The use of Fpocket and virtual screening techniques enabled us to identify potential allosteric druggable pockets within the SARS-CoV-2 RNA-dependent RNA polymerase (RdRp). Of the compounds screened, compound 1 was identified as a promising inhibitor, lowering a SARS-CoV-2 RdRp activity to 57 % in an enzymatic assay at 10 μM concentration. The structure of compound 1 was subsequently optimized in order to preserve or enhance inhibitory activity.
View Article and Find Full Text PDFYohimbine, a natural indole alkaloid and a nonselective adrenoceptor antagonist, possesses potential benefits in treating inflammatory disorders and sepsis. Nevertheless, its broader clinical use faces challenges due to its low receptor selectivity. A structure-activity relationship study of novel yohimbine analogues identified amino esters of yohimbic acid as potent and selective ADRA2A antagonists.
View Article and Find Full Text PDFBackground: Currently, PD-L1 expression in patients with tumors of various localizations is being actively studied. Studies on the expression of PD-L1 detected by clones SP142 and SP263 in gastric cancer (for the drugs atezolizumab and durvalumab, respectively) are rare in the literature. The prognostic role of PD-L1 expression in patients who were not treated with immune checkpoint inhibitors has also not been investigated.
View Article and Find Full Text PDFObjective: Clarification of the prognostic value and relationship of MUC-phenotypes of gastric cancer with clinical and morphological parameters.
Material And Methods: Surgical material from 310 patients with a verified diagnosis of gastric cancer was studied. Samples were immunohistochemically stained with antibodies to MUC2, CD10, MUC5AC.
Objective: Evaluation of the frequency of microsatellite instability in gastric adenocarcinomas in patients of the Russian Federation, determination of the relationship of microsatellite instability with clinical and morphological characteristics and the impact on the prognosis.
Material And Methods: We used samples of surgical material from 310 patients with a verified diagnosis of gastric cancer. The age of the patients ranged from 22 to 85 years (mean 63 years).
Objective: Assessment of the incidence of PD-L1 expression in EBV-associated gastric adenocarcinomas, as well as clarification of the clinical and morphological characteristics and median survival of patients with PD-L1-positive EBV-associated gastric cancer.
Material And Methods: Samples of surgical material from 127 patients with stomach cancer were studied. Each sample was stained by hybridization using primers for the Epstein-Barr virus-encoded small RNAs (EBER).
Objective: Assessment of the incidence of EBV-associated gastric adenocarcinomas in a sample of Russian patients, as well as clarification of the clinical and morphological characteristics and median survival of patients with EBV-associated gastric cancer.
Material And Methods: We used samples of surgical material from 282 patients with a verified diagnosis of gastric cancer. Each sample was stained by in situ hybridization using primers for the Epstein-Barr virus-encoded small RNAs (EBER).
The Aim Of The Study: Is to establish the relationship between the persistence of viral antigens of the Epstein-Barr virus (EBV) and the cellular composition of the immune microenvironment of tumor tissue and the mucous membrane of peritumoral area in gastric cancer.
Material And Methods: We used samples of surgical material from 55 patients with a verified diagnosis of gastric cancer. The expression of CD4, CD8, CD68, CD1a and LMP-1 was assessed.
Vopr Kurortol Fizioter Lech Fiz Kult
April 2018
Unlabelled: Myopia (short-sightedness) is the most common refractive disorder throughout the world prone to progression which is caused, inter alia, by violation of the working regime and resting conditions in the combination with the enhanced physical and psychological stresses.
Aim: The objective of the present study was to evaluate the influence of the strenuous physical exercises on the visual analyzer in the children and adolescents regularly engaged in sports activities.
Material And Methods: A total of 600 children and adolescents at the age from 8 to 17 years were recruited for the participation in the study.