• A second advance came with

  2020-12-12

  

  A second advance came with the discovery that conformationally-flexible benzamide analogs having an N-phenylpiperazine moiety possessed good affinity and modest selectivity for D3 versus D2 receptors [3,[14], [15], [16]]. This observation spawned a significant effort by medicinal chemists to develop

• cGAS has a central role in STING

  2020-12-12

  

  cGAS has a central role in STING activation after DNA sensing, but it is unknown if most of the DNA sensors act independently or in cooperation with the cGAS-cGAMP pathway. This was addressed for IFI16 (Almine et al., 2017, Jønsson et al., 2017) and PQBP1 (Yoh et al., 2015) but remains to be tested

• Thymine glycol severely inhibits DNA

  2020-12-12

  

  Thymine glycol severely inhibits DNA synthesis by replicative DNA polymerases and requires the action of specialized DNA polymerases for translesion synthesis (e.g. Ref. [26]). Eukaryotic and archaeal RNAPs were shown to pause after nucleotide insertion opposite TG [27,28]. Surprisingly, we found th

• During these processes meiotic recombination plays a critica

  2020-12-12

  

  During these processes, meiotic recombination plays a critical role by physically associating homologs and ensures accurate chromosome segregation. In addition, meiotic recombination redistributes genetic material between homologs, resulting in haplotype diversity among progeny, impacting ecological

• br Experimental methods br Results and discussion br Conclus

  2020-12-12

  

  Experimental methods Results and discussion Conclusion Rational design of highly selective fluorescent probes to detect G-quadruplexes is of profound importance for basic research. On this basis, we designed and synthesized a series of N-alkylated styrylquinolinium dyes Ls-1, Ls-2 and Ls-3.

• br Hypothesis on DDR protective mode of action The

  2020-12-12

  

  Hypothesis on DDR1 protective mode of action The documented protective role of DDR1 is quite impressive, demonstrated using different preclinical models (immunologic [46,54,58], obstructive [45], and hypertensive [50]) with different intervention paradigms: genetic ablation [45,50,58,72], silenci

• Ligand independent constitutively active variants have

  2020-12-12

  

  Ligand-independent, constitutively active variants have also been found in receptors with associated tyrosine kinases. In approximately 60% of patients harboring inflammatory hepatocellular adenomas (IHCAs), these adenomas have been caused by small in-frame deletions in the cytokine-binding domain o

• Taking into account that Gr

  2020-12-11

  

  Taking into account that Gr dysfunction is involved in the molecular mechanisms underlying HPA axis disorder (Li et al., 2017b) and Gr activity has been reported to be lowered in patients with severe mood disorders (Rush et al. 1996) and in adult rats (Green et al. 2016), PFOS could alter HPA axis a

• Rambabu et al reported A series

  2020-12-11

  

  Rambabu et al. reported A series of novel N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide derivatives synthesized from readily available 4-hydroxy coumarin to the corresponding ethyl 2-(2-oxo-2H-chromen-4-yloxy)propanoate followed by hydrolysis and further reacted with different substituted am

• RQ What are the different factors that influence the decisio

  2020-12-11

  

  RQ2: What are the different factors that influence the decision to choose among different component origins? In total eleven factors grouped into three high-level themes that influence the decision to choose a component origin were identified. The project metrics factors are: time, cost, effort and

• In most cases the ligand affinity between subtypes is simila

  2020-12-11

  

  In most cases, the ligand affinity between subtypes is similar, but their tissue distribution is different. In the case of the estrogen receptors (ER), two subtypes (ERα and ERβ) exist (Kuiper et al., 1996) and ERβ has several isoforms, designated ERβ1–5 (Moore et al., 1998) or ERβcx (Ogawa et al.,

• Prostanoids typically act in an autocrine and

  2020-12-11

  

  Prostanoids typically act in an autocrine and paracrine fashion by binding to specific receptors in target BCTC and there is evidence that both PGE2 and prostacyclin may be required for the optimal activation of angiogenesis (Hata and Breyer, 2004). PGE2 and prostacyclin bind to their specific 7-mem

• Next we elucidated that the Mtb enolase binds to host

  2020-12-11

  

  Next, we elucidated that the Mtb enolase binds to host plasminogen with a high affinity. The KD value of 360nM for this interaction suggested an avid binding between the two proteins in vivo. This observation is also in conciliation with the observed KD values for enolase-plasminogen interactions in

• Upon Edn ligand binding endothelin receptors can

  2020-12-11

  

  Upon Edn ligand binding, endothelin receptors can induce a variety of intracellular signaling cascades leading to diverse cellular responses such as contraction in the case of smooth muscle cells, or cell growth and mitogenesis. Ednrs are expressed in a variety of cell types and tissues, for example

• br Conflict of interest br Introduction

  2020-12-11

  

  Conflict of interest Introduction Endothelin receptors are members of the superfamily of G-protein-coupled receptors (GPCRs) and central regulators of vascular tension and other physiological functions in higher eukaryotes [1]. The human endothelin system comprises the highly homologous endoth

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