DNA-binding drugs have shown potential against the parasitic disease African trypanosomiasis (sleeping sickness), but they have several disadvantages, such as toxic effects or inability to cross the blood-brain barrier, which may prevent them from treating individuals in which the parasites have entered the central nervous system.
Researchers at the Massachusetts Institute of Technology have developed a generative AI model that was able to generate novel antibiotic structures from either chemical fragments or de novo, starting from ammonia, methane, water or no starting point at all. In a study that was published online in Cell, the team tested two dozen of more than 10 million structures that were proposed as potential antibiotics by the model.
Lifemine Therapeutics Inc. has identified serine/threonine-protein phosphatase 2B (PPP3CC; PP2Bγ; calcineurin) inhibitors reported to be useful for the treatment of coronavirus acute respiratory syndrome (SARS), fungal infections, transplant rejection, and dermatological, respiratory and eye disorders.
Mycobacterium abscessus, a nontuberculous mycobacterium, is a significant cause of chronic pulmonary infections, particularly in individuals with compromised immune systems or structural lung conditions, such as cystic fibrosis.
Innovstone Therapeutics Ltd. has divulged prodrugs of deuterated baloxavir marboxil derivatives acting as polymerase basic protein 2 (PB2) (influenza virus) inhibitors reported to be useful for the treatment of influenza A, influenza B and influenza C viral infections.
Francisella tularensis, the causative agent of tularemia, is capable of causing severe illness at extremely low infectious doses through inhalation. No licensed tularemia vaccines exist in most Western countries, and current candidates lack efficacy against pneumonic forms. This highlights an urgent need for more effective vaccine strategies.
Chronic infection with the parasitic protozoan Cryptosporidium can cause debilitating diarrhea and lead to cognitive impairment and cachexia. Researchers at the University of Washington and collaborators have identified the 5-aminopyrazole-4-carboxamide BKI-1708 as an inhibitor of calcium-dependent protein kinase 1, which is highly expressed during proliferation of the parasite.
Methicillin-resistant Staphylococcus aureus (MRSA) is the leading cause of nosocomial infections, with an increasing prevalence worldwide. Researchers aimed to apply a new approach called “pseudo-natural product” (PNP) scaffolds for antibacterial development, and hypothesized that the indotropane class of PNPs might show potential activity against bacterial strains.
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