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Direct Mass Spectrometry Technologies for Intraoperative Tissue Analysis and Surgical Margin Evaluation

Surgical resection remains a primary treatment for solid tumors. However, achieving tumor-free margins during surgery is challenging. Residual cancer cells at surgical margins are associated with increased recurrence and reduced survival rates. Intraoperative evaluation of surgical margins could enable more complete resection and reduce positive margins. Traditional frozen section histopathology has limitations including time-consumption, sampling errors, and availability of expertise.

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Natural Product-Inspired Peptide Cyclization Strategies and Their Therapeutic Applications

Peptide cyclization methods are useful in the development of therapeutic peptide leads with improved metabolic stability properties. To develop residue-selective peptide cyclization strategies, we draw inspiration from cyclic and lassoed peptide natural product scaffolds that exhibit diverse biological activities.

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Photoredox Catalysis in Late-Stage Aryl C(sp3 )−H Functionalizations

The high prevalence of aromatics in natural products and potential drug candidates makes them intriguing candidates for continued development of C-H functionalization reactions that proceed with high positional selectivity. Achieving site-selectivity can be a steep challenge as when there is a lack of appropriate directing groups or substitution patterns, more than one product isomer is commonly produced. Therefore, the development of aromatic C-H functionalization by means of chemo and site-selective activation is of interest. 

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Pure and Applied Chemistry of Trisubstituted Hydroxylamines: From Reaction Discovery to Drug Design

The presence of a heteroatom-heteroatom bond is a “structural alert” in medicinal chemistry, of which the hydroxylamine N-O bond, with its bond dissociation energy of 55-65 kcal·mol-1 and reputation for inherent mutagenicity and genotoxicity, is a pertinent example.1-3  Due to this broad moratorium, hydroxylamines are overwhelmingly excluded in medicinal chemistry optimization schemes and have thus received little attention from the synthetic chemistry or drug discovery communities.

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Strained Cyclic Allenes in Stereoselective Reactions and Total Synthesis of Lissodendoric Acid A

Strained Heterocyclic Allene systems are an underexplored building block in chemical synthesis, in spite of being known for more than five decades. Recent advances in azacyclic allenes showed inherent axial chirality that can be transferred to cycloaddition products to obtain highly complex polycyclic systems stereoselectively. With the total synthesis of Lissodendoric acid A is demonstrated that cyclic allenes are a powerful tool for complex molecule synthesis.

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Discovery of A New Subclass of Class I Ribonucleotide Reductase

Ribonucleotide reductases (RNRs) catalyze de novo biosynthesis of deoxynucleotides in almost all organisms that use DNA as their genetic material. They are current drug targets for both cancer and infectious diseases. All RNRs share a common catalytic mechanism initiated by a cysteinyl radical, while the radical generation varies greatly and provides the biochemical basis dividing the RNRs into the three major classes and several subclasses. All class I RNRs contain two subunits, R1 and R2, that are both essential for enzyme activity.

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