effects against seizures induced by KA and PTZ (Frye et al., 2001b; Reddy, 2004b). Estrogens, on the other hand, have proconvuls

• The androgen receptor gene AR is located on

  2024-01-12

  

  The androgen receptor gene (AR) is located on the X-chromosome and consists of eight exons in humans (Brown et al., 1989; Kuiper et al., 1989). The similar gene structure in mice, monotremes and marsupials indicates AR is highly conserved in mammals (Choong et al., 1998; Faber et al., 1991; He et al

• Some of previous immunohistochemical studies have compared

  2024-01-12

  

  Some of previous immunohistochemical studies have compared the levels of AR expression in low-grade versus high-grade and/or non-muscle-invasive versus muscle-invasive tumors. There was a significant or marginal decrease (Boorjian et al., 2004, Miyamoto et al., 2012b, Rau et al., 2011, Shyr et al.,

• Second the phosphorylation events e g Thr and Ser

  2024-01-12

  

  Second, the phosphorylation events (e.g., α-Thr172 and β-Ser108) needed for AMPK activation by small molecules binding at the ADaM or other sites remains unclear. Within the β-GBD, phosphorylation of β1-Ser108 was shown to be required for the activation by small molecules binding in the ADaM site, s

• Analyses of brain CSCs isolated from

  2024-01-12

  

  Analyses of EDC.HCl synthesis CSCs isolated from 24 pediatric and six adult brain tumors detected ALDH levels proportional to tumor type and aggressiveness. ALDH-expressing cells (ALDH+) formed spheroids while ALDH1 pharmacological inhibition by a combination of DEAB and RA decreased significantly s

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