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Amphotericin primarily kills yeast by simply binding ergosterol
Amphotericin B (AmB) is a prototypical small molecule natural product that can form ion channels in living eukaryotic cells and has remained refractory to microbial resistance despite extensiveExpand
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Amphotericin forms an extramembranous and fungicidal sterol sponge
Amphotericin has remained the powerful but highly toxic last line of defense in treating life-threatening fungal infections in humans for over 50 years with minimal development of microbialExpand
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Synthesis of many different types of organic small molecules using one automated process
A block-by-block way to manufacture molecules Carbon-based small molecules involved in biochemistry and drug design exhibit extraordinary structural diversity. But can we come up with a general setExpand
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A planning strategy for diversity-oriented synthesis.
In contrast to target-oriented synthesis (TOS) and medicinal or combinatorial chemistry, which aim to access precise or dense regions of chemistry space, diversity-oriented synthesis (DOS) populatesExpand
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Synthesis-enabled functional group deletions reveal key underpinnings of amphotericin B ion channel and antifungal activities
Amphotericin B is the archetype for small molecules that form transmembrane ion channels. However, despite extensive study for more than five decades, even the most basic features of this channelExpand
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Saliva-Based Molecular Testing for SARS-CoV-2 that Bypasses RNA Extraction
Convenient, repeatable, large-scale molecular testing for SARS-CoV-2 would be a key weapon to help control the COVID-19 pandemic. Unfortunately, standard SARS-CoV-2 testing protocols are invasive andExpand
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C2'-OH of amphotericin B plays an important role in binding the primary sterol of human cells but not yeast cells.
Amphotericin B (AmB) is a clinically vital antimycotic but is limited by its severe toxicity. Binding ergosterol, independent of channel formation, is the primary mechanism by which AmB kills yeast,Expand
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Non-toxic antimicrobials that evade drug resistance
Drugs that act more promiscuously provide fewer routes for the emergence of resistant mutants. But this benefit often comes at the cost of serious off-target and dose-limiting toxicities. The classicExpand
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A simple and modular strategy for small molecule synthesis: iterative Suzuki-Miyaura coupling of B-protected haloboronic acid building blocks.
  • E. Gillis, M. Burke
  • Chemistry, Medicine
  • Journal of the American Chemical Society
  • 9 May 2007
We herein describe a simple and highly modular strategy for small molecule synthesis involving the iterative cross-coupling of B-protected bifunctional haloboronic acids. Enabling this approach, weExpand
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A synthesis strategy yielding skeletally diverse small molecules combinatorially.
The efficient synthesis of small molecules having many molecular skeletons is an unsolved problem in diversity-oriented synthesis (DOS). We describe the development and application of a synthesisExpand
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