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Changes in actin microfilaments are mediated by changes in e
2024-09-29
Changes in [Ala92]-p16 (84-103) receptor microfilaments are mediated by changes in extracellular matrix, mechanical stimulation or growth factors intracellular signaling. We observed significant changes in a number of intracellular signaling pathways associated with changes in actin dynamics during
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Our initial approach to identify hits was two
2024-09-29
Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI Chrysin library as well as a virtual screening (VS) campaign, utilizing a publically available crystal structure of ACK1 (PDB code: ). A tolerance for protein flexibility was inco
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br Improvement of endothelial function The vascular
2024-09-29
Improvement of endothelial function The vascular endothelium is a single layer of Phosphate Colorimetric Assay Kit synthesis that lines the inner surface of all blood vessels and the heart. In addition to function as a selective barrier to prevent the diffusion of macromolecules from the blood l
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Introduction The lysosomal storage disorder Gaucher
2024-09-29
Introduction The lysosomal storage disorder Gaucher disease (Mendelian Inheritance in Man, OMIM #230800) results from the recessively inherited deficiency of lysosomal glucocerebrosidase (GCase, EC 3.2.1.45), caused by mutations in the gene GBA1 (MIM# 606463) located on chromosome 1q21. The enzymat
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Taken together BRP represents a
2024-09-29
Taken together, BRP-187 represents a novel chemotype of LT biosynthesis inhibitors with outstanding potency in human PMNL and monocytes activated under pathophysiological relevant conditions and with effectiveness in vivo. Using the PLA that visualizes the in situ interaction between 5-LO and FLAP i
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Numerous studies have reported high
2024-09-29
Numerous studies have reported high glutamate levels in the brains of patients with depression, indicating that the glutamate system plays a crucial role in depression (Sanacora et al., 2004; Kendell et al., 2005; Hashimoto et al., 2007). Furthermore, several clinically effective antidepressant drug
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HT modulates cortical and hippocampal pyramidal cell functio
2024-09-29
5-HT modulates cortical and hippocampal pyramidal cell function in a very complex manner, since most 5-HT receptor subtypes (excitatory as well as inhibitory) are expressed on pyramidal Forsythoside A as well as GABAergic interneurons that exert inhibitory control over pyramidal cells (Leiser et al
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The synthetic route to M developed by Rice was
2024-09-29
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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In conclusion AXL overexpression preexisted in a subgroup
2024-09-29
In conclusion, AXL overexpression preexisted in a subgroup of treatment-naive lung adenocarcinoma specimens harboring an activating EGFR mutation or in those with wild-type EGFR. Anti-AXL therapeutics delivered up front in combination with the EGFR inhibitor might overcome intrinsic or acquired resi
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In PMCA Mg favors the conversion E P
2024-09-28
In PMCA, Mg2+ favors the conversion E1P → E2P [13] and, as in SERCA [11], it accelerates the phosphorylation displacing the E1–E2 equilibrium towards E1. In SERCA, Sørensen et al. [41], proposed that ATP reacts by an associative mechanism mediated by two Mg2+ ions to form an aspartyl-phosphorylated
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br Materials and methods br
2024-09-28
Materials and methods Results Discussion CUs, which have been used as traditional medicine for thousands of years in East Asian countries, have the potential to be used for cancer chemoprevention and chemotherapy [17], [18], [19], [20]. CuB is one of the most promising agents as it is repor
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dynorphin receptor br Materials and methods br Results br Di
2024-09-28
Materials and methods Results Discussion I/R injury is characterized by myocardial damage triggered by the ischemic insult followed by reperfusion injury. While the primary insult depends mainly on the severity and duration of blood flow restriction and the breakdown of ATP-dependent dynorp
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Plasma apelin levels predict the major cardiovascular event
2024-09-28
Plasma apelin levels predict the major cardiovascular event after percutaneous coronary intervention in patients with ST elevation myocardial infarction (STEMI), and adverse events are higher in patients with lower plasma apelin levels [75]. Apelin and its receptor are markedly upregulated in the he
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AP activity is increased by MAP
2024-09-28
AP-1 activity is increased by MAP kinase stimulation in different cell types (Whitmarsh and Davis, 1996), while MKP-1, the enzyme that catalyzes the dephosphorylation and inactivation of MAP kinases in the nucleus, inhibits AP-1 (Rössler et al., 2008, Rössler and Thiel, 2009, Mayer et al., 2011, Thi
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HOBt Most human diseases e g cancer diabetes and neurodegene
2024-09-28
Most human diseases (e.g., cancer, diabetes, and neurodegenerative diseases) are complex and multifactorial. Several investigations in the literature focused on new multi-target drug development, which implies active pharmacophores incorporation in one scaffold (Meunier, 2008, Lazar et al., 2004, Te
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