Search for dissertations about: "prodrug activation"

Showing result 1 - 5 of 14 swedish dissertations containing the words prodrug activation.

  2. 1. Mutational Analysis and Redesign of Alpha-class Glutathione Transferases for Enhanced Azathioprine Activity

    Author : Olof Modén; Bengt Mannervik; Mikael Widersten; Kenneth Tew; Uppsala universitet; []
    Keywords : NATURVETENSKAP; NATURAL SCIENCES; TEKNIK OCH TEKNOLOGIER; ENGINEERING AND TECHNOLOGY; allelic variants; azathioprine; bioactivation; chimeric mutagenesis; directed evolution; DNA shuffling; enzyme engineering; glutathione transferase; GST; lysate screening; molecular docking; multiple alignment; multivariate analysis; polymorphism; principal component analysis; prodrug; prodrug activation; protein engineering; protein redesign; reduced amino acid alphabet; saturation mutagenesis; semi-rational enzyme engineering; site-directed mutagenesis; structure-activity relationship; structure-based redesign; Biokemi; Biochemistry;

    Abstract : Glutathione transferase (GST) A2-2 is the human enzyme most efficient in catalyzing azathioprine activation. Structure-function relationships were sought explaining the higher catalytic efficiency compared to other alpha class GSTs. READ MORE

  4. 2. Affibody-mediated targeting of HER-family receptors for cancer imaging and therapy

    Author : Charles Dahlsson Leitao; Stefan Ståhl; John Löfblom; Christoph Rader; KTH; []
    Keywords : NATURVETENSKAP; NATURAL SCIENCES; MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Cancer therapy; radionuclide imaging; affibody molecules; HER-receptors; prodrug; protein design; Cancerterapi; radionuklidavbildning; affibody molekyler; HER-receptorer; prodrog; proteindesign; Bioteknologi; Biotechnology;

    Abstract : Proteins are remarkable molecules with diverse and specialized functions playing essential roles in most biological processes. One such function is protecting us from diseases by the action of antibodies in our immune system that can recognize and mediate the destruction of invading pathogens by binding to foreign epitopes found on non-self proteins. READ MORE

  5. 3. Preclinical Studies of the Melphalan Prodrug J1 for Cancer Therapy

    Author : Malin Wickström; Joachim Gullbo; Rolf Larsson; Johan Hansson; Uppsala universitet; []
    Keywords : Pharmacology; Pharmacology; Chemotherapy; Melphalan prodrug; Cancer; Farmakologi;

    Abstract : J1 (L-melphalanyl-L-p-fluorophenylalanyl ethyl ester) is a dipeptide derivative of the alkylating agent melphalan with increased cytotoxicity. In this thesis the preclinical pharmacology of J1 has been characterized.Our results show that J1 rapidly enters the cells, where melphalan is released by hydrolysis. READ MORE

  6. 4. Novel Agonists and Antagonists of Platelet Receptors

    Author : Carl Högberg; Kardiologi; []
    Keywords : MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Platelets; P2Y12; SUCNR1; FPP; hypothermia;

    Abstract : Platelets are central for the primary haemostatis. The platelet has surface bound receptors that are vital for the platelet activation. READ MORE

  7. 5. Cytochrome P450 2W1 (CYP2W1) as a novel drug target in colon cancer therapy

    Author : Sandra Travica; Karolinska Institutet; Karolinska Institutet; []
    Keywords : ;

    Abstract : Cytochrome P450 2W1 (CYP2W1), is a monooxygenase enzyme endogenously expressed in fetal colon and normally silenced after birth. In adult life, the expression of CYP2W1 occurs exclusively in tumor cells yielding high amounts of the enzyme in 30% of human colon cancers. READ MORE