Протеїнкіназа PknB як перспективна мішень для розробки антибактеріальних препаратів проти Staphylococcus aureus

• Дата: 2023
• Автори: Moskovets, Anastasiia O., Pletnova, Larysa V., Maiula, Taras G., Tverdyy, Dmytro O., Volynets, Galyna P.
• Формат: Стаття
• Мова: English
• Опубліковано: V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine 2023
• Теми: Antibiotic resistance; antibacterial drugs; Staphylococcus aureus; Антибіотикорезистентність; антибактеріальні препарати
• Онлайн доступ: https://bioorganica.com.ua/index.php/journal/article/view/47
• Назва журналу: Ukrainica Bioorganica Acta

Antibiotic resistance is one of the biggest challenges in modern medicine. Uncontrolled use of antibiotics has led to the emergence of multidrug and extensively drug-resistant bacterial strains which are non-susceptible to almost all currently known antimicrobial drugs. Unfortunately, only a few novel antibacterial drugs have been developed in recent decades. Approximately 30% of the human population is colonized by Staphylococcus aureus. Unfortunately, the treatment of staphylococcal infections is complicated due to the ability of S. aureus to produce antibiotic-neutralizing enzymes. Today, methicillin-(MRSA) and vancomycin-resistant (VRSA) S. aureus strains are very widespread in the world and become serious medical and public problem. For example, in 2019, more than 1 million people died from infections caused by antibiotic-resistant S. aureus. Therefore, the search of novel antistaphylococcal agents with unexploited mechanisms of action is of urgent need. The serine/threonine protein kinase PknB is involved in a number of important signaling pathways of S. aureus, such as cell wall metabolism, antibiotic susceptibility, and virulence regulation. Taking into account that protein kinase PknB is a key component of the bacterial cell signaling network involved in a number of important biological processes, this enzyme can be considered as a promising molecular target for the search of novel inhibitors as antibacterial agents [7]. In this review we analyzed the current data on the structure, mechanisms of PknB activity regulation and functions, and also summarized the results of inhibitors search.