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Constitutive tyrosine kinase activity of BCR ABL fusion gene
2023-11-23
Constitutive tyrosine kinase activity of BCR/ABL fusion genes causes uncontrolled cell growth and is also thought to be responsible for a variety of changes in normal cellular functions like differentiation, adhesion, migration and apoptotic response in CML. Therefore it is important to know the exp
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As an alternative to chronic receptor
2023-11-22
As an alternative to chronic receptor blockade, we have been targeting adenosine kinase (ADK) – an astrocyte-based enzyme that catalyses the phosphorylation of adenosine, as a means to modify 1,4-DPCA receptor adenosinergic signalling (Boison, 2006, Etherington et al., 2009). Up-regulating ADK faci
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Sperm total motility and hyperactivated motility are
2023-11-22
Sperm total motility and hyperactivated motility are mediated by PLD-dependent IMR-1 mg polymerization [20]. Reduction of PIP2 synthesis inhibited actin polymerization and motility, and increasing PIP2 synthesis enhanced these activities. Furthermore, sperm demonstrating low motility contained low
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Using constant potential amperometry and electrochemical enz
2023-11-22
Using constant potential amperometry and electrochemical enzyme-based biosensors selective for choline—and, therefore, an accurate readout of MS023 release (Baker et al., 2015; Bruno et al., 2006a; Parikh et al., 2004, 2007)—tonic and phasic release of acetylcholine were measured simultaneously in
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Molecular docking simulations were carried out for
2023-11-22
Molecular docking simulations were carried out for ligands – in the ACE crystal structure (1O86) and DPP4 crystal structure (2G5P). Comparison of the binding mode of – () with enalaprilat (a) in ACE shows that the phenethyl group (–, enalaprilat) occupies the S1 pocket and the adjacent carboxylic si
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In humans the major LOs are subdivided by their positional
2023-11-22
In humans, the major LOs are subdivided by their positional specificity into 5-(ALOX5), 12-(ALOX12) and 15-LO (ALOX15) (Kuhn et al., 2015). 5-LO is the key enzyme for LT biosynthesis and mainly found in mature cells from myeloid origin, including neutrophil, eosinophil and basophil granulocytes, mon
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Celecoxib The srd a isoforms showed unique expression
2023-11-22
The srd5a isoforms showed unique expression profiles in early FHM development (Fig. 2). Similar to amphibian embryos, there was a high abundance of both srd5a1 and srd5a3 at 1dpf in FHMs, suggesting that mRNA for these enzymes may be maternally deposited and that these enzymes may play a key role in
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Skeletal pain associated with bone fracture is another area
2023-11-22
Skeletal pain associated with bone fracture is another area of critical need for a novel pain medication. NSAIDs and opiates are the two major therapies currently used to manage bone fracture pain. However, both of these therapies lead to significant unwanted side effects. Using the osteotomy model
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cytochalasin d PF also a dual Aurora A and
2023-11-22
PF-03814735, also a dual Aurora-A and Aurora-B inhibitor, was administered in a phase I dose escalation study in a 3-weekly cytochalasin d for 5 or 10 consecutive days [69], [70]. To date 25 patients have been included in 7 dose levels (5–100mg/day for 5 days). Using the 5-day schedule the MTD was
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sphingosine br Conflicts of interest br Introduction Phospha
2023-11-22
Conflicts of interest Introduction Phosphatidic sphingosine phosphatase (PAP) enzymes are responsible for catalyzing the reaction that dephosphorylates phosphatidic acid (PA), which in turn produces diacylglycerol (DAG) and a phosphate group during phospholipid regulation (Fig. 1A) [1]. Subse
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Significant reductions in GYN cancer patient mortality and m
2023-11-22
Significant reductions in GYN cancer patient mortality and morbidity rates require treatments that proactively prevent and reverse resistance to chemotherapy and radiation. Combining chemotherapy and radiation with inhibitors of key DDR proteins targets is likely to enhance the ability of genotoxic
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ATM dependent initiation of radiation induced G
2023-11-22
ATM-dependent initiation of radiation-induced G2/M checkpoint arrest is well established [11], [34], [35]. However, the ATR pathway may also be involved [36], [37]. Brown and Baltimore generated Cre/lox-conditional cell lines or ampicillin sodium with a kinase inactive allele of ATR (ATRkd) to eval
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Introduction Apoptosis signal regulating kinase ASK a family
2023-11-22
Introduction Apoptosis signal-regulating kinase 1 (ASK1), a family member of the mitogen-activated protein (MAP) kinase kinase kinase (MAP3K) family, selectively activates the JNK and p38 MAP kinase pathways in response to various types of stresses, including oxidative stress, and subsequently indu
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Phosphatase Inhibitor Cocktail 3 (100X in DMSO) Citral or di
2023-11-22
Citral or 3,7-dimethyl-2,6-octadien-1-al is a mixture of two stereoisomeric monoterpene aldehydes (the trans isomer geranial, citral A (40–62%)) and the cis isomer neral, citral B (25–38%) and serves one of the main constituent of essential oils of C. citratusis used in cosmetic, food, fungicides, p
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Phosphatase Inhibitor Cocktail (2 Tubes, 100X) Mitochondrial
2023-11-22
Mitochondrial dysfunction resulting from mtDNA abnormalities may trigger retrograde signaling pathways from the mitochondrion to the nucleus, which regulate the expression of genes involved in diverse cellular processes, including metabolism, stress responses, tumor progression, nutrient sensing, li
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