Дизайн и синтез коротких пептидов с ноотропной и нейропротективной активностью
Диссертация
Таким образом, в данной работе впервые сконструированы и синтезированы биологически активные низкомолекулярные миметики N0?, представляющие собой циклические тетра-, пентаи гексапептиды и линейные мономерные и димерные Ы-ацилдипептиды. Разработан метод циклизации. С помощью оригинального подхода к дизайну биологически активных пептидов, заключающегося в замене аминокислотных остатков на остатки… Читать ещё >
Содержание
- Страницы
- Глава 1. Литературный обзор
- 1. 1. Нейротрофины
- 1. 1. 1. Члены семейства нейротрофинов
- 1. 1. 2. Структура нейротрофинов
- 1. 2. Рецепторы нейротрофинов
- 1. 2. 1. Тирозинкиназные рецепторы
- 1. 2. 1. 1. Структура тирозинкиназных рецепторов
- 1. 2. 1. 2. Механизм передачи сигнала посредством Тгк рецепторов и биологические ответы
- 1. 2. 2. Рецептор р
- 1. 2. 2. 1. Структура р75 рецептора
- 1. 2. 2. 2. Механизм передачи сигнала посредством р75 рецептора и биологические ответы
- 1. 2. 1. Тирозинкиназные рецепторы
- 1. 1. Нейротрофины
- 1. 3. Вовлеченность нейротрофина NGF в патогенез нейродегенеративных заболеваний
- 1. 3. 1. Фармакологические данные NGF при применении его на различных моделях
- 1. 3. 2. Перспективы генной терапии NGF
- 1. 3. 3. Клинические испытания NGF
- 1. 4. Низкомолекулярные миметики нейротрофина NGF
- 1. 4. 1. Развитие низкомолекулярных миметиков нейротрофина NGF
- 1. 4. 2. Низкомолекулярные миметики 1 и 4 петель NGF
- 2. 1. Синтез дипептидов, соответствующих точечным мутантам АУР (4−5), и изучение взаимосвязи между видом точечной мутации и активностью дипептида
- 2. 2. Дизайн и синтез биологически активных циклических тетра-, пента- и гексапептидов, содержащих трипептидный фрагмент Р-изгиба 4-й петли NGF
- 2. 2. 1. Дизайн
- 2. 2. 2. Синтез
- 2. 2. 2. 1. Синтез линейных предшественников
- 2. 2. 2. 2. Синтез циклических пептидов
- 2. 2. 3. Биологическая активность циклических миметиков 4-й петли NGF in vitro
- 2. 3. Дизайн и синтез биологически активных N-ацилдипептидных мономерных и димерных миметиков 4-й и 1-й петель NGF
- 2. 3. 1. Дизайн
- 2. 3. 2. Синтез
- 2. 3. 2. 1. Синтез миметиков 4-й петлиNGF
- 2. 3. 2. 2. Синтез миметиков 1-й петли NGF
- 2. 3. 3. Биологическая активность синтезированных миметиков NGF
- 2. 3. 3. 1. Нейропротективные свойства пептидов in vitro
- 2. 3. 3. 2. Влияние пептидов на дифференцировку клеток
- 2. 3. 3. 3. Влияние пептидов на фосфорилирование тирозинкиназы А
- 3. 1. Синтез пироглутамилсодержащих дипептидов
- 3. 1. 1. Синтез пентахлорфенилового эфира ¿-пироглутаминовой кислоты и пентахлорфенилового эфира D-пироглутаминовой кислоты
- 3. 1. 2. Синтез амида?-пироглутамил-?-аспарагина.'
- 3. 1. 3. Синтез амида ?-пироглутамил-?-аспарагиновой кислоты
- 3. 1. 4. Синтез амида ?-пироглутамил-?-серина
- 3. 1. 5. Синтез амида ?)-пироглутамил-?-серина
- 3. 1. 6. Синтез амида?-пироглутамил-1)-серина
- 3. 1. 7. Синтез амида ?>-пироглутамил-1)-серина
- 3. 1. 8. Синтез амида ?-пироглутамил-^-гистидина
- 3. 1. 9. Синтез амида ?-пироглутамил-^-тирозина
- 3. 1. 10. Синтез /яре/я-бутилового эфира 1-пироглутамил-/я/?е/я-бутил-/<�аспарагиновой кислоты
- 3. 1. 11. Синтез /яре/я-бутилового эфира /,-пироглутамил-/яре/я-бутил-/,-серина
- 3. 2. Синтез циклопептидных аналогов фактора роста нервов
- 3. 2. 1. Получение линейных предшественников H-Gly-Gly-Gly-Asp (OBu')-Glu (OBu')-Lys (Boc)-OH, Н-С1у-С1у-А8р (ОВи')-С1и (ОВи')-Ьу8(Вос)-ОН) HH-Gly-Asp (OBu)-Glu (OBu)-Lys (Boc)-OH
- 3. 2. 2. Циклизация пептидов
- 3. 2. 2. 1. cyclo (-Gly-Gly-Gly-Asp (OBu')-Glu (OBu')-Lys (Boc)-)
- 3. 2. 2. 2. cyclo (-Gly-Gly-Asp (OBu')-Glu (OBu')-Lys (Boc)-)
- 3. 2. 2. 3. cyclo (-Gly-Asp (OBu)-Glu (OBu')-Lys (Boc)-) и димер
- 3. 2. 3. Удаление защитных групп
- 3. 2. 3. 1. cyclo (-Gly-Gly-Gly-Asp-Glu-Lys-)
- 3. 2. 3. 2. cyclo (-Gly-Gly-Asp-Glu-Lys-)
- 3. 2. 3. 3. cyclo (-Gly-Asp-Glu-Lys-)
- 3. 3. 1. Миметики 4-й петли
- 3. 3. 1. 1. Синтез амида N-моносукцинил-глутамил-лизина
- 3. 3. 1. 2. Синтез гексаметилендиамида бг/с-(К-моносукцинил-глутамил-лизина)
- 3. 3. 1. 3. Синтез триметилендиамида бис-(ТЧ-моносукцинил-глутамил-лизил-6-аминогексановой кислоты)
- 3. 3. 1. 4. Синтез гексаметилендиамида (пентаметилен, тетраметилен, пропилен, этилен) бмс-(моносукцинил-глутамил-лизина)
- 3. 3. 2. Миметики 1-й петли
- 3. 3. 2. 1. Синтез амидаN-ацетил-лизил-глутаминовой кислоты
- 3. 3. 2. 2. Синтез гексаметилендиамида бг/с-(1Ч-ацетил-лизил-глутаминовой кислоты)
- 3. 3. 2. 3. Синтез амида 6-аминокапроил-глицил-лизина
- 3. 3. 2. 4. Синтез гексаметилендиамида бмс-(6-аминокапроил-глицил-лизина)
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