Search Results - "Tan, Derek S."

Cheminformatic comparison of approved drugs from natural product versus synthetic origins by Stratton, Christopher F., Newman, David J., Tan, Derek S.

“…[Display omitted] Despite the recent decline of natural product discovery programs in the pharmaceutical industry, approximately half of all new drug approvals…”
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Diversity-oriented synthesis: exploring the intersections between chemistry and biology by Tan, Derek S

“…Diversity-oriented synthesis (DOS) is an emerging field involving the synthesis of combinatorial libraries of diverse small molecules for biological screening…”
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Cheminformatic analysis of natural product-based drugs and chemical probes by Stone, Samantha, Newman, David J, Colletti, Steven L, Tan, Derek S

“…Covering: 1981 to 2019Natural products continue to play a major role in drug discovery, with half of new chemical entities based structurally on a natural…”
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Biomimetic diversity-oriented synthesis of benzannulated medium rings via ring expansion by Bauer, Renato A, Wenderski, Todd A, Tan, Derek S

“…Medium-sized ring structures can provide unique entry points into natural product–like chemical space but are synthetically challenging to access. A…”
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General Platform for Systematic Quantitative Evaluation of Small-Molecule Permeability in Bacteria by Davis, Tony D., Gerry, Christopher J., Tan, Derek S.

“…The chemical features that impact small-molecule permeability across bacterial membranes are poorly understood, and the resulting lack of tools to predict…”
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Structural basis for adenylation and thioester bond formation in the ubiquitin E1 by Hann, Zachary S., Ji, Cheng, Olsen, Shaun K., Lu, Xuequan, Lux, Michaelyn C., Tan, Derek S., Lima, Christopher D.

“…The ubiquitin (Ub) and Ub-like (Ubl) protein-conjugation cascade is initiated by E1 enzymes that catalyze Ub/Ubl activation through C-terminal adenylation,…”
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A diversity-oriented synthesis approach to macrocycles via oxidative ring expansion by Kopp, Felix, Stratton, Christopher F, Akella, Lakshmi B, Tan, Derek S

“…Macrocycles are well represented in natural product structures but have been challenging to access for inclusion in synthetic libraries. A new method uses ring…”
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Targeting adenylate-forming enzymes with designed sulfonyladenosine inhibitors by Lux, Michaelyn C., Standke, Lisa C., Tan, Derek S.

“…Adenylate-forming enzymes are a mechanistic superfamily that are involved in diverse biochemical pathways. They catalyze ATP-dependent activation of carboxylic…”
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Total Synthesis, Relay Synthesis, and Structural Confirmation of the C18-Norditerpenoid Alkaloid Neofinaconitine by Shi, Yuan, Wilmot, Jeremy T, Nordstrøm, Lars Ulrik, Tan, Derek S, Gin, David Y

“…The first total synthesis of the C18-norditerpenoid aconitine alkaloid neofinaconitine and relay syntheses of neofinaconitine and 9-deoxylappaconitine from…”
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Diisonitrile Lipopeptides Mediate Resistance to Copper Starvation in Pathogenic Mycobacteria by Buglino, John A., Ozakman, Yaprak, Xu, Yao, Chowdhury, Farhan, Tan, Derek S., Glickman, Michael S.

“…Bacterial pathogens and their hosts engage in intense competition for critical nutrients during infection, including metals such as iron, copper, and zinc…”
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Chemoenzymatic Synthesis of Novel Cytotoxic Epoxyketones Using the Eponemycin Biosynthetic Enzyme EpnF by Corless, Broderick C., Geißen, Raphael, Prescott, Nicholas A., David, Yael, Scheinberg, David A., Tan, Derek S.

“…Eponemycin is an α,β-epoxyketone natural product that inhibits the proteasome via covalent interaction of the epoxyketone warhead with catalytic N-terminal…”
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Principal component analysis as a tool for library design: a case study investigating natural products, brand-name drugs, natural product-like libraries, and drug-like libraries by Wenderski, Todd A, Stratton, Christopher F, Bauer, Renato A, Kopp, Felix, Tan, Derek S

“…Principal component analysis (PCA) is a useful tool in the design and planning of chemical libraries. PCA can be used to reveal differences in structural and…”
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Hydrogen-Bonding Catalysis and Inhibition by Simple Solvents in the Stereoselective Kinetic Epoxide-Opening Spirocyclization of Glycal Epoxides to Form Spiroketals by Wurst, Jacqueline M, Liu, Guodong, Tan, Derek S

“…Mechanistic investigations of a MeOH-induced kinetic epoxide-opening spirocyclization of glycal epoxides have revealed dramatic, specific roles for simple…”
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Stereoselective Synthesis of Acortatarins A and B by Wurst, Jacqueline M, Verano, Alyssa L, Tan, Derek S

“…Acortatarins A and B have been synthesized via stereoselective spirocyclizations of glycals. Mercury-mediated spirocyclization of a pyrrole monoalcohol side…”
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Small-molecule inhibition of siderophore biosynthesis in Mycobacterium tuberculosis and Yersinia pestis by Tan, Derek S, Quadri, Luis E N, Ferreras, Julian A, Ryu, Jae-Sang, Di Lello, Federico

“…Mycobacterium tuberculosis and Yersinia pestis, the causative agents of tuberculosis and plague, respectively, are pathogens with serious ongoing impact on…”
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The tert-Butylsulfinamide Lynchpin in Transition-Metal-Mediated Multiscaffold Library Synthesis by Bauer, Renato A., DiBlasi, Christine M., Tan, Derek S.

“…A unified synthetic approach to diverse polycyclic scaffolds has been developed using transition-metal-mediated cycloaddition and cyclization reactions of…”
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5-(Methylthio)tetrazoles as Versatile Synthons in the Stereoselective Synthesis of Polycyclic Pyrazolines via Photoinduced Intramolecular Nitrile Imine-Alkene 1,3-Dipolar Cycloaddition by Pla, Daniel, Tan, Derek S, Gin, David Y

“…A key thioether substituent in readily accessible 2-alkyl-5-(methylthio)tetrazoles enables facile photoinduced denitrogenation and intramolecular nitrile imine…”
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Pharmacokinetic and In Vivo Efficacy Studies of the Mycobactin Biosynthesis Inhibitor Salicyl-AMS in Mice by Lun, Shichun, Guo, Haidan, Adamson, John, Cisar, Justin S, Davis, Tony D, Chavadi, Sivagami Sundaram, Warren, J David, Quadri, Luis E N, Tan, Derek S, Bishai, William R

“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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Mechanism-based inhibitors of MenE, an acyl-CoA synthetase involved in bacterial menaquinone biosynthesis by Lu, Xuequan, Zhang, Huaning, Tonge, Peter J., Tan, Derek S.

“…The design, synthesis, and biochemical evaluation of mechanism-based OSB-CoA synthetase inhibitors is reported. Menaquinone (vitamin K 2) is an essential…”
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Advancing chemistry and biology through diversity-oriented synthesis of natural product-like libraries by Shang, Shiying, Tan, Derek S

“…Natural products provide the inspiration for a variety of strategies used in the diversity-oriented synthesis of novel small-molecule libraries. These…”
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