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Hydantoin in region F bridging the phenoxybenzene and benzim
2022-03-22

Hydantoin in region F bridging the phenoxybenzene and benzimidazole moieties was replaced by cyclic building blocks, diketopiperazine (25) and imidazolidinone (26), and linear bonds, amide (27) and urea (28). Analogs 25–28 possessing the linkers other than hydantoin were not tolerated in LBD of FXR,
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In order to understand the determinants
2022-03-22

In order to understand the determinants of high affinity of with amide side chain, an X-ray crystal structure of human liver FBPase in complex with was determined (). The position of phosphonate group and tricyclic scaffold of is similar to those of with no side chain, which suggests the formati
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br Expression and Purification of LSD
2022-03-22

Expression and Purification of LSD1 Proteins In Vitro Enzymatic Assays Analysis of LSD1 Demethylase Activity Acknowledgments Conflict of Interest Statement: Y.S. is a cofounder of Constellation Pharmaceuticals, Inc. and is a member of its scientific advisory board. Y.S. is also a consu
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T0070907 receptor While the dogma of the mainstream
2022-03-22

While the dogma of the mainstream considers Hippo pathway as a series of size-controlling kinases, there were still some controversial data supporting that YAP, a vital oncoprotein of Hippo downstream, is antagonistic to regenerative proliferation [[20], [21], [22]]. Known for its expansion-driving
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br Tissue Specific Roles for HIF PHD Isoforms Hypoxia signal
2022-03-22

Tissue-Specific Roles for HIF/PHD Isoforms Hypoxia signaling pathways are active in almost all mammalian cells, including immune Isotretinoin and tissues such as the epithelium and endothelium. This is of crucial importance when considering the influence of environmental hypoxia in inflammatory c
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In the Hedgehog signaling pathway cholesterol is
2022-03-21

In the Hedgehog signaling pathway, cholesterol is required to activate SMO (Cooper et al., 2003), the downstream target of PTCH1. A previous study (Bidet et al., 2011) reported that Patched expression in yeast 4 mu increased extrusion of a fluorescent boron dipyromethanene sterol derivative (BODIPY-
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Eastern Guangdong is a Teochew dialect area We found
2022-03-21

Eastern Guangdong is a Teochew dialect area. We found that subtype 1b (3.1%) in this region was significantly lower than in other areas. Subtype 1b began its spread from the central part of China out into the whole country through illegal blood donation in the mid-1990s (Lu et al., 2013) and is now
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Spindle positioning is governed by
2022-03-21

Spindle positioning is governed by the actin cytoskeleton. After a transient metaphase arrest, cells lacking haspin exhibit a misdistribution of actin, which accumulates within the bud. Actin dynamics is modulated by an intricate network including septins, the polarisome complex, and formins. We sho
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Despite the similarities there are some differences
2022-03-21

Despite the similarities, there are some differences between the augmentation by hypoxia and that by thymoquinone. While in porcine coronary arteries they both depend on calcium sensitization mediated by ROCK12, 32, 33, L-type calcium channels are involved only in thymoquinone-induced augmentation.
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br Introduction Human immunodeficiency virus HIV is a retrov
2022-03-21

Introduction Human immunodeficiency virus-1 (HIV-1) is a retrovirus that primarily infects components of the human immune system, such as CD4+ T cells, macrophages and dendritic ddhUTP of (Clapham and McKnight, 2001). HIV directly and indirectly destroys CD4+ T cells, which leads to severe immun
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The first described synthetic FFA active
2022-03-21

The first described synthetic FFA1 active agonist, GW9508 (4- [(3-phenoxyphenyl)methyl]amino benzenepropanoic acid), was immediately shown to also activate FFA4, although with some 100-fold lower potency [38]. Therefore, in the initial absence of FFA4-selective synthetic agonist ligands, GW9508 was
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br Materials and methods br Results br Discussion To fulfill
2022-03-21

Materials and methods Results Discussion To fulfill its role in tissue homeostasis, repair and immunoregulation, MSCs must be able to (i) renew themselves by cell division and proliferation, (ii) migrate to its target end-site in response to chemotaxis signals and (iii) undergo appropriate
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br Material and methods br Results br Discussion Neurosteroi
2022-03-21

Material and methods Results Discussion Neurosteroids capable of blocking the NMDAR channel attract a lot of attention as possible therapeutic agents for the treatment of neurodegenerative diseases. A large number of new Halopemide with different structures have been synthesized in order to
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br Materials and methods br
2022-03-21

Materials and methods Results Discussion l-glutamate is the major excitatory neurotransmitter in the brain, and is functionally involved in many processes of the nervous system which have been connected with several neurological diseases [4]. These conditions are characterized by the time-d
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Since the late s synthetic
2022-03-21

Since the late 1940s, synthetic GC (e.g. prednisone, prednisolone, dexamethasone) have been used extensively in the treatment of chronic inflammatory conditions such as rheumatoid arthritis and asthma, and for their immunosuppressant action in preventing organ rejection post transplantation. Cortico
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