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br Development of lorlatinib from crizotinib
2023-10-19

Development of lorlatinib from crizotinib (1) to a clinical candidate (6) Xalkori (1, PF-02341066, crizotinib), was the first-in-class ALK inhibitor approved by the Unites States Food and Drug Administration (FDA) in 2011 as a first-line treatment for ALK+- NSCLC patients. This section describes
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Extracellular adenosine acts as a
2023-10-19

Extracellular adenosine acts as a local modulator of cell function via four adenosine receptor subtypes (A1Rs A2AR, A2BR, and A3R) that are involved in numerous physiological and pathophysiological processes [31]. Each is encoded by a separate gene and has different functions, although with some ove
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glutamate receptor Curcumin is the principal natural polyphe
2023-10-19

Curcumin is the principal natural polyphenol curcuminoid of turmeric (Curcuma longa) rhizome, a member of the ginger family (Zingiberaceae) [13]. Curcumin has a wide spectrum of therapeutic properties, and it has been shown to possess antioxidant, anti-inflammatory, anticancer, antiangiogenesis, che
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Nexturastat A synthesis The difference in the mean values
2023-10-19

The difference in the mean values of serum ADA in sputum positive PTB and controls was found to be highly significant (P Discussion Tuberculosis is a major health problem in India, and out of all its forms PTB is the commonest. A definite diagnosis of PTB can be made with the presence of Nexturast
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An alternative to the agonist or antagonist potential in dru
2023-10-19

An alternative to the agonist or antagonist potential in drug discovery is the positive allosteric modulator (PAM) approach, which can augment the normal processes of neurotransmission as opposed to directly replacing or antagonizing them. PAMs are thought to bind to sites that are distinct from the
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br Concluding Remarks and Future Directions The physiologica
2023-10-19

Concluding Remarks and Future Directions The physiological significance of autophagy in neuronal function is steadily emerging. The studies discussed herein reveal that key neuronal functions, such as neurotransmitter release, pruning of dendritic spines, and behavioural outputs of neural network
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The overall mechanism of the Cdc complex resembles
2023-10-19

The overall mechanism of the Cdc48 complex resembles that of the 19S regulatory subunit of the proteasome, which also uses receptor proteins to bind polyubiquitin chains attached to a substrate and employs a translocation mechanism (for review, see Kish-Trier and Hill, 2013). As with Cdc48, full sub
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Protein protein interaction networks are an important ingred
2023-10-19

Protein–protein interaction networks are an important ingredient for the system-level understanding of cellular processes. Such networks can be used for filtering and assessing functional genomics data and for providing an instinctive platform for annotating structural, functional and evolutionary p
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Since obesity appears to impact
2023-10-19

Since obesity appears to impact leptin and adiponectin levels in opposite manners, several studies have suggested that the serum adiponectin/leptin ratio may be a key parameter in indicating the relative risk of postmenopausal breast cancer (Ollberding et al, 2013, Cleary et al, 2009). Therapeutic
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Here the so called alkali
2023-10-19

Here the so-called alkali assay [18] is proposed as a method to be applied directly on the purified recombinant enzyme sharing the same structural and functional features of the wild-type enzyme [19], [20], [21] using its physiological substrate androstenedione. The assay that was already successful
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To elucidate whether membrane fluidity changes could impact
2023-10-19

To elucidate whether membrane fluidity changes could impact on signaling pathways, we examined the effects of Rh2 on the activation of Akt, a lipid raft-associated protein kinase, which promotes cell survival and blocks the apoptotic pathways. Upon pretreatment with 5 mM MβCD and in the absence of R
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As with most G protein coupled receptors GPCRs
2023-10-19

As with most G protein-coupled receptors (GPCRs), sustained activation of APJ can cause desensitization and this has been reported to occur for APJ-mediated effects on cytoplasmic Ca2+ concentration, as well as for effects on activity of adenylyl cyclase, ERK and Akt (Ishida et al., 2004, Masri et a
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Optical coherence tomography angiography is
2023-10-18

Optical coherence tomography angiography is another promising method for the assessment of corneal neovascularization. This relatively new modality is not yet widely used in part because of current limitations in the definition of images produced, lack of functional information, and inability to det
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Oxaliplatin How do increased levels of ammonia as observed
2023-10-18

How do increased levels of ammonia as observed in clinical HE constrain synaptic plasticity? Numerous studies have investigated the modulation of signal transduction pathways activated in LTP or LTD irrespective of being necessary or sufficient for changes in synaptic efficacy (Wen et al., 2013). Ye
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The functional significance of the cap residues with
2023-10-18

The functional significance of the cap residues with regard to the established role of PfA-M1 in hemoglobin catabolism in the food vacuole is a key question that is difficult to address with in vitro studies. We note that three of the dipeptide substrates used in our study are found in the sequences
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