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Design, synthesis and enzymatic activity of highly selective human mitochondrial thymidine kinase inhibitors
- Publication Year :
- 2001
-
Abstract
- Highly selective arabinofuranosyl nucleosides, which inhibit the mitochondrial thymidine kinase (TK-2) without affecting the closely related herpes simplex virus type 1 thymidine kinase (HSV-1 TK), varicella-zoster virus thymidine kinase (VZV-TK), cytosolic thymidine kinase (TK-1) or the multifunctional Drosophila melanogaster deoxyribonucleoside kinase (Dm-dNK), have been obtained. SAR studies indicate a close relation between the length of the substituent at the 2' position of the arabinofuranosyl moiety and the inhibitory activity.
- Subjects :
- Models, Molecular
viruses
Clinical Biochemistry
Pharmaceutical Science
Mitogen-activated protein kinase kinase
Biochemistry
Thymidine Kinase
MAP2K7
chemistry.chemical_compound
Inhibitory Concentration 50
Structure-Activity Relationship
Viral Proteins
TANK-binding kinase 1
Catalytic Domain
Drug Discovery
Humans
Enzyme Inhibitors
Molecular Biology
biology
Kinase
Organic Chemistry
Cyclin-dependent kinase 2
Mitochondria
Deoxyribonucleoside
chemistry
Thymidine kinase
Drug Design
biology.protein
Molecular Medicine
Cyclin-dependent kinase 9
Arabinonucleosides
Subjects
Details
- Language :
- English
- Database :
- OpenAIRE
- Accession number :
- edsair.doi.dedup.....28b09843dc4da5c2a55345d29dd7ca25