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Much is known about FPPS structure and
2022-04-01
Much is known about FPPS structure and function, with over 120 FPPS crystal structures being currently available. This wealth of information is largely the consequence of human FPPS serving as a drug target for the treatment and/or prevention of pathologies such as osteoporosis, hypercalcemia and Pa
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Although drug monitoring is not usually requested there are
2022-04-01
Although drug monitoring is not usually requested, there are some cases where measurement of DOACs in Cy3 NHS ester synthesis is useful, and of special help for managing patients at risk. These cases include the control of adherence to a therapeutic protocol, surveillance of drug accumulation risk
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Previous evidence suggests that PRC
2022-04-01
Previous evidence suggests that PRC2 is an important regulator of chromatin looping interactions in embryonic stem Panobinostat . The new study by Donaldson-Collier and colleagues provides the first evidence that similar processes may be at play in lymphoma. It is still largely unclear, however, bot
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Recently the spectrin cytoskeleton a deformable actin
2022-03-31
Recently, the spectrin cytoskeleton, a deformable actin-associated network, has been identified as a modulator of Yki function, potentially acting both apically and basally in different cell types [75•, 76•, 77•]. Several mechanisms have been proposed, including regulation via Crb/Ex tethering [], t
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Studies conducted in our laboratory thus far have shown that
2022-03-31
Studies conducted in our laboratory, thus far, have shown that HKDC1 is broadly expressed [28]. Using the first developed HKDC1 mouse model, we found that complete loss of HKDC1 function is embryonic lethal, similar to other HKs [29,30]. Further studies using HKDC1 heterozygous knockout mice showed
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Given the overexpression of HO in
2022-03-31
Given the overexpression of HO-1 in some tumors, such as CML, and its potential involvement in chemoresistance to classical chemotherapeutic agents, compounds 4 and 8f were tested in CML cell lines resistant to IM, a classical TK inhibitor used in CML. Compounds 4 and 8f, in combination with IM, sho
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Importantly recent in vivo results
2022-03-31
Importantly, recent in vivo results demonstrated that combining an HDACi and a IKK inhibitor significantly reduced ovarian tumor growth compared with either inhibitor alone [26]. The slowest tumor growth in the HDACi/IKK inhibition combination group was associated with the lowest CXCL8 tumor and pla
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The PAS and CC domains of sGC
2022-03-31
The PAS and CC domains of sGC have been studied less by comparison, though their function in sGC signal transduction is likely important. PAS domains are versatile as they can play varied roles in different proteins, such as quaternary structure organization, cofactor binding, and signal transductio
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AP and NF B activation is inhibited by curcumin diferuloylme
2022-03-31
AP-1 [16], [17] and NF-κB activation is inhibited by curcumin (diferuloylmethane) [18], [19], the yellow component of Curcuma longa that gives curry its colour and flavour. Curcumin has shown anti-inflammatory and antioxidant properties [20], [21], [22], [23], [24], [25], [26] due to the inhibition
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We show that pharmacological inactivation of GSTP over a sus
2022-03-31
We show that pharmacological inactivation of GSTP1 over a sustained period does not show any observable toxicity, and not only prevents breast tumor growth but even slows established breast tumor growth in mice. A highly potent GSTP1 inhibitor, ezatiostat (developed by Telik Inc.) has passed phase I
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The mechanism underlying the anorectic
2022-03-30
The mechanism underlying the anorectic effect of OXM is well established. It is centrally mediated via GLP-1 receptor activation, confirmed by both pharmacological blockade of the GLP-1 receptor, and using GLP-1 receptor knock-out mice [2], [11], [12]. However, the mechanism by which it increases en
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The OTR and GHSR are known to play
2022-03-30
The OTR and GHSR are known to play similar roles in centrally regulated behaviours, where the OTR is implicated in mood, sociability and appetite regulation (Morton et al., 2012; Myers et al., 2014; Sala et al., 2013; Lukas et al., 2011; Slattery and Neumann, 2010), with the GHSR primarily involved
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br Presenilins and Wnt catenin
2022-03-30
Presenilins and Wnt/β-catenin signalling Several groups have provided substantial data indicating that PS1 acts as a negative modulator of the transcriptional activity of the β-catenin/Tcf-4 complex (Fig. 4) [120], [121], [122]. β-Catenin is a multifunctional protein that was first described as a
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br Concluding remarks br Introduction
2022-03-30
Concluding remarks Introduction The hair ligand gated channels of vestibular organs detect linear and rotational head movements, providing sensory information that is essential for normal postural and visual reflexes. Most vestibular hair cells are produced during embryonic development, but t
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AM251 To investigate an involvement of
2022-03-30
To investigate an involvement of GPR120 and GPR40 in the enhancement of cell motile activity of MG-63 cells, highly migratory (MG63-R7) AM251 were established from MG-63 cells (Fig. 2A). The expression level of GPR120 gene was significantly higher in MG63-R7 cells than in MG-63 cells, while no chang
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