• We have previously disclosed the discovery of a

  2020-10-17

  

  We have previously disclosed the discovery of a 7-azaindole-3-acetic U 46619 CRTh2 antagonist chemotype 1 from HTS and its subsequent optimization to give 2 as a potent and orally bioavailable inhibitor of eosinophil shape change (SC) in human whole blood. Subsequent to disclosure of that work, othe

• br Materials and methods br Results br

  2020-10-17

  

  Materials and methods Results Discussion Recently it has been found that prostaglandins play an important role in modulating the host immune system [1,3,22,23], and some parasites produce these eicosanoid mediators to survive into their hosts [6,[10], [11], [12],24,25]. The discovery that p

• Some limitations of this study must

  2020-10-16

  

  Some limitations of this study must be noted. First, since the pretransplant evaluation of the T-cell immune response was performed just before transplantation, we cannot establish whether samples obtained at different times before the transplant would offer similar results, since end terminal disea

• Programmed cell death via apoptosis is associated

  2020-10-16

  

  Programmed cell death via apoptosis is associated with a series of morphological and biochemical characteristics, including cell shrinkage, the rapid increase of intracellular calcium, nuclear condensation, DNA fragmentation and the formation of apoptotic bodies. Known as a shared feature of most ap

• Programmed cell death via apoptosis is associated

  2020-10-16

  

  Programmed cell death via apoptosis is associated with a series of morphological and biochemical characteristics, including cell shrinkage, the rapid increase of intracellular calcium, nuclear condensation, DNA fragmentation and the formation of apoptotic bodies. Known as a shared feature of most ap

• AZ20 Selective inhibitor of phosphodiesterase type PDE I

  2020-10-16

  

  Selective inhibitor of phosphodiesterase type 5 (PDE5I) is commonly used for ED treatment. PDE5I exhibits its vasodilatory effect by inhibiting the degradation of cyclic guanosine monophosphate (cGMP), which relaxes the smooth muscle and allows increased blood flow for penile tumescence. Udenafil (D

• CCT241533 The inhibition of CYP activity

  2020-10-16

  

  The inhibition of CYP11β activity by NOR was 11- and 2.5-fold higher than those reported for the antifungal agents ketoconazole (IC50: 4.4μM) and clotrimozole (IC50: 1.0μM) (Fernandes and Porte, 2013). Furthermore, NOR was able to inhibit P450 aromatase activity in carp ovaries, although at a rather

• ERR is constitutively active in the absence of endogenous li

  2020-10-16

  

  ERRγ is constitutively active in the absence of endogenous ligand. However, several synthetic ligands that can repress or induce ERRγ function by disrupting ERRγ-coactivator interactions have been reported to date. The estrogen receptor modulators diethylstilbestrol (DES) and 4-hydroxytamoxifen (4-O

• So far several important flovonoids

  2020-10-16

  

  So far, several important flovonoids and polyphenoilc compounds were subjected to various human studies regarding their potential therapeutic and adverse effects (Ide et al., 2014; Turner et al., 2015; Witte et al., 2014) (Table 1). Resveratrol (trans-3,4, 5-trihydroxystilbene) is widespread stilbe

• Furan analogs and N methylpyrrole analogs

  2020-10-16

  

  Furan analogs and N-methylpyrrole analogs had completely different SARs. For example, replacement of the furan-2-sulfonyl moiety of 6 with the furan-3-sulfonyl moiety resulted in 8 with a decreased EP1 topotecan sale affinity and an increased antagonist activity, while the corresponding chemical mo

• br Acknowledgment We thank Professor Yuh Chang

  2020-10-16

  

  Acknowledgment We thank Professor Yuh-Chang Sun for providing helpful advice and the Ministry of Science and Technology of the Republic of China for financial support (grants MOST ). Introduction Past century has witnessed a tremendous increase in life expectancy of the human population, achi

• NT157 br Materials and methods br Results br Discussion

  2020-10-16

  

  Materials and methods Results Discussion Studies have suggested that the Hh signaling pathway, which plays as an essential autocrine viability factor for MFBs [10], [11], is a potential therapeutic target for liver fibrosis. Previously reported works have proven the effectiveness of the Hh

• C PHNO has been described as a full agonist

  2020-10-15

  

  [11C]-(+)-PHNO has been described as a full agonist at both D2 and D3 receptors [54,55]. [11C]-(+)-PHNO was initially developed as a PET radiotracer for imaging the high affinity state of the D2 receptor (i.e., highD2) as a means of measuring synaptic dopamine changes in response to pharmacologic ch

• Herein we explored by docking studies the effectiveness

  2020-10-15

  

  Herein, we explored by docking studies the effectiveness of replacing the dimethyl substitution at C (6) of dihydrotriazine with a folded azaspiro-containing substituent, along with the introduction of differently substituted phenyl- and benzyl-rings or alkyl chains, linked at the position 1 of the

• br Concluding remarks br Introduction Hypertrophic pachymeni

  2020-10-15

  

  Concluding remarks Introduction Hypertrophic pachymeningitis (HP) is a neurologic disorder characterized by diffuse or focal thickening of the intracranial or spinal dura mater, presenting with intracranial hypertension, cranial nerve palsy and spinal cord dysfunction (Kupersmith et al., 2004;

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