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Samenvatting Omcirkelde delen van structuren met bijhorende functies

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25-09-2025

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Structuren die voorkomen in deel 3 van het vak Medicinale chemie. Substituenten en onderdelen omcirkeld en bijhorende functies van de omcirkelde delen gegeven.

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INSULINE EN DIABETES
INSULINE

• A-keten: 21 AZ -> activiteit wanneer volledig intact
o Intramoleculaire S2-brug Cys6-Cys11
• B-keten: 30 AZ -> verwijdering eindstandige AZ met behoud activiteit
• Verbonden via 2 S2-bruggen 7A-7B cysteïne en 20A-19B cysteïne

INSULINE ANALOGEN – ultrasnelwerkende
INSULINE LISPRO
• 2e (lysine) en 3e (proline) laatste AZ B-
keten omgewisseld

INSULINE ASPART

• 3e (proline) laatste AZ B-keten
gemuteerd naar asparaginezuur

INSULINE GLULISINE
• 3e (asparagine) en 29e (lysine) AZ B-
keten gemuteerd naar resp. lysine en
glutaminezuur

INSULINE ANALOGEN - traagwerkende
INSULINE GLARGINE

, • 2 argine’s toegevoegd aan C-
terminus B-keten + 1 glycine
toegevoegd aan C-terminus A-keten

INSULINE DETIMIR
• C12-vetzuur toegevoegd op lysine-
B29

INSULINE DEGLUDEC
• C16-vetzuur via linker toegevoegd op
lysine-B29

DPP4-INHIBITOREN - INCRETINE (GIP en GLP-1) VERSTERKERS
VILDAGLIPTINE
• Pirolidine als proline-mimic
• Nitrille -> inhiberende activieit (amide-mimic van
natuurlijk substraat dat hydrolyse ondergaat)
• Specifieke interacties met bindingsplaats in enzyme

SAXAGLIPTINE
• Pirolidine als proline-mimic
• Nitrille -> inhiberende activieit (amide-mimic van
natuurlijk substraat dat hydrolyse ondergaat)
• Specifieke interacties met bindingsplaats in enzyme

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Institution: Katholieke Universiteit Leuven (KU Leuven)
Study: Farmaceutische Wetenschappen
Course: Medicinale chemie (K0B30A)

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Uploaded on: September 25, 2025
Number of pages: 18
Written in: 2024/2025
Type: SUMMARY

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functies
omcirkelde delen met functies

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Samenvatting Omcirkelde delen van structuren met bijhorende functies

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