The first part of this manuscript is about the total synthesis of the aspidosperma alkaloids leuconoxine, melodinine E and mersicarpine. Our synthetic strategy used a radical translocation-conjugate addition cascade to construct the core of the natural product. Specifically, a vinyl radical was generated from the homolysis of the C–I bond...
In biology, function and disease are closely intertwined, requiring the coordination of hundreds of intricate chemical reactions. Interdisciplinary cooperation between chemical and biological approaches is necessary to decipher the chemical links between physiological and pathological conditions. In this arena, the precision tools made possible with chemical biology can manipulate and...
Toxoflavin, a toxic secondary metabolite produced by a variety of bacteria, has been implicated as a causative agent in food poisoning and a virulence factor in phytopathogenic bacteria. This toxin is produced by the tox operon in Burkholderia glumae, in which the encoded protein, ToxD, was previously characterized as essential...
Polyphenolic compounds found in foods such as fruits, vegetables, legumes, nuts and grains, are an integral part of the human diet. Within polyphenols, proanthocyanidins are referred to as condensed tannins and encompass procyanidins, propelargonidins and prodelphinidins. Among these, procyanidins are the largest group. Recent interest in these compounds is related...
M. avium subsp. hominissuis (MAH) and M. abscessus subsp. abscessus (MAB) both belong to the clinically important non-tuberculous mycobacterial (NTM) group that infect immunocompromised patients with AIDS and individuals with underlining lung conditions such as bronchiectasis or cystic fibrosis. The main challenge of treating MAH and MAB patients is an...
Mensacarcin is a stereogenic complex polyketide with potent anti-tumor activity produced by a soil-dwelling Streptomyces bottropensis. The US National Cancer Institute (NCI) 60 human tumor cell line anticancer drug screen (NCI-60) reveals mensacarcin’s cytostatic properties in almost all tested cell lines and distinct cytotoxic properties specifically in eight melanoma cell...
Atopic Dermatitis (AD) is a widespread skin disorder, affecting some 20% of the world’s population. Though the precise molecular underpinnings are still being understood, changes in lipid composition within the epidermal stratum corneum (SC) layer have been shown to be closely linked with AD. Previous studies have identified several specific...
Neisseria gonorrhoeae is the sexually transmitted pathogen responsible for millions of cases of gonorrhea worldwide each year. Rapidly-spreading antibiotic resistance is diminishing the ability to effectively treat a disease with significant consequences to female and male reproductive health, as well as to neonatal well-being. A protective vaccine has the potential...
The function of a protein is defined by its three-dimensional structure, and in understanding the three-dimensional structure of a protein, we gain an understanding of its function and mechanism. Protein structures, especially at high resolution, can provide detailed insights into many elements of enzyme function and catalysis – identifying residues...
Gadusol is a UV-B-absorbent compound found in fish and other marine organisms where it is presumed to play a role as a sunscreen and antioxidant. In light of commercial potential as a replacement for problematic synthetic sunscreens, a process to produce recombinant gadusol in the yeast Saccharomcyces cerevisiae was investigated....