Nonsymmetrically Substituted 1,1'-Biphenyl-Based Small Molecule Inhibitors of the PD-1/PD-L1 Interaction.

Therapeutic antibodies directed against either programmed cell death-1 protein (PD-1) or its ligand PD-L1 have demonstrated efficacy in the treatment of various cancers. In contrast with antibodies, small molecules have the potential for increased tissue penetration; better pharmacology; and therefore, improved antitumor activity. A series of nonsymmetric C2 inhibitors were synthesized and evaluated for PD-1/PD-L1 interaction inhibition.

IGF2 Peptide-Based LYTACs for Targeted Degradation of Extracellular and Transmembrane Proteins.

Lysosome-targeting chimeras (LYTACs) have recently been developed to facilitate the lysosomal degradation of specific extracellular and transmembrane molecular targets. However, the LYTAC particles described to date are based on glycopeptide conjugates, which are difficult to prepare and produce on a large scale. Here, we report on the development of pure protein LYTACs based on the non-glycosylated IGF2 peptides, which can be readily produced in virtually any facility capable of monoclonal antibody production.

[Effect of fullerene C60 on free-radical induced lipid peroxidation processes in bronchial asthma].

Lipids peroxidative oxidation as well as antioxidative enzymes superoxidedismutase and catalase activity state at the mice sensibilization with ovalbumine, its correction with fulleren FC60 as well as by its forms (FC60-OVA, mFC60 mFC60-OVA) modified and conjugated with ovalbumines have been studied. It has been demonstrated that the mice sensibilization with ovalbumin leads to the tissues peroxidative lipid oxidation processes enforcement as well as lowering antioxidative enzymes activity in lungs and spleen. Used different rulleren forms expressed antioxidative effect and modifying effect to antioxidative protection enzymes at a given pathology.

[Fullerene C60 exhibits immunomodulatory activity during adjuvant-induced arthritis in rats].

The effect of fullerene C60 (FC60) on the immune processes during experimental adjuvant-induced arthritis (AA) in rats has been studied. The results indicate the inhibitory action of FN60 during AA on cellular splenocyte proliferation, neutrophil phagocytic and oxygen-stimulatory activities in the NBT test, and humoral immune mechanisms involved in the production of antinuclear antibodies, formation of circulating immune complexes, and restoration of morphological structure of spleen. Taken together, these results allow FC60 to be considered as a new potential pharmacological agent that can realize its effects mainly through anti-inflammatory and immunomodulatory activity.

[The effectiveness of pioglitazone in the treatment of patients with coronary heart disease on the background of metabolic syndrome].

We investigated the effectiveness of pioglitazone in the treatment of patients with coronary heart disease in combination with MS. In the conduct of research revealed that the addition to standard therapy in patients with coronary heart disease on the background of metabolic syndrome pioglitazone led to a reliable slight decrease in body weight, BMI, hip circumference, waist their relationship. Receiving pioglitazone also significantly reduces the concentration of immunoreactive insulin and blood glucose levels, significantly altered lipid metabolism, which generally leads to a lower level of systemic inflammation, metabolism and reduces the severity of insulin resistance.