• br Development of lorlatinib from crizotinib to a clinical

  2024-08-15

  

  Development of lorlatinib from crizotinib (1) to a clinical candidate (6) Xalkori (1, PF-02341066, crizotinib), was the first-in-class ALK inhibitor approved by the Unites States Food and Drug Administration (FDA) in 2011 as a first-line treatment for ALK+- NSCLC patients. This section describes

• 12-O-tetradecanoyl phorbol-13-acetate Although several studi

  2024-08-15

  

  Although several studies indicate that ALDH2 protects the heart from injury and maladaptive remodeling (reviewed in [11], [12], [13]), accumulating evidence indicates that deficiency of the enzyme could be protective as well. For example, mice expressing the defective Aldh2*2 mutation show lower al

• Numerous studies have shown that PUFA incorporation into the

  2024-08-14

  

  Numerous studies have shown that ω-3 PUFA incorporation into the lipid raft can affect the distribution and function of protein in the lipid raft by altering raft composition [25], [26], [27]. For example, DHA treatment excluded phospholipase D (PLD) from lipid raft toward non-lipid raft, resulting

• Endogenous adenosine systems have largely

  2024-08-14

  

  Endogenous adenosine systems have largely been implicated in drug actions by the demonstration that caffeine (non-selective A1R and A2AR antagonist) (see Section The issue of caffeine), in doses up to 7.5–10mg/kg, inhibits antinociception, and when this occurs, it WIKI4 is generally also seen with

• Our co IP data show

  2024-08-14

  

  Our co-IP data show that 5HT1A or 5HT2A receptors do not heterodimerize with mGluR1α receptors. Given that both 5-HT and mGlu receptors are GPCRs and produce anxiolytic effects, a degree of cooperativity via a functional cross-talk may still exist between these receptors [11]. In addition to the fun

• It has been reported that HT R

  2024-08-14

  

  It has been reported that 5-HT2R involves in type 2 diabetes mellitus and 5-HT-induced IR [22,23]. The present study also demonstrated that it is 5-HT2R rather than other 5-HT receptors, including 5-HT1BR and 5-HT7R, in the liver that mediates HFD-induced abnormality of hepatic lipid metabolism, and

• Acknowledgments br P c is expressed in

  2024-08-14

  

  Acknowledgments P450c17 is expressed in several steroidogenic tissues, including the adrenal cortex, the ovary, and the testes (). Thus, 17α-hydroxylase/17,20-lyase is a key enzyme required for the production of both cortisol and sex steroids. This enzyme defect blocks the synthesis of cortisol,

• Matrix metalloprotease inhibitors are increasingly available

  2024-08-14

  

  Matrix metalloprotease inhibitors are increasingly available and tested for other indications in clinical trials. The present study suggests that either ADAM10 or TACE inhibition alone will not maximally restore leukocyte Axl function. We found that lower doses of ADAM10/TACE inhibitors exhibit simi

• br Conflicts of interest br Acknowledgments The authors ackn

  2024-08-14

  

  Conflicts of interest Acknowledgments The authors acknowledge National Institute for Medical Research Development (NIMAD) project no. 940943 and National Research Institute for Science Policy (NRISP) no. 1456 for financial support of this work. AM appreciates National Institute for Genetic Eng

• br Regulatory mechanisms of ASK activity br

  2024-08-14

  

  Regulatory mechanisms of ASK1 activity The functions of ASK1 in disease ASK1 inhibitor As mentioned above, ASK1 plays a pivotal role in the pathogenesis of various diseases; hence, an ASK1 inhibitor has therapeutic potential. Although inhibitors of the ASK1 downstream kinases p38 and JNK ar

• In our study caspase and DRAM were identified as

  2024-08-14

  

  In our study, caspase3 and DRAM were identified as being involved in full-length AIFM1-induced apoptosis. Caspase3 is best known for its role in the execution phase of apoptosis in both intrinsic and extrinsic apoptotic pathways [17]. The members of the caspase family are generally in inactive pro-f

• AT signaling is distinct to that of

  2024-08-14

  

  AT2 signaling is distinct to that of AT1 (Kaschina and Unger, 2003). As shown here, opposite to the stimulating effect of AT1 signaling, it inhibits apelin secretion. Activation of AT2 receptor, which is also G-protein coupled, is known to decrease cAMP and cGMP levels by inhibiting adenylyl cyclase

• br Methodology br Antibiotics in lakes

  2024-08-14

  

  Methodology Antibiotics in lakes Antibiotic resistance genes in lakes Perspectives of study on ldk378 and ARGs in lakes Conclusion This paper systematically reviewed the distribution of antibiotics and ARGs in global lakes. A total of 57 antibiotics reported at least once in the wate

• Of the cardiovascular studies involving ARBs reported renal

  2024-08-14

  

  Of the cardiovascular studies involving ARBs, 3 reported renal outcomes. In the Losartan Intervention For Endpoint study, albuminuria was observed less frequently in the losartan than in the atenolol arm (7% vs. 13%; p=0.002) (5). In the Candesartan Antihypertensive Survival Evaluation in Japan tria

• In another study Yerra and Kumar used

  2024-08-13

  

  In another study, Yerra and Kumar (2016) used streptozotocin to induce diabetic neuropathy in rats. Mechanical/thermal hyperalgesia, motor/sensory nerve conduction velocities (MNCV and SNCV) and sciatic nerve blood flow (NBF) were evaluated. In vitro studies of Neuro2a (N2A) cell culture were perfor

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