Sökning: "inhibitor design"

Visar resultat 1 - 5 av 128 avhandlingar innehållade orden inhibitor design.

  1. 1. Structure-aided design of antiviral drugs : Application of the method on HIV-1 protease and SIV reverse transcriptase

    Författare :Hans Ola Andersson; Uppsala universitet; []
    Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; Developmental biology; HIV; protease; SIV; reverse transcriptase; structure; inhibitor; drug design; Utvecklingsbiologi; Developmental biology; Utvecklingsbiologi; molekylärbiologi; Molecular Biology;

    Sammanfattning : Many efforts have been made to control the AIDS epidemic. Extensive studies have been done on the biology, biochemistry, and structural biology of HIV in the search for antiviral drugs. The viral-encoded enzymes reverse transcriptase and protease have been main targets for drug design. LÄS MER

  2. 2. Cyclic Sulfamide HIV-1 Protease Inhibitors : Design, Synthesis and Modelling

    Författare :Anna Ax; Anders Karlén; Anders Hallberg; Tommy Liljefors; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Pharmaceutical chemistry; AIDS; HIV; protease inhibitor; aspartic protease; molecular modelling; 3D-QSAR; CoMFA; Farmaceutisk kemi; Pharmaceutical chemistry; Farmaceutisk kemi;

    Sammanfattning : Ten years ago, the first protease inhibitor targeting the human immunodeficiency virus (HIV) was approved for clinical use. Highly active antiretroviral therapy (HAART), which combined protease and reverse transcriptase inhibitors, quickly became the standard therapy for treating patients infected with HIV and Acquired Immune Deficiency Syndrome (AIDS). LÄS MER

  3. 3. Approaches to soft drug analogues of dihydrofolate reductase inhibitors : Design and synthesis

    Författare :Malin Graffner Nordberg; Uppsala universitet; []
    Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Pharmaceutical chemistry; soft drug; dihydrofolate reductase; synthesis; Farmaceutisk kemi; Pharmaceutical chemistry; Farmaceutisk kemi; Organic Pharmaceutical Chemistry; Organisk farmaceutisk kemi;

    Sammanfattning : The main objective of the research described in this thesis has been the design and synthesis of inhibitors of the enzyme dihydrofolate reductase (DHFR) intended for local administration and devoid of systemic side-effects. The blocking of the enzymatic activity of DHFR is a key element in the treatment of many diseases, including cancer, bacterial and protozoal infections, and also opportunistic infections associated with AIDS (Pneumocystis carinii pneumonia, PCP). LÄS MER

  4. 4. Peptide-Based Inhibitors of Hepatitis C Virus NS3 Serine Protease: Kinetic Aspects and Inhibitor Design

    Författare :Anton Poliakov; Helena Danielson; Boris Turk; Uppsala universitet; []
    Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; Biochemistry; serine protease; inhibitor; slow-binding; protein purification; Biokemi; Biochemistry; Biokemi;

    Sammanfattning : Hepatitis C is a serious disease that affects about 200 million people worldwide. No anti-HCV vaccine or specific anti-viral drugs are available today. Non-structural protein 3 (NS3) of HCV is a bifunctional serine protease/helicase, and the protease has become a prime target in the search for anti-HCV drugs. LÄS MER

  5. 5. Homotrimeric dUTPases : Principles of Catalysis and Inhibitor Design

    Författare :Lorena Gonzalez Palmén; Jan Kvassman; Dolores Gonzalez-Pacanowska; Högskolan i Kalmar; []
    Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; dUTPases; kinetics; ground state destabilization; inhibitors; Biochemistry; Biokemi; Natural Science; Naturvetenskap;

    Sammanfattning : The ubiquitous enzyme dUTPase hydrolyzes dUTP into dUMP and pyrophosphate, preventing DNA fragmentation and cell death due to accumulation of dUTP. Inhibitors of dUTPase could serve as drugs in the treatment of cancers and infectious diseases. This thesis presents five studies. LÄS MER