Total synthesis of himastatin
The Pentelute Lab aims to invent new chemistry for the efficient and selective modification of proteins, to ‘hijack’ these biological machines for efficient drug delivery into cells and to create new machines to rapidly and efficiently manufacture peptides and proteins.
Pentelute Lab, Chemistry, MIT, Chemistry Department, Boston, Cambridge, Biology, Peptides, Peptide, Proteins, Science, Rapid, Brad Pentelute, Brad,
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Total synthesis of himastatin

Total synthesis of himastatin

SCIENCE 24 Feb 2022 Vol 375, Issue 6583 pp. 894-899 DOI: 10.1126/science.abm6509

KYAN A. D’ANGELO, CARLY K. SCHISSEL, BRADLEY L. PENTELUTE, AND MOHAMMAD MOVASSAGHI

Abstract

The natural product himastatin has an unusual homodimeric structure that presents a substantial synthetic challenge. We report the concise total synthesis of himastatin from readily accessible precursors, incorporating a final-stage dimerization strategy that was inspired by a detailed consideration of the compound’s biogenesis. Combining this approach with a modular synthesis enabled expedient access to more than a dozen designed derivatives of himastatin, including synthetic probes that provide insight into its antibiotic activity.

Category
2022, Publications