Combating a Master Manipulator: Staphylococcus aureus Immunomodulatory Molecules as Targets for Combinatorial Drug Discovery

Abstract

Staphylococcus aureus is a bacterial pathogen that can cause significant disease burden and mortality by counteracting host defenses through producing virulence factors to survive the immune responses evoked by infection. This emerging drug-resistant pathogen has led to a decline in the efficacy of traditional antimicrobial therapy. To combat these threats, precision antimicrobial therapeutics have been created to target key virulence determinants of specific pathogens. Here we review the benefits of, progresses in, and roadblocks to the development of precision antimicrobial therapeutics using combinatorial chemistry.

1,2,4‐Triazole hybrids with potential antibacterial activity against methicillin‐resistant Staphylococcus aureus

“…[ 1–5 ] Methicillin‐resistant Staphylococcus aureus (MRSA), which has been spreading throughout communities since the 1990s, is one of the most common healthcare‐associated multidrug‐resistant organisms across the world. [ 6–9 ] Currently, over 60% of S. aureus isolates are MRSA, and around 2% of healthy people carry MRSA. [ 10–12 ] MRSA is responsible for several difficult‐to‐treat infections in human beings, including skin and soft tissue infections, septicemia, endocarditis, pneumonia, enteritis, meningitis, osteomyelitis, and toxic shock syndrome.…”

One-Pot Parallel Synthesis of Unclosed Cryptands—Searching for Selective Anion Receptors via Static Combinatorial Chemistry Techniques

“…Combinatorial chemistry is a technology that allows for the parallel synthesis of a large number of chemical compounds, reaching hundreds of thousands or even millions, in a single chemical process. It is usually used to search for new drugs in the pharmaceutical industry, 1 although it is increasingly being used in creating new semiconductors, 2 catalysts, 3 and polymers. 4 Parallel synthesis and analysis of the resulting library allow costs to be minimized and significantly shorten the time of studies.…”

The increasing impact of Chinese innovative drug research on the global stage with a focus on drug discovery

“…After China's reform and opening up, notably since the implementation of 'the national significant new drug innovation program,' China's biopharma has achieved rapid development, Chinese scientists are transforming from the imitation of the generic drugs to the pursuit of the best-in-class drugs and first-in-class drugs [1][2][3][4].…”