Microbial proteasomes as drug targets
| Autor: | Hao Zhang, Gang Lin |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
Trypanosoma
Life Cycles Proteasome Endopeptidase Complex Drug Research and Development QH301-705.5 Parasitic Life Cycles Immunology Plasmodium falciparum Cancer Treatment Review Library Screening Research and Analysis Methods Microbiology Biochemistry Medical Conditions Virology Genetics Medicine and Health Sciences Parasitic Diseases Animals Humans Chagas Disease Biology (General) Molecular Biology Techniques Molecular Biology Leishmaniasis Pharmacology Protozoans Molecular Biology Assays and Analysis Techniques Bacteria Organisms Biology and Life Sciences Proteins Protein Complexes Proteasomes Eukaryota Mycobacterium tuberculosis RC581-607 Parasitic Protozoans Actinobacteria Oncology Parasitology Immunologic diseases. Allergy Proteasome Inhibitors Developmental Biology |
| Zdroj: | PLoS Pathogens, Vol 17, Iss 12 (2021) PLoS Pathogens PLoS Pathogens, Vol 17, Iss 12, p e1010058 (2021) |
| ISSN: | 1553-7374 1553-7366 |
| Popis: | Proteasomes are compartmentalized, ATP-dependent, N-terminal nucleophile hydrolases that play essentials roles in intracellular protein turnover. They are present in all 3 kingdoms. Pharmacological inhibition of proteasomes is detrimental to cell viability. Proteasome inhibitor rugs revolutionize the treatment of multiple myeloma. Proteasomes in pathogenic microbes such as Mycobacterium tuberculosis (Mtb), Plasmodium falciparum (Pf), and other parasites and worms have been validated as therapeutic targets. Starting with Mtb proteasome, efforts in developing inhibitors selective for microbial proteasomes have made great progress lately. In this review, we describe the strategies and pharmacophores that have been used in developing proteasome inhibitors with potency and selectivity that spare human proteasomes and highlight the development of clinical proteasome inhibitor candidates for treatment of leishmaniasis and Chagas disease. Finally, we discuss the future challenges and therapeutical potentials of the microbial proteasome inhibitors. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|