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br Development of lorlatinib from crizotinib to
2023-02-01

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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Heat shock protein Hsp is a
2023-02-01

Heat shock protein 90 (Hsp90) is a molecular chaperone that plays a central role in regulating the maturation, activation and stability of numerous “client proteins” that drive the development and progression of many cancers. Therefore, inhibition of Hsp90 would result in degradation of the client p
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There has been growing interest over computational methods
2023-02-01

There has been growing interest over computational methods to predict the biological activity by chemical structure, so as to decide whether it Oligomycin A has objective qualities or not. In this contribution, the well-known method, which is called quantitative structure–activity relationship (QSA
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T7 Tag Peptide The next level of possible correlation and co
2023-02-01

The next level of possible correlation and comparison between the α7 and 5HT3 receptors is at the subunit arrangement and protein folding. Crystal structures of the nicotinic and serotoninergic T7 Tag Peptide receptors [45], [46] reinforced the concept of similarities between these families of rece
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Our study like that of Zill et al included European
2023-02-01

Our study, like that of Zill et al. (2012) included European Caucasians, although their population was much smaller (n=162) and more heterogeneous (19–72years). Further, potential confounding or effect modification by other health, lifestyle or genetic factors was not considered. These differences m
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The synthetic route to M developed by Rice was
2023-02-01

The synthetic route to M100907 developed by Rice was utilized, however, the chiral resolution was carried out at an earlier stage to provide the possibility of introducing different substituents onto the piperidinyl group. The conditions for this resolution were different from previously reported.
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Prostate cancer is the second leading
2023-02-01

Prostate cancer is the second leading cause of cancer-related death in men in the United States [25]. Similar to pancreatic cancer, prostate cancer has few diagnostic options available, particularly to differentiate indolent from aggressive disease. Axl is also overexpressed in ∼50% of prostate canc
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Here the so called alkali assay
2023-01-31

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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Apelin induced G i activation has
2023-01-31

Apelin induced Gαi activation has been demonstrated as a benefiting effect on cardiac contractility [12], [38], [39], and a vasodilator activity that protects against angiotensin-II-induced cardiovascular fibrosis and atheroma [40], [41]. In contrast, stretch causes hypertrophy through diminishing G
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br Emerging Vascular Mechanisms of AA Therapy Resistance
2023-01-31

Emerging Vascular Mechanisms of AA Therapy Resistance Experimental and clinical evidence indicates that physiological angiogenesis generates blood vessels capable of restoring perfusion [1], whereas tumoral angiogenesis gives rise to vessels that are structurally and functionally abnormal, therei
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Earlier studies with SERMs identified that distinct
2023-01-31

Earlier studies with SERMs identified that distinct chemical scaffolds have the ability to induce unique conformational changes in the ER, resulting in interaction with different cofactor subsets. The same has been demonstrated with SARMs, which induce distinct conformational changes compared to tes
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br Results We set out to
2023-01-31

Results We set out to identify in an unbiased manner a set of candidate “scaling factors” that might participate in transcription-dependent synaptic scaling up. The ex vivo slice and profiling studies were conducted on HsCt5 mice (described later) at postnatal day (P) 14 to P15, an age at which s
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Another possible scenario is that the
2023-01-31

Another possible scenario is that the same pathologic process has different effects in different people. It might be that the pathway outlined in Fig. 6A is operative in some individuals, but other individuals have a factor Q (which could be genetic or environmental) that blocks the effect of A on T
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Heat shock protein Hsp is a molecular chaperone that plays
2023-01-31

Heat shock protein 90 (Hsp90) is a molecular chaperone that plays a central role in regulating the maturation, activation and stability of numerous “client proteins” that drive the development and progression of many cancers. Therefore, inhibition of Hsp90 would result in degradation of the client p
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Aprotinin Cancer stem cells CSCs may have
2023-01-31

Cancer stem cells (CSCs) may have been first identified in teratocarcinomas [11], [12], with its initial clues date back to the 19th century [13]. Kleinsmith and Pierce [12] established the immortal pluripotent teratocarcinoma lines from a single transplanted multi-potent malignant cell, strongly su
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