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The enzyme mediated ATP sensing mechanism in zebrafish can b
2024-04-02

The enzyme-mediated ATP-sensing mechanism in zebrafish can be compared with previous studies in other animal species reporting that enzymatic conversion of chemicals in the peripheral olfactory organ results in either “activation” or “inactivation” of odorants and pheromones. In male silkmoth, the a
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AdipoRon is an orally active synthetic small molecule that
2024-04-02

AdipoRon is an orally active, synthetic small molecule that activates adiponectin receptor (AdipoR). It mimics the antidiabetic effects of adiponectin, exhibiting its effect through the activation of AMPK and PPARα pathways via AdipoR1 and AdipoR2, respectively (Fig. 2) [62]. AdipoR activation has r
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We have previously reported that
2024-04-02

We have previously reported that interfering with 2-Cl-IB-MECA assembly dynamics by knocking down cofilin-1 in hMSCs increased polymerized actin that promoted osteoblast cell differentiation through a mechanism of enhancing focal adhesion kinase (FAK), p38 and c-Jun N-terminal kinase (JNK) signaling
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imipramine hcl In the olfactory bulb expression was especial
2024-04-02

In the olfactory bulb, expression was especially prominent in the mitral cell layer from embryonic stages to adult tissues (Figs. 1D–G). By E14–E16, Ack1 signal was remarkably intense in the proliferative ventricular zone (Fig. 1D). From E18 to adult, expression was also observed in glomerular and g
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A high throughput small molecule
2024-04-02

A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found 2-APB to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work was perfor
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Several reports of single cases of MG patients treated
2024-04-02

Several reports of single cases of MG patients treated with Rituximab have claimed a favourable response (Baek et al., 2007, Gajra et al., 2004, Hain et al., 2006, Thakre et al., 2007, Wylam et al., 2003, Zaja et al., 2000). We report our experience with Rituximab in 6 patients with severe MG, 3 pa
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The zebrafish Danio rerio is a
2024-04-02

The zebrafish (Danio rerio) is a popular model organism for virtually any biological function of vertebrates, and has, therefore, received a wide distribution in particular in developmental biology and toxicology (Strähle et al., 2012). With respect to AChE, the zebrafish has, e.g., been identified
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The discovery of acetylsalicylic acid aspirin in paved the
2024-04-02

The discovery of acetylsalicylic leptomycin b (aspirin) in 1897 paved the way for the development of classical NSAIDs as first-line therapeutics for anti-inflammatory, anti-pyretic and analgesic therapy. Large efforts have been made in the following decades to improve the efficacy and in particular
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br Research perspective In vitro and
2024-04-02

Research perspective In vitro and in vivo studies have demonstrated that increased LPA/ATX signaling contributes to cancer initiation and progression. Recent findings on the role of non-tumoral ATX in cancer progression and metastasis highlighted a new functional contribution for the microenviron
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br Conflict of interest br Acknowledgements We thank Ann
2024-04-02

Conflict of interest Acknowledgements We thank Ann Jackman, Mike Ormerod and members of Julian Downward's and Alan Ashworth's groups for helpful discussions. This work was supported by grant number PEM/GME/D391/40 from the Kidani Trust (S. Kaye) and by Keele University. Introduction Autota
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Having taken a step back from affinity to gain
2024-04-02

Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci
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apoptosis br Introduction The process of mitosis is highly c
2024-04-02

Introduction The process of mitosis is highly complex and tightly regulated. This phase of the apoptosis resulted in two identical daughter cells. The aurora kinases (aurora A, B, and C) are a family of three highly homologous serine-threonine protein kinases that play a key role in regulating t
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Illustrated in is the protocol we
2024-04-02

Illustrated in is the protocol we applied for the screens of novel furoic acids as ACL inhibitors. We constructed our furan carboxylate library that contained 1446 2-furoic biotin-LC-LC-tyramide receptor derivatives and 501 3-furoic acid derivatives by performing substructural searches of the ZINC d
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ATM is generally regarded to be the principal
2024-04-02

ATM is generally regarded to be the principal mediator of the G1 Donitriptan hydrochloride receptor checkpoint, whereas the induction of the intra-S-phase and G2/M checkpoints are usually primarily related to ATR function. However, several studies have demonstrated that, depending on the cellular c
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Previous investigations have established that aromatase acti
2024-04-02

Previous investigations have established that aromatase activity is regulated via two different pathways in a tissue-specific manner. The first is a slower transcription regulatory pathway that involves an alteration in gene transcription and represents what is classically thought of as the way by w
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