Sökning: "inhibitors"
Visar resultat 6 - 10 av 1476 avhandlingar innehållade ordet inhibitors.
6. Design and synthesis of HIV-1 protease inhibitors
Sammanfattning : Human Immunodeficiency Virus (HIV) is the causative agent of Acquired Immune Deficiency Syndrome (AIDS). The C2-symmetric HIV-1 protease is one of the prime targets for chemotherapy in the treatment of the HIV infection. Inhibition of HIV-1 protease leads to immature and non-infectious viral particles. LÄS MER
7. Inhibitors of Human and Malaria Parasite Dihydroorotate Dehydrogenase
Sammanfattning : In the first part of the PhD work, small chemical entities (fragments) found to inhibit human dihydroorotate dehydrogenase (DHODH), were chemically optimized. As part of an ample program at Active Biotech to find new drugs against autoimmune diseases, expanded fragments were repeatedly designed, synthesized and evaluated in a human DHODH assay. LÄS MER
8. Novel Procedures for Identification and Characterization of Viral Proteases Inhibitors
Sammanfattning : Viral proteases are often considered to be attractive drug targets because of their crucial function in the viral replication machinery. In order to increase our knowledge of these important targets and to contribute to the discovery and development of new antiviral drugs, the proteases from hepatitis C virus (HCV) and human cytomegalovirus (HCMV) have been produced and their interactions with inhibitors and fragments have been characterized, using enzyme inhibition and SPR biosensor based interaction assay. LÄS MER
9. Modulating Sirtuin Activity - Design, Synthesis and Evaluation of Sirtuin 2 Inhibitors
Sammanfattning : Sirtuins (SIRTs) are NAD+-dependent lysine deacetylating enzymes targeting histones and a multitude of non-histone proteins. The SIRTs have been related to important cellular processes such as gene expression, cell proliferation, apoptosis and metabolism. They are proposed to be involved in the pathogenesis of e.g. LÄS MER
10. Characterization of conjugated protease inhibitors
Sammanfattning : The overall theme of this thesis is a step by step approach for the design and characterization of conjugated protease inhibitors. This involves both a new assay method for protease activity and protease inhibition (paper I), a study of the stoichiometry for protease inhibitor interaction (paper II), design of inhibitory peptides (paper IV) and the construction of inhibitor conjugates (paper III & IV). LÄS MER