Novel Autotaxin Inhibitor ATX-1d Significantly Enhances Potency of Paclitaxel-An In Silico and In Vitro Study.

The development of drug resistance in cancer cells poses a significant challenge for treatment, with nearly 90% of cancer-related deaths attributed to it. Over 50% of ovarian cancer patients and 30-40% of breast cancer patients exhibit resistance to therapies such as Taxol. Previous literature has shown that cytotoxic cancer therapies and ionizing radiation damage tumors, prompting cancer cells to exploit the autotaxin (ATX)-lysophosphatidic acid (LPA)-lysophosphatidic acid receptor (LPAR) signaling axis to enhance survival pathways, thus reducing treatment efficacy.

Synthesis and Characterization of Derivatives of the Antifungal Peptoid RMG8-8.

Cryptococcal meningitis, caused by the fungal pathogen , is a devastating disease with a mortality rate of over 80%. Due to the increasing prevalence of resistance to antifungals and the high mammalian toxicity of current treatments, the development of new antifungal therapies is vital. In an effort to improve the biological properties of a previously discovered antifungal peptoid, termed RMG8-8, an iterative structure-activity relationship study was conducted.

Development of an Anti-Biofilm Screening Technique Leads to the Discovery of a Peptoid with Efficacy against .

Bacteria and fungi can secrete and reside within a complex polysaccharide matrix, forming a biofilm that protects these pathogens from the immune response and conventional antibiotics. Because many microbial pathogens grow within biofilms in clinical settings, there is a need for antimicrobial agents effective against biofilm-protected infections. We report the adaptation of a phenotypic high-throughput assay for discovering antimicrobial peptoids toward the screening of combinatorial libraries against established biofilms.

Discovery and Characterization of a Rapidly Fungicidal and Minimally Toxic Peptoid against .

A limited number of antifungals are available to treat infections caused by fungal pathogens such as and . Current clinical antifungals are generally toxic, and increasing resistance to these therapies is being observed, necessitating new, effective, and safe antifungals. Peptoids, or N-substituted glycines, have shown promise as antimicrobial agents against bacteria, fungi, and parasites.

Recent advances in the development of anti-infective peptoids.

In the search for new sources of antimicrobials many researchers have investigated antimicrobial peptides (AMPs) as templates for the design of innovative therapeutics. However, efforts to develop AMPs in this area has been severely hampered by their inherent susceptibility to enzymatic degradation. Given this only a handful of AMPs are currently in clinical trials.