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In an effort to discover additional GPCRs
2020-08-10
In an effort to discover additional GPCRs directing the migratory events of responding B cells, we identified Epstein-Barr virus (EBV)-induced gene 2 (EBI2) as a promising candidate. The gene encoding EBI2 (Ebi2, also known as Gpr183) was originally identified together with Ebi1 (Ccr7) as the most h
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Estrogen treatment in postmenopausal women requires combinat
2020-08-08
Estrogen treatment in postmenopausal women requires combination with a progestogen in order to prevent endometrial stimulation. This is not necessary, however, with tibolone as progestogenic activity is associated with its Δ4-metabolite that is formed in the liver, as well as locally in the endometr
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The effect of transformation of the linker Y between
2020-08-08
The effect of transformation of the linker Y between the carboxylic LDN-212854 residue and the phenyl moiety of 2b was also investigated, and is illustrated in Table 5. Analogs 2b, 16, and 17, possessing conformationally restricted carboxylic acid residues, tended to show stronger antagonist activit
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A-803467 The conservation of numerous ET related genes was
2020-08-07
The conservation of numerous ET-related genes was also observed in several mammalian species examined, including human, pig, and rat. Further, four cardiotoxic peptides highly homologous to ETs, sarafotoxins (S6a-S6d), were isolated from the snake venom of Atractaspis engaddensis. ET-like immunoreac
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As it was recently found native synuclein interacts with
2020-08-07
As it was recently found [28], native α-synuclein interacts with anion-binding groove between O and R (or P and Q) subunits of GAPDH which comprises NAD+-binding pocket and active site (Fig. 2A). In all 10 simulations, α-synuclein bound to this region of GAPDH (Fig. 2D, E). The following GAPDH resid
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Herein we performed the design
2020-08-06
Herein, we performed the design, synthesis, and biological evaluation of three Levonorgestrel of triple inhibitors of VEGFR-2, Tie-2, and EphB4. Several biphenyl-aryl ureas incorporated with quinazolin-4(3H)-one displayed promising anti-angiogenic and anti-cancer potency. The representative compound
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As the compounds in had shown they were
2020-08-06
As the compounds in had shown they were amenable to alternative heterocyclic acids we next investigated this region of the molecule, namely the 1-position of the indole (). The thiazole could be replaced by the analogous oxazole (, FLIPR p 9.0±0.5) with minimal change in activity. The regioisomeri
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Compound was obtained through a multicomponent
2020-08-06
Compound 1 was obtained through a multicomponent reaction from the natural benzoquinone embelin (I) [34], 4-chlorobenzaldehyde (II) and malonotrile (III). Based on calculated values of the Fukui function (f−) as local density functional descriptor [32], the synthesis of this Doxofylline can be rati
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In this study we have identified and
2020-08-05
In this study, we have identified and characterized three sunflower ENO isoforms. We surveyed the expression of ENO genes and the subcellular localization of the corresponding protein products. Recombinant ENO proteins were expressed in Escherichia coli in order to determine their kinetic properties
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Proinflammatory cytokines induce ER stress in many mammalian
2020-08-05
Proinflammatory cytokines induce ER stress in many mammalian cell systems.32, 33, 34 Our results demonstrate that these cytokines also trigger ER stress in trophoblast JEG-3 cells. However, the severity of stress is likely low grade because only the PERK-EIF2A arm of the UPRER pathway was activated.
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In this issue Sidhu and colleagues develop inhibitors for
2020-08-05
In this issue, Sidhu and colleagues develop inhibitors for USP15, a member of the Ub-specific protease (USP) family of DUBs (Teyra et al., 2019). USP15 removes ubiquitin from a number of substrates, including transforming growth factor beta (TGF-β) receptor, as well as the E3 ligases MDM2, TRIM25, a
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Alosetron br The major regulator of radiation sensitivity
2020-08-05
The major regulator of radiation sensitivity Tumor cell resistance to radiation is a big issue for radiation therapy, and a major concern of radiation oncologist. Understanding the regulation mechanism of radiation sensitivity is still a research hotspot. Increased sensitivity to ionizing radiat
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br Role of Cdk in
2020-08-05
Role of Cdk5 in plaque formation In AD pathogenesis, the key component of amyloid plaques is the accumulation of amyloid-β peptide (Barucker et al., 2015, Mawuenyega et al., 2010). Aβ is formed due to the sequential cleaving of integral membrane glycoprotein APP by β-secretase (BACE1) succeeded b
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br Introduction br Materials and methods br Results br Discu
2020-08-05
Introduction Materials and methods Results Discussion In the present study, etifoxine attenuated the anxiogenic-like behavioral and autonomic responses to i.c.v. injection of CRF in the rodent. Thus, in the open field, rats receiving CRF responded with an increased sensitivity to the str
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A conserved binding site for estrogen related receptor ERR
2020-08-05
A conserved binding site for estrogen-related receptor γ (ERRγ) has been identified in the WZ3146 of the Vegfa gene [7], [8], [9]. ERRγ, like other members of the ERR subfamily, is a constitutively active orphan nuclear receptor. It is selectively expressed in metabolically active tissues such as s
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