• ALK fusion positive NSCLC is clinically actionable because

  2025-03-03

  

  ALK fusion-positive NSCLC is clinically actionable because it can be targeted by several FDA-approved drugs, including the first generation TKI crizotinib, which is a dual inhibitor to MET and ALK [15], and the second generation inhibitors, alectinib and ceritinib, both of which are highly-selective

• AhR was proven to participate in

  2025-03-03

  

  AhR was proven to participate in carcinogenesis. Its high expression was demonstrated in a variety of tumors, i.e. pancreatic, prostate, urinary tract, lung and papillary thyroid carcinoma (Safe et al., 2013, Mian et al., 2014). However, cell line studies showed variable AhR levels/responses. AhR kn

• The central problem in amnesia developing following

  2025-03-03

  

  The central problem in amnesia developing following impairment of long-term memory consolidation or reconsolidation is a question of the underlying mechanisms, whether it is caused by impairment of retrieval or memory storage mechanisms [3,8,9,[15], [16], [17], [18]]. To answer this question, severa

• br Acknowledgments This work was supported by a

  2025-03-03

  

  Acknowledgments This work was supported by a grant of the Romanian National Authority for Scientific Research, CNCS – UEFISCDI, project no. PN-II-ID-PCE-2011-3-0571, awarded to F.A.M. D.V.N. was co-financed from the European Social Fund through Sectorial Operational Program Human Resources Develo

• The first rationally designed dual

  2025-03-03

  

  The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic 23401 zip code - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been synt

• From an historical perspective ligands for GPCRs

  2025-03-01

  

  From an historical perspective, ligands for GPCRs (adrenaline, serotonin, Tipiracil hydrochloride or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endogenous

• ML 221 In conclusion we report that the widely prescribed dr

  2025-03-01

  

  In conclusion, we report that the widely prescribed drug VPA exerts therapeutic effects on optic nerve demyelination and retinal degeneration in a mouse model of MS. Our findings raise an interesting possibility that combination therapy of VPA and ASK1 inhibition may be useful for treatment of autoi

• br Roles of apelin and APJ

  2025-03-01

  

  Roles of apelin and APJ in cardiovascular diseases Therapeutic potential of apelin/APJ in cardiovascular diseases Since the apelin/APJ system plays a key role in the occurrence and development of cardiovascular diseases, it seems logical to presume that targeting this axis should be feasible a

• AT signaling is distinct to that

  2025-03-01

  

  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 Experimental section br Acknowledgements The authors than

  2025-03-01

  

  Experimental section Acknowledgements The authors thank Prof. Yongbing Cao from School of Pharmacy, the Second Military Medical University, for providing the fluconazole-resistant strains of Candida albicans(strain 100 and strain 103). This work was supported by Program for Innovative Research

• Some of previous immunohistochemical studies have compared t

  2025-03-01

  

  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.,

• Based on the general structure function principle in

  2025-03-01

  

  Based on the general structure-function principle in biology [[19], [20], [21]], toxic oligomers are expected to have well-defined three-dimensional structures to carry out their pathological functions. A common amyloid toxicity mechanism also suggests that toxic oligomers of different amyloid prote

• We have recently begun to demonstrate

  2025-03-01

  

  We have recently begun to demonstrate this concept by reporting a novel class of β-hairpin peptidomimetics, built on a piperidine-pyrrolidine semi-rigid β-turn inducer [12] and bearing two recognition pentapeptide sequences, designed on oligomeric and fibril structures of Aβ1-42 (compound 1, Fig. 1)

• The reactions and the control

  2025-03-01

  

  The reactions and the control mechanisms described are all supported by observations. For example the reactions require that different compounds are formed in different groups of MOG (35-55) cells and this has been observed [15]. Intravenous injection of glycine results in reduced utilisation of gl

• The lactam emerged as lead candidate due to its high

  2025-03-01

  

  The lactam (6) emerged as lead candidate due to its high selectivity, outstanding potency (against ALK or in clinically known ALK mutants), low in vitro clearance, and low efflux potential. The lactam (6) was selected for further profiling against the resistant ALK mutants. Preclinical rat pharmacok

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