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TIC10 Matrix metalloprotease inhibitors are increasingly ava
2024-11-22

Matrix metalloprotease inhibitors are increasingly available and tested for other indications in clinical trials. The present study suggests that either ADAM10 or TACE inhibition alone will not maximally restore leukocyte Axl function. We found that lower doses of ADAM10/TACE inhibitors exhibit simi
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Autotaxin has been linked to chemoresistance through its
2024-11-22

Autotaxin has been linked to chemoresistance through its ability to inhibit apoptosis induced by paclitaxel in breast cancer CGK733 [15] and LPA can inhibit cell death induced by cisplatin [40]. Autotaxin was included in the present study because it was identified as being over-expressed in patient
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In this paper we describe the formation of a structure
2024-11-22

In this paper, we describe the formation of a structure-based pharmacophore which lead to the discovery of several hydrophobic, yet non-lipid inhibitors of ATX. These compounds docked within the same volume occupied by the initial non-lipid inhibitors of ATX used to build the pharmacophore. Violati
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Investigating these possibilities will illuminate whether ce
2024-11-22

Investigating these possibilities will illuminate whether cytidine triphosphate possess mechanisms to differentially detect ACLY-generated versus ACSS2-generated acetyl-CoA as well as define the functional relationship between histone acetylation levels and cellular functions and phenotypes. Given t
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br Discussion Arginase and Arginase are homologous enzymes t
2024-11-22

Discussion Arginase 1 and Arginase 2 are homologous enzymes that consume l-arginine to produce l-ornithine and urea [14], [15]. These enzymes compete with NO synthases for the same substrate [14], [15], [30], and therefore may reduce NO production [21], [24], [30]. The colocalization of arginases
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br Acknowledgements This work was supported by
2024-11-21

Acknowledgements This work was supported by National Natural Science Foundation of China (Nos. 21376172, 21528601 and 21621004) and the Natural Science Foundation of Tianjin from Tianjin Municipal Science and Technology Commission (Contract No. 16JCZDJC32300). Introduction Alzheimer’s disease
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The amino acids evaluated in this study represent
2024-11-21

The amino acids evaluated in this study represent proteinogenic (amino acids that are applied in the genetic code) or even essential ones (amino acids that cannot be synthesised by the organism and need to be taken up by nutrition). Tryptophan, phenylalanine, tyrosine, isoleucine, threonine and vali
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Tissue distribution showed that ctrp was abundantly
2024-11-21

Tissue distribution showed that ctrp9 was abundantly expressed in the kidney of male and female tilapia. In mice, the Ctrp9 was identified in adipose tissue, and the expression levels were higher in females than that of males (Wong et al., 2009). Recent studies indicated that Ctrp9 was also expresse
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Regarding the HT B receptors they act as terminal receptors
2024-11-21

Regarding the 5-HT1B receptors, they act as terminal receptors and are involved in the presynaptic regulation of the release of 5-HT. But at spinal level these receptors are principally situated post-synaptically (Sari, 2004). The ability of autoreceptors to regulate extracellular levels of 5-HT du
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Introduction Pyometra is relatively common
2024-11-21

Introduction Pyometra is relatively common in intact bitches and its diagnosis is aided by ultrasonography (Bigliardi et al., 2004), along with measurement of acute phase proteins and leucocyte (white blood cell, WBC) counts; assessment of these parameters during recovery may be helpful for monitor
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All consecutive patients who were
2024-11-21

All consecutive patients who were confirmatively diagnosed with MP-PPE and TPE, respectively, between January 2008 and December 2016 at Kyungpook National University Hospital, a tertiary referral hospital in South Korea, an area with an intermediate prevalence of active tuberculosis, were enrolled.
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br Results br Discussion The
2024-11-21

Results Discussion The 5-Methoxy-CTP cytoskeleton is a highly attractive target for many bacterial toxins, owing to its role in activation and locomotion of immune cells, secretion of humoral response factors, and maintenance of protective barriers at the cellular (sub-membrane cytoskeleton)
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Having established the structural requirements for
2024-11-20

Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vitr
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The combination of Aurora kinase
2024-11-20

The combination of Aurora kinase inhibitors with standard chemotherapeutics or radiotherapeutics are currently in progress, such as AZD1152 plus radiotherapy in various solid cancer models. In addition, Azzariti et al. found that AZD1152-HQPA enhanced oxaliplatin and gemcitabine effectiveness in the
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br Aurora A Aurora B and
2024-11-20

Aurora-A, Aurora-B and Aurora-C small molecule inhibitors Nicholas et al. described phenotypic cellular screening of new highly potent and selective class of Aurora kinase inhibitors. Fragment based approach was utilized; core structure of 57 (Fig. 5) was optimized and selective inhibitor 58 (Fig
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