Sökning: "inhibitory activity"

Visar resultat 26 - 30 av 449 avhandlingar innehållade orden inhibitory activity.

1. 26. Inhibitors Targeting Insulin-Regulated Aminopeptidase (IRAP) : Identification, Synthesis and Evaluation

   Författare :Karin Engen; Mats Larhed; Mikael Elofsson; Uppsala universitet; []
   Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; compound screening; insulin-regulated aminopeptidase; IRAP; inhibitors; cognitive disorders; spiro-oxindole; quinazolinone; imidazopyridine; medicinal chemistry; structure-activity relationship; microwave heating; Medicinal Chemistry; Läkemedelskemi;

   Sammanfattning : Insulin-regulated aminopeptidase (IRAP) has emerged as a potential new therapeutic target for treatment of cognitive disorders. Inhibition of the enzymatic activity facilitates cognition in rodents. LÄS MER

3. 27. Design and Synthesis of Hepatitis C Virus NS3 Protease Inhibitors : Targeting Different Genotypes and Drug-Resistant Variants

   Författare :Anna Karin Belfrage; Anja Sandström; Ulf Ellervik; Uppsala universitet; []
   Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; NATURVETENSKAP; NATURAL SCIENCES; hepatitis C virus; HCV; NS3 protease inhibitors; structure-activity relationship; 2 1H -pyrazinone; quinazoline; resistance; Pd catalysis; Medicinal Chemistry; Läkemedelskemi; Farmaceutisk vetenskap; Pharmaceutical Science;

   Sammanfattning : Since the first approved hepatitis C virus (HCV) NS3 protease inhibitors in 2011, numerous direct acting antivirals (DAAs) have reached late stages of clinical trials. Today, several combination therapies, based on different DAAs, with or without the need of pegylated interferon-α injection, are available for chronic HCV infections. LÄS MER

4. 28. Design and Synthesis of Acyclic and Macrocyclic Peptidomimetics as Inhibitors of the Hepatitis C Virus NS3 Protease

   Författare :Anna Lampa; Anja Sandström; Youla Tsantrizos; Uppsala universitet; []
   Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; hepatitis C virus; HCV; NS3 protease inhibitor; structure-activity relationship; phenylglycine; ring-closing metathesis; Medicinal Chemistry; Läkemedelskemi;

   Sammanfattning : Hepatitis C is a blood-borne disease affecting 130-170 million people worldwide. The causative agent, hepatitis C virus (HCV), infects the liver and is the major reason for chronic liver disease worldwide. The HCV NS3 protease, a key enzyme in the virus replication cycle, has been confirmed to be an important target for drug development. LÄS MER

5. 29. p53 transcriptional activity as a tool to uncover novel and diverse druggable targets in cancer

   Författare :Marcus James Graeme Watson Ladds; Karolinska Institutet; Karolinska Institutet; []
   Nyckelord :;

   Sammanfattning : The transcription factor p53 is one of the most studied tumour suppressors with over 90 000 publications in PubMed referring to the protein. It is also the most frequently mutated gene across all cancer types with around 50% of cancers presenting as mutant p53, and when it is not mutated, it is frequently inactivated to circumvent its tumour suppressor function. LÄS MER

7. 30. Peptidomimetic Enzyme Inhibitors : Targeting M. tuberculosis Ribonucleotide Reductase and Hepatitis C Virus NS3 Protease

   Författare :Johanna Nurbo; Anders Hallberg; Anders Karlén; Anja Sandström; Per Arvidsson; Uppsala universitet; []
   Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; enzyme inhibitor; peptidomimetics; structure-activity relationship; tuberculosis; ribonucleotide reductase; hepatitis C virus; NS3 protease; Pharmaceutical chemistry; Farmaceutisk kemi; Medicinal Chemistry; Läkemedelskemi;

   Sammanfattning : This thesis focuses on the design and synthesis of inhibitors targeting Mycobacterium tuberculosis ribonucleotide reductase (RNR) and hepatitis C virus (HCV) NS3 protease; enzymes that have been identified as potential drug targets for the treatment of tuberculosis and hepatitis C, respectively. Small peptides have been recognized as inhibitors of these enzymes. LÄS MER