Publications by authors named "A I Yudin"
Stabilization of biologically relevant structural motifs has been a long-standing challenge. Here we show that atropisomeric dominant rotors can stabilize rare 3-helices in macrocycles. The target molecules were prepared using solid-phase peptide synthesis and subjected to extensive structural analysis.
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- The study focuses on the synthesis of anilinocyclophanes using naturally occurring terpenes like citronellol, geraniol, and farnesol.
- The resulting compounds show significant ring strain, reaching up to 31 kcal/mol, which affects their molecular structure and chirality.
- The research reveals unexpected results, such as the production of isomerized neraniline, illustrating how ring strain impacts the stability and reactivity of these cyclophanes.
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- Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN) are rare but severe skin reactions to medications, and analyzing a national database provides valuable insights into their occurrence.
- A study was conducted using reports from the Russian National Pharmacovigilance database between April 2019 and December 2023, focusing on demographic data and the drugs implicated in SJS and TEN cases.
- Out of 170 reports, 32.9% were SJS, 67.1% were TEN, with a notable number of cases in both pediatric and elderly populations; the most common drugs linked to these conditions included lamotrigine, ibuprofen, and ceftriaxone.
Passive membrane permeability is an important property in drug discovery and biological probe design. To elucidate the cell-penetrating ability of oxadiazole-containing (Odz) peptides, we employed the Chloroalkane Penetration Assay. The present study demonstrates that Odz cyclic peptides can be highly cell-penetrant depending on the position of specific side chains and the chloroalkane tag.
View Article and Find Full Text PDFWhile peptide macrocycles with rigidified conformations have proven to be useful in the design of chemical probes of protein targets, conformational flexibility and rapid interconversion can be equally vital for biological activity and favorable physicochemical properties. This study introduces the concept of "structural pin", which describes a hydrogen bond that is largely responsible for stabilizing the entire macrocycle backbone conformation. Structural analysis of macrocycles using nuclear magnetic resonance (NMR), molecular modelling and X-ray diffraction indicates that disruption of the structural pin can drastically influence the conformation of the entire ring, resulting in novel states with increased flexibility.
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