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Integrin engagement triggers activation of several signaling
2021-09-22

Integrin engagement triggers activation of several signaling pathway including Fak, which is recognized as the key signal transduction factor in the integrin signaling pathway that functions by activating downstream signaling in focal adhesion plaques. Whether changes in integrin-FAK signaling pathw
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br Experimental procedures br Results br Discussion This
2021-09-22

Experimental procedures Results Discussion This study demonstrates that the genetic disruption or pharmacological inhibition of FAAH completely prevented all manifestations of pain symptoms in an NTG-induced migraine animal model. Thus, FAAH disruption or blockade abolished the activation o
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br Introduction Nasopharyngeal carcinoma NPC is a head
2021-09-22

Introduction Nasopharyngeal carcinoma (NPC) is a head and neck epithelial malignancy with high prevalence in southern China, southeast Asia, and northern Africa [1,2]. NPC is caused by a combination of factors: infection with Epstein-Barr virus (EBV), environmental influences, and heredity [3]. A
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A compound structurally similar to PF has been developed by
2021-09-22

A Rifapentine structurally similar to PF-03654746 has been developed by Pfizer (PF-03654764), with a minor change in the substituent attached to the cyclobutanecarboxamide moiety (Wager et al., 2011). This compound, with the chemical name trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-
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Arena Pharmaceutical introduced a biaryl sulfone derivative
2021-09-22

Arena Pharmaceutical introduced a biaryl sulfone derivative with antagonistic activity at H3Rs known as APD-916, ((R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine), which was rationally designed from corresponding sulfonamides in order to yield compounds with short dura
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Both plant hormones and some second
2021-09-22

Both plant hormones and some second messengers are involved in Fe-deficiency-related responses in plants (Kobayashi and Nishizawa, 2012). Among these second messengers, nitric oxide (NO) accumulation was induced by Fe deficiencies in tomato and Arabidopsis roots, and it acts as the downstream signal
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Etoposide VP a semisynthetic podophyllotoxin derivative agen
2021-09-22

Etoposide (VP-16), a semisynthetic podophyllotoxin derivative agent, is widely used as a chemotherapic treatment for many cancers (Hande, 1998). VP-16 has been known that its activity is mediated by the interaction with topoisomerase II (an ATP-dependent nuclear enzyme) which regulates DNA topology
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Adenosine Kinase Inhibitor hydrate receptor As natural ligan
2021-09-22

As natural ligands of GPR120, several long chain polyunsaturated fatty acids (Lc-PUFAs) have been demonstrated to modulate the 3T3-L1 adipogenic differentiation. However, the effects of the Lc-PUFAs are inconclusive. DHA is shown to inhibit, promote or even not affect the differentiation of preadipo
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Firstly the impact on activity and selectivity
2021-09-22

Firstly, the impact on activity and selectivity was made by replacing the 2, 3-di-F substitution of ring A with 2,3-OCHO- () and 2-NO () substitutions, and replacing the 3, 5-di-F substitution of ring B with 3,5-di-OMe () and 3,5-di-Me () substitutions. Compound kept moderate activity (EC = 220 nM)
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br Conclusion br Author statement br Acknowledgments br Intr
2021-09-22

Conclusion Author statement Acknowledgments Introduction The hypothalamic-pituitary-gonadal (HPG) axis is an important neurohormone network for vertebrates that regulates their gonadal development and maturation, guarantees their pubertal development and maintains their normal reproducti
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The aim of our study was to investigate
2021-09-22

The aim of our study was to investigate the polymorphisms of RAGE and glyoxalase I gene and sRAGE serum levels in patients with pathological pregnancy trying to describe the genetic background of pathological pregnancy or to find a new biochemical marker (sRAGE) of these pathological states in pregn
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Herein we report the discovery of AM
2021-09-22

Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative t
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There are two ways to transport FFAs
2021-09-22

There are two ways to transport FFAs into cells. First by passive diffusion. Second as the putative long-chain fatty Dihydroeponemycin transporters are proposed, CD36 the plasma membrane-associated fatty acid-binding protein (FABPpm) and fatty acid transport proteins (FATP) [11], where CD36 is resp
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br Indirect GLI antagonists br
2021-09-22

Indirect GLI antagonists Direct GLI antagonists Concluding remarks Targeting GLI effectors represents a promising therapeutic strategy for cancer treatment. This is particularly relevant for certain tumors, such as MB, since, although classified into four distinct molecular groups (Hh- or W
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The widespread involvement of HH GLI in human
2021-09-22

The widespread involvement of HH/GLI in human malignancies has initiated a remarkable effort to identify selective HPIs. As shown in Table 2.1, most of these small molecule inhibitors target the essential effector protein SMO, which should lead to pathway abrogation by eventually decreasing the GLIA
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