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In our previous report we synthesized
2023-07-05
In our previous report, we synthesized derivatives with some straight chain residues on the 2-position of the 3-cyanopyridine ring of compound 1. In this time we tried to introduce aromatic ring on the chain of the 2-position. Namely, we replaced the hydroxyl-alkylamino group in the position 2 of t
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It is reported that calpain plays a critical
2023-07-05
It is reported that calpain-2 plays a critical role in BDNF-induced signaling and memory formation, and knockdown of calpain-2, but not calpain-1, completely suppresses BDNF-induced pathway activation and protein translation (Briz et al., 2013). BDNF prevents neuronal apoptosis or death (Ferrer et a
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br HMG proteins mobile modulators of chromatin structure
2023-07-05
HMG proteins: mobile modulators of chromatin structure and cellular phenotype The term “High Mobility Group” was originally coined for the HMG proteins because of their unusual solubility properties, their small size and their rapid mobility, relative to other chromatin proteins, during gel elect
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Angiogenesis is a process of
2023-07-05
Angiogenesis is a process of formation of new vessels from arterial vascularization created by endothelial cells. It is essential for the continuous growth of the tumor because it supplies the tumor with nutrients and oxygen, and eliminates cellular waste, which can be toxic to cancer cells [8]. Inf
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Inhibition of autophagy has been shown to alleviate
2023-07-05
Inhibition of autophagy has been shown to alleviate neuronal damage after cerebral ischemia, both in cell culture and rodent models (Koike et al., 2008, Li et al., 2015, Wang et al., 2016, Zhang et al., 2014, Zheng et al., 2014). Therefore, blockage of autophagy is a potential target for prevention
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First investigation of numerous membered
2023-07-05
First, investigation of numerous 12-14-membered ether-linked macrocycles revealed that smaller motifs were most lipophilic efficient. Compound (3) (12-membered macrocycle) exhibited good cellular potencies (ALK IC50 = 1.0 nM; ALK-L1196 M IC50 = 20 nM) and the highest LipE (4.4) with picomolar bindin
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br Acknowledgement This work was supported by grants from th
2023-07-05
Acknowledgement This work was supported by grants from the American Heart Association Scientist Development Grant (SDG) to A. Elmarakby and 1R01EY023315-01 award to M. Al-Shabrawey. Introduction Inflammatory response is the result of a complex interaction between immune Prochlorperazine mg an
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br Conclusion br Conflicts of
2023-07-05
Conclusion Conflicts of interest Compliance with ethical standards Introduction Tuberculosis is one of the leading causes of morbidity and mortality, amongst infectious diseases. India is a high burden country for Tuberculosis. Caused by Mycobacterium tuberculosis, it artesunate austral
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Encouraged by this observation a systematic SAR study on
2023-07-05
Encouraged by this observation, a systematic SAR study on the A ring -alkoxy was conducted as summarized in . The A ring methoxy-containing KRCA-0008 was proven an optimal substituent in terms of potency after all and its bigger size derivatives were detrimental in both biochemical and H3122 cellula
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Despite their different effects on cell survival
2023-06-29
Despite their different effects on cell survival, the functions of autophagy and apoptosis are not completely independent. Additionally, Cho et al. (2009) suggested that the mediation of caspase-3 links the apoptotic and autophagic signaling pathways. Consequently, to illuminate the correlation, exc
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6656 br Nanoparticle Conjugated Topoisomerase Inhibitors The
2023-06-27
Nanoparticle-Conjugated Topoisomerase Inhibitors The safety and efficacy of topotecan administered as LDM or MTD have been evaluated in several preclinical studies and a few clinical trials whose results showed that there can be significant adverse effects likely precluding its use in patients [5
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Due to anatomical and physiologic characteristics of the eye
2023-06-27
Due to anatomical and physiologic characteristics of the eye, administration of ophthalmic medicines is difficult and many studies showed that only approximately 5% of the administrated dose are absorbed by intraocular tissues, making the treatment unfeasible for diseases located in posterior segmen
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The first and the best characterized mechanism of receptor d
2023-06-26
The first and the best-characterized mechanism of receptor-dependent internalization of Aβ is mediated via the α7-nicotinic DPQ receptor [82]. Lipoprotein receptor protein represents the second best-studied route that facilitates the uptake of Aβ by neurons, involving additional molecules such as a
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Osteocytes the most abundant cells in an adult skeleton
2023-06-15
Osteocytes, the most abundant cells in an adult skeleton, are essentially mature osteoblasts that are surrounded by the products they secreted (Noble and Reeve, 2000). Osteocytes serve as mechanosensors that direct bone remodeling and that regulate the activities of osteoblasts and osteoclasts (Bone
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Docking studies were performed on the selected compounds to
2023-06-13
Docking studies were performed on the selected compounds to explore their binding patterns and to examine SAR in more detail. The co-crystal structure of ATX in complex with PF-8380 (PDB code: ) was selected for the docking studies due to structural similarity of the most potent compound with PF-83
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