Gennady B Lapa

Ученая степень не указана    /    страна не указана

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Сфера научных интересов

Публикации

Synthesis of New Congeners of 1-methyl-3-aminoisoquinolines, Evaluation of Their Cytotoxic Activity, In Silico and In Vitro Study of Their Molecular Targets as PDE4B.

Lapa GB, Tsunoda T, Shirasawa S, et al
To examine the cytotoxic activity of congeners of 3-amino-isoquinoline, we performed the phenotypic screening using panel of 60 cell lines and found that (N-(6,7-dimethoxy-1-methyl-isoquinolin-3-yl)-4-{[(1-ethyl-4-methyl-1H-pyrazol-3-yl)methyl]amino}benzamide (4d)) exhibited the significant...
Chem Biol Drug Des. 2016 Apr;87(4):575-82. doi: 10.1111/cbdd.12691. Epub 2015 Dec 29.
→ 3-amino-isoquinoline   → 3D floating culture   → HCT116   → HKe3   → K562   → KRAS   → PDE   → T-47D   → breast cancer   → colorectal cancer   → phenotypic screening   → reversal docking   → virtual screening  

Thienoquinolines as novel disruptors of the PKCe/RACK2 protein-protein interaction

Rechfeld F, Gruber P, Kirchmair J, Boehler M, Hauser N, Hechenberger G, Garczarczyk D, Lapa GB, Preobrazhenskaya MN, Goekjian P, Langer T, Hofmann J.
ABSTRACT: Ten protein kinase C (PKC) isozymes play divergent roles in signal transduction. Because of sequence similarities, it is particularly difficult to generate isozyme-selective small molecule inhibitors. In order to identify such a selective binder, we derived a pharmacophore model from...
J Med Chem. 2014 Apr 24;57(8):3235-46.
→ protein-protein interaction   → Thienoquinolines   → PKCe  

Образование

Профессиональный опыт

фев 2008 — авг 2009 Chemist — ASINEX

Научные и исследовательские проекты

Synthesis and biological evaluation of thienoquinolines as disruptors of the PKCe/RACK2 protein-protein interaction

The superfamily of the protein kinase C (PKC) comprises ten isozymes and is widely known for its key role in signal transduction. Acquiring isozyme-selective inhibitors is a difficult task due to the high sequence similarity within the ten PKCs. It was found that N-(4-acetylphenyl)-3-amino-6,7-ethelendioxy-thieno[2,3-b]quinoline-2-carboxamide (1b) shows promising inhibitory activities on the...

Two approaches to the use of bezo[c][1,2]oxaboroles as active fragments for synthetic transformation of clarithromycin

Two synthetic pathways for conjugates of clarithromycin (active against Gram positive infections) and congeners of 1-hydroxy-1,3-dihydrobenzoxa[2,1][c]borol (effective for Gram negative microbes) are elaborated. Clarithromycin and benzoxa[2,1][c]borol derivatives are the ligands of bacterial RNA. First pathway explored the substitution of the C-9 carbonyl group of clarithromycin, the second...

Ингибиторы фосфодиэстеразы PDE4 с противоопухолевым эффектом

Проведен дизайн, синтез и скрининг 3-амино-изохинолинов с противоопухолевыми свойствами.

Мои курсы

Общая биохимия

Сент , РНИМУ им Пирогова, каф биохимии МБФ (Нет описания курса)
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