• The first natural product described as LO inhibitor was

  2023-05-29

  

  The first natural product described as 5-LO inhibitor was the polyphenol nordihydroguaiaretic W146 from the Mexican dessert plant Larrea divaricata in 1981 (Bokoch and Reed, 1981), short after the initial identification of 5-LO in 1979 (Borgeat and Samuelsson, 1979). Long time before mPGES-1 was dis

• Finasteride was the first steroidal reductase inhibitor appr

  2023-05-29

  

  Finasteride (13) was the first steroidal 5α-reductase inhibitor approved by the US Food and Drug Administration (FDA) in 1992 for treatment of BPH. In fact, long term clinical studies with this drug demonstrated a sustained reduction of the prostatic specific antigen and an overall improvement in BH

• However cancer and fibrotic diseases are the most extensivel

  2023-05-29

  

  However, cancer and fibrotic diseases are the most extensively studied disease states. ATX is connected to various cancers because it can stimulate chemokinesis and chemotaxis in melanoma cells. Upregulated ATX resveratrol has been reported in breast cancer,, prostate cancer, thyroid cancer, non-s

• Since innate immune responses represent

  2023-05-29

  

  Since innate immune responses represent the first defense against incoming infectious microorganisms, they are particularly engaged during the early stages of viral infections. Many innate defense mechanisms rely on the engagement of pattern recognition receptors (PRRs) which are conserved, germ lin

• Introduction Mitotic kinases play an essential role in mitos

  2023-05-29

  

  Introduction Mitotic kinases play an essential role in mitosis, Aurora and other mitotic kinases are often observed over-expression in human solid and many hematologic cancers. As one of serine/threonine kinases, Aurora kinase family is involved in centrosome maturation, mitotic spindle formation,

• br Perspective AA LA and other PUFAs and their lipid

  2023-05-29

  

  Perspective AA, LA and other PUFAs and their lipid metabolites play an important role in human diseases. 12/15-LOX which is the metabolic enzyme of them plays an important role in the pathogenesis-related diseases such as atherosclerosis, diabetic nephropathy, neurological diseases and other path

• The known crystal structures of class

  2023-05-29

  

  The known crystal structures of class C GPCR VFTs do not include attached TM domains, therefore current conformational data may not accurately reflect the dynamics of extracellular domains in full-length receptors. Nevertheless, compelling mechanisms of signal transduction can still be postulated. S

• In our study S aureus

  2023-05-29

  

  In our study, S. aureus activated the TLR signaling pathways of BMECs, thus inducing profibrogenic growth factor expression via NF-κB and AP-1. Since fibrosis is an important pathogenic process in both bovine and human mastitis, further studies on the molecular mechanisms of S. aureus infection are

• br Acknowledgments This work was

  2023-05-26

  

  Acknowledgments This work was supported by Grant-in-aid for Scientific Research (S) (20229008) (to T.K.), Targeted Proteins Research Program (to T.K.), the Global COE Research Program (to T.K.) and Translational Systems Biology and Medicine Initiative (to T.K.) from the Ministry of Education, Cul

• Since the cloning of ARs in the beginning of the

  2023-05-26

  

  Since the cloning of ARs in the beginning of the 1990s, the efforts to characterize them have led to the accumulation of a substantial amount of experimental data. Decades of site-directed mutagenesis (SDM; Box 1) studies, in combination with pharmacological data and computational modeling, have pav

• br Trauma and ACEs screening the past present and

  2023-05-26

  

  Trauma and ACEs screening: the past, present, and future Traditionally, allopathy’s biomedical model has utilized an etic perspective; the outsiders’ view of the problem. Development of diagnostic screening tools requires an etic approach, which relies heavily on a completely objective perspectiv

• Conclusion Twenty compounds with dinitrobenzoate scaffold

  2023-05-26

  

  Conclusion Twenty compounds with 3,5-dinitrobenzoate scaffold were synthesized and evaluated using cell-free and HWB assays for their 5-LOX inhibition activities. Compared to the parent compound, six compounds show significantly increased enzyme inhibition activities. The best compound, 3-tolyl 3,5

• Our co IP data show that

  2023-05-26

  

  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

• Another significant group of reductase inhibitors is the

  2023-05-26

  

  Another significant group of 5α-reductase inhibitors is the steroidal 3-carboxylic CTPB 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 and C4 and an anionic carboxy

• br Involvement of LPA receptors in cancer LPA s effects

  2023-05-26

  

  Involvement of LPA receptors in cancer LPA׳s effects are mediated by at least six different G protein-coupled receptors (LPA1–6). Human gastric and ovarian cancers overexpress the mRNA encoding LPA1 and LPA2 compared to healthy tissues [6], [11], [12]. Papillary and follicular thyroid cancers exh

14294 records 244/953 page Previous Next First page 上5页 241242243244245 下5页 Last page