Engelhardt Institute of Molecular Biology

The sensitivity of acute myeloid leukemia to CDK8/19 inhibitors is determined by their metabolic profile

Cyclin-dependent kinases CDK8/19 are serine/threonine kinases that regulate transcription as part of the Mediator complex and phosphorylate several non-transcriptional substrates in both normal and tumor cells. Several studies have demonstrated that inhibition of CDK8/19 leads to...

Aspartate-dependent polyamine biosynthesis in bacteria: chemical synthesis of carboxypolyamines and mechanism-based design of hydroxylamine-containing inhibitors of carboxyspermidine decarboxylase

Abstract Biogenic polyamines spermidine, spermine and some of their derivatives are small organic polycations vitally important in all domains of life. Recent studies have demonstrated that polyamine biosynthesis is subject to convergent evolution and that some bacteria employ bi...

SLE-Associated rs2295613(A) Allele Strengthens a Predicted c-MYC Motif and Enhances SLAMF1 Promoter Reporter Activity in B Cells

SLAMF1 encodes CD150, an immunoregulatory receptor involved in lymphocyte activation, T–B-cell interactions, and humoral immune responses. The SLAMF1 promoter polymorphism rs2295613(G>A) was previously associated with systemic lupus erythematosus (SLE) susceptibility in a Chinese...

SIRT3 determines the sensitivity of cancer cells to mitochondrial targeting

Abstract SIRT3 is a mitochondria-localized member of the sirtuin family, playing a key role in cellular antioxidant defense. Its function in carcinogenesis and therapy response remains uncertain. In the present study, we sought to identify the role of SIRT3 in regulating cell dea...

Ring Contractionof Bicyclic Lactams: A MolecularEditing Aza-Favorski-Type Approach to Tetrahydroquinoline-2-carboxylicAcids

Abstract Development of skeletal editing methods offers new horizons for the acceleration of drug discovery. An original aza-Favorski-type approach is described for the ring contraction of benzazepine-2-ones, providing versatile tetrahydroquinoline-2-carboxylic acids. The sequenc...