Gentests

Exploiting Enzymatic Promiscuity to Engineer a Focused Library of Highly Selective Antifungal and Antiproliferative Aureothin Analogues

“…The successful incorporation of the mutasynthons was monitored by HPLC and HRMS. The expected masses and isotope patterns were recorded for all deoxyaureothin derivatives (7)(8)(9)(10)(11) resulting from the incorporation of all p-halogenated BAs, and the pseudohalide p-cyanobenzoate. Likewise, we observed the incorporation of p-methyl-BA and p-methoxysubstituted benzoate, yielding 12 and 13.…”

“…Interestingly, mainly deoxyaureothin and deoxyaureonitrile are produced when adding the entire variety of possible starter units (Figure 3c). We next omitted PNBA and noted an increased production of deoxyaureonitrile (7) and several halogenated analogues (8)(9)(10)(11) in low amounts (Figure 3b). Feeding a mixture lacking p-nitro-BA and p-cyano-BA led to a similar pattern but increased the yields of halogen-and methyl-substituted analogues (Figure 3a).…”

“…AurH proved to be remarkably tolerant toward artificial substrates. The oxygenase is capable of transforming deoxyaureonitrile ( 7), all four p-halogenated derivatives (8)(9)(10)(11), and even the unusual naphthoate (15) into the corresponding aureothin analogues 21-26. However, when R-pyrones like 17 were administered, no heterocycle formation was observed.…”

“…5,6 During the past two decades, the portfolio of methods for structural variation has been greatly increased by the knowledge of biosynthetic pathways and their rational reprogramming. Synthetic methods can now be complemented by feeding synthetic building blocks to suitable mutant strains (mutasynthesis), 7,8 using individual enzymes for biotransformations, 9 and swapping biosynthesis genes in a mix-and-match fashion (combinatorial biosynthesis). [10][11][12] These techniques have been predominantly applied to the large and diverse group of † HKI.…”

One‐pot, facile synthesis of well‐defined molecular brush copolymers by a tandem RAFT and ROMP, “Grafting‐through” strategy

“…INTRODUCTION Over the past decade, molecular brush copolymers, as an important type of nanoscopic single macromolecule, have attracted significant interest because of their synthetic challenges, 1-5 unique properties, 6-8 and potential applications as organic-inorganic hybrid nanomaterials, [9][10][11] photonic materials, [12][13][14] and carriers for nanomedicine. [15][16][17][18][19][20] Composed of densely grafted side chains along a polymeric backbone, brush copolymers can adopt spherical, cylindrical, or worm-like structures by varying the composition and chain length of either backbone or side chains.…”