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Enlarging the ligand binding pocket by reduction
2019-12-09
Enlarging the ligand-binding pocket by reduction of the size of the residue F435 switched DES to an agonist indicating that F435 is involved in mediating the antagonistic effect of DES (Fig. 7E) [13]. The conformation of the smaller side chain of L435 was either not altered by DES or was too small t
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EP is the major receptor to
2019-12-09
EP4 is the major receptor to mediate PGE2-induced inflammatory pain. EP4 is upregulated by liver x receptor in DRG neurons [16]. Intrathecal injection of the EP4 agonist produced pain responses [25]. Either systemic or local injection of EP4 antagonists relieves inflammatory pain [3], [16], [26]. H
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In this study we have explored a functional role
2019-12-09
In this study we have explored a functional role of the oxysterol/EBI2 system in this process. In 2011 we and others reported the discovery of oxysterols as ligands for EBI2 [6], [7]. Oxysterols are metabolites generated by hydroxylation of cholesterol and have been linked to a variety of fundamenta
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br Materials and methods br Results br Discussion
2019-12-09
Materials and methods Results Discussion Plant U-box E3 Ub ligases regulate diverse plant-specific cellular processes [1], [2], [3], [4]. However, structural and functional relationships between U-box E3s and their E2 partners are largely unknown in higher plants [24], [25]. In this study,
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Addressing whether impaired activation of D and D
2019-12-09
Addressing whether impaired activation of D1 and D2 receptors regulates memory capacity is relevant for all human pathologies that lead to reduced activation of these Irsogladine pathways, such as ageing [39], certain genetic polymorphisms [40] and neurodegenerative disorders. In this study, we hav
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br Conclusion The present work describes the synthesis of
2019-12-09
Conclusion The present work describes the synthesis of 18 naphthoquinonolyl-1,2,3-triazole compounds based on natural product modification with antiplasmodial activity. Lapachol derivatives disclosed higher activity than the natural product. Six of these final modified lapachol 1,2,3-triazole com
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br Multi hierarchical structure of collagen Protein structur
2019-12-06
Multi-hierarchical structure of collagen Protein structure is the foundation of protein functions and properties. It is generally accepted that the protein has biological function only when it has tertiary structure or above. Among the identified 28 types of collagen, most is known about type I c
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CK comprises a family of serine
2019-12-06
CK1 comprises a family of serine/threonine protein kinases, that includes different CK1 isoforms namely α, β, δ, ε and γ their various splice variants [56]. It was reported that the pharmacological inhibitor IC261 shows an order of magnitude of higher selectivity for CK1δ or CK1ε isoforms (IC50 of 1
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By using live imaging of an ERK fluorescence resonance
2019-12-06
By using live imaging of an ERK fluorescence resonance energy transfer (FRET) sensor, the authors show that ERK activity propagates in a stepwise manner from the center to the periphery of the tracheal placode. This row-by-row propagation of ERK activity fits a relay model in which each row activate
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Little information is available regarding the expression of
2019-12-06
Little information is available regarding the expression of the different EP receptor subtypes on human monocytic cells, particularly those that are involved in downregulating cytokine production. The receptors are controlled by the respective genes for each receptor i.e. PTGER1–PTGER4 for EP1–EP4 r
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The biological actions of ET are mediated
2019-12-06
The biological actions of ET‐1 are mediated via two distinct receptor subtypes, the endothelin A and endothelin B receptors (ETA/ETB). While activation of ETA is assumed to mediate contraction of smooth muscle cells, the activity of ETB is related to transient vasodilation [22]. In human corpus cave
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Her eldest daughter individual had a
2019-12-06
Her eldest daughter (individual 4) had a normal birth and health history in early childhood. She developed contractures of her fourth fingers at 4–5 years of age; these contractures were associated with painless, non-erythematous swelling of the involved joints. Her PIP contractures were ∼90 degrees
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br Results br Discussion Mucosal barriers are constitutively
2019-12-06
Results Discussion Mucosal barriers are constitutively challenged by various stimuli, and the homeostasis of mucosal barriers both at steady state and upon challenge are maintained by tissue-resident immune ganciclovir (Kurashima et al., 2013, Okumura and Takeda, 2016). ILC3s are found in lym
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br E E backside interaction The
2019-12-06
E3–E2 backside interaction The E2 possesses an important regulatory interface which is termed its backside as it is opposite to the catalytic cleft that bears the active-site cysteine forming the thioester with SUMOD. This backside site interacts noncovalently with a scaffold SUMOB and was origin
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While apparent that His Artemis fractionated over a HAP colu
2019-12-06
While apparent that [His]6-Artemis fractionated over a HAP column is devoid of 5′–3′ exonuclease activity but still retains DNA-PK dependent hairpin-opening activity, we sought to further assess DNA-PK dependent Artemis overhang cleavage activity to ensure all the in vivo, intrinsic enzymatic activi
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