Sökning: "plasmepsin"

Visar resultat 1 - 5 av 9 avhandlingar innehållade ordet plasmepsin.

  1. 1. Computational Studies of Enzymatic Enolization Reactions and Inhibitor Binding to a Malarial Protease

    Författare :Isabella Feierberg; Modesto Orozco; Uppsala universitet; []
    Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; Theoretical chemistry; enzyme mechanism; enolate; molecular dynamics; empirical valence bond; glyoxalase I; ketosteroid isomerase; triosephosphate isomerase; malaria; aspartic protease; plasmepsin; linear interaction energy; drug design; Teoretisk kemi; Theoretical chemistry; Teoretisk kemi; Molecular Biotechnology; Molekylär bioteknik;

    Sammanfattning : Enolate formation by proton abstraction from an sp3-hybridized carbon atom situated next to a carbonyl or carboxylate group is an abundant process in nature. Since the corresponding nonenzymatic process in water is slow and unfavorable due to high intrinsic free energy barriers and high substrate pKa s, enzymes catalyzing such reaction steps must overcome both kinetic and thermodynamic obstacles. LÄS MER

  2. 2. Design and Synthesis of Malarial Aspartic Protease Inhibitors

    Författare :Karolina Ersmark; Anders Hallberg; Michael Rowley; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Pharmaceutical chemistry; malaria; plasmepsin; aspartic protease; protease inhibitor; macrocycle; Farmaceutisk kemi; Pharmaceutical chemistry; Farmaceutisk kemi;

    Sammanfattning : Malaria is one of the major public health problems in the world. Approximately 500 million people are afflicted and almost 3 million people die from the disease each year. Of the four causative species Plasmodium falciparum is the most lethal. LÄS MER

  3. 3. On the Versatility of Microwave-Assisted Chemistry : Exemplified by Applications in Medicinal Chemistry, Heterocyclic Chemistry and Biochemistry

    Författare :Kristina M. Orrling; Mats Larhed; Fredrik Almqvist; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; NATURVETENSKAP; NATURAL SCIENCES; NATURVETENSKAP; NATURAL SCIENCES; microwave-assisted chemistry; malaria; aspartic protease; plasmepsin; PfPM4; PmPM4; PoPM4; PvPM4; inhibitor; unsaturated lactone; unsaturated lactam; unsaturated amide; lactam; Bestmann s ylide; ionic liquid; polymerase chain reaction; thermophilic enzyme; Pharmaceutical chemistry; Läkemedelskemi; Organic synthesis; Organisk syntes; Biochemistry; Biokemi; Biochemistry; biokemi;

    Sammanfattning : Today, the demand for speed in drug discovery is constantly increasing, particularly in the iterative processes of hit validation and expansion and lead optimization. Irradiation with microwaves (MWs) has been applied in the area of organic synthesis to accelerate chemical reactions and to facilitate the generation of new chemical entities since 1986. LÄS MER

  4. 4. Design and synthesis of aspartyl protease inhibitors : Targeting HIV-1 and malaria plasmepsin I and II

    Författare :Daniel Nöteberg; Charles Hedgecock; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Pharmaceutical chemistry; Farmaceutisk kemi; Pharmaceutical chemistry; Farmaceutisk kemi; Medicine; medicin;

    Sammanfattning : Aspartyl proteases can generally be inhibited by peptide mimics containing an uncleavable peptide bond isostere at the proposed cleavage site. One such peptide bond isostere is the hydroxyethylamine moiety, which in this thesis has successfully been incorporated in potential inhibitors of the HIV-1-protease as well as the malarial proteases plasmepsin I and II. LÄS MER

  5. 5. Structure-Assisted Design of Drugs Towards HIV-1 and Malaria Targets : Applied on Reverse Transcriptase and Protease from HIV-1 and Plasmepsin II from Plasmodium falciparum

    Författare :Jimmy Lindberg; Torsten Unge; Alexander Wlodawer; Uppsala universitet; []
    Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; Molecular biology; X-ray crystallography; Drug design; HIV-1; Malaria; Molekylärbiologi; Molecular biology; Molekylärbiologi;

    Sammanfattning : Globally of today, acquired immunodeficiency syndrome (AIDS) and malaria are two of the most threatening diseases known to mankind. The World Health Organization estimated that AIDS and malaria together claimed nearly 4 million lives in 2003 and many more were infected by the causative agent human immunodeficiency virus (HIV) and the Plasmodium falciparum (P. LÄS MER