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A second feature of the Ras type GTPases is
2022-03-07

A second feature of the Ras-type GTPases is that their ‘on’ and ‘off’ states are temporally and often spatially separated from one another. This feature is essential for GTPases mediating signaling and other processes that need to be kept ‘off’ until the arrival of signaling cues. The need to recrui
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While published data around the functional significance of G
2022-03-07

While published data around the functional significance of GPR84 are quite sparse, details of signaling pathways initiated by the receptor are even more limited, including in recombinant systems. In recombinant cells, GPR84 activation reportedly leads to Gi pathway activation, resulting in pertussis
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br Mutagenesis and Receptor Modeling Studies br Signal Trans
2022-03-07

Mutagenesis and Receptor-Modeling Studies Signal Transduction and Receptor Desensitization Therapeutic Potential of HCA Receptor Ligands Although all members of the HCA receptor family are potentially interesting drug targets, only HCA2 is currently exploited as such. Therefore, this sectio
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INTRODUCTION Scar formation and tissue regeneration are
2022-03-07

INTRODUCTION Scar formation and tissue regeneration are opposite results of the wound healing process. Although fibrosis is more common after skin injury, full skin regeneration results in complete replacement of adnexa and function. Examples of tissue regeneration in mammalian systems include annu
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Compounds and were synthesized according to The synthesis of
2022-03-07

Compounds –, , and were synthesized according to . The synthesis of compounds – commences with C-acylation of 3,4-dibromothiophene to the form ketone , the ring closure to form the ester , Hiyama cross-coupling or Suzki cross-coupling to produce , or to , respectively. Compound was produced from ket
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br Next we explored the SAR around the aryl
2022-03-07

Next, we explored the SAR around the aryl ring attached to the pyrrole nitrogen in the presence of the 3-CF and the 2,6-difluorophenylpropionic (±)-Bay K 8644 sidechain (). The EC value of the unsubstituted phenyl was about 100 nM. The 4-methyl was 2-fold more potent, however ethyl and bromo
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One difficulty in studying gp is
2022-03-07

One difficulty in studying gp120 is that it binds to more than one receptor. Understanding how Ezatiostat respond to gp120 is complex because of this promiscuity. In an attempt to establish the contribution of CXCR4 in the antagonistic effect of gp120 on morphine-induced antinociception, AMD3100 wa
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It is important to clarify whether
2022-03-04

It is important to clarify whether the decrease in USV after administration was secondary to the central depressant actions of the test compounds. Several reports have addressed the possibility that central depressant actions such as motor incoordination or changes in body temperature might affect U
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br The glycine transporter GlyT was originally identified as
2022-03-04

The glycine transporter 1 (GlyT1) was originally identified as a member of the solute carrier family 6 of sodium- and chloride-dependent neurotransmitter transporters . GlyT1 is expressed in the central nervous system and in peripheral tissues; mainly in erythroid cells, from erythroblasts in the
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Evaluation of Provider Prompts Elimination of the Q R bridge
2022-03-04

Elimination of the Q234–R244 bridge significantly affected the protein Evaluation of Provider Prompts but had little effect on its activity at a permissive temperature, which may seem contrary to the known functional importance of this motif in Fpg. However, since the mutants fully or partially ret
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Tail group SAR of the imidazole derived
2022-03-04

Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methyl
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AST 487 The HH signaling has also been implicated
2022-03-04

The HH signaling has also been implicated in the regulation of cancer stem AST 487 (CSC) by promoting their self-renewal [53]. Activated HH signaling has been identified in CSCs of many solid tumors, such as glioblastoma, breast, colon, pancreatic cancer, melanoma, and hematological malignancies, in
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In the small intestine digestion and absorption of the nutri
2022-03-04

In the small intestine, digestion and KPT-185 of the nutrients are the next processes with an impact on the resulting plasma profile. Normally, neither carbohydrate digestion nor absorption are limiting factors, which is illustrated by the rapid and extensive absorption of glucose in conditions wit
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A single ICV injection of GALP stimulated food intake in
2022-03-04

A single ICV injection of GALP stimulated food intake in goldfish at 1h post-administration. This result is similar to that observed in rats, where ICV injection of GALP exerted an acute orexigenic effect [14], [15], [16]. Simultaneously, our findings counter the results found in mice, where central
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Interestingly transgenic mice that constitutively express ac
2022-03-04

Interestingly, transgenic mice that constitutively express active FXR in the intestine (iVP16FXR) are protected from chemically-induced and genetically-induced cholestasis. This protective effect is attributed to the induction of intestinal FGF15 and repression of hepatic Cyp7a1 expression, downregu
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