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Evaluation of high-affinity phenyltetrahydroisoquinoline aldoximes, linked through anti-triazoles, as reactivators of phosphylated cholinesterases.

Maček Hrvat N, Kalisiak J, Šinko G, Radić Z, Sharpless KB, Taylor P, Kovarik Z.

Toxicol Lett. 2020 Mar 15;321:83-89. doi: 10.1016/j.toxlet.2019.12.016. Epub 2019 Dec 19.


Modular click chemistry libraries for functional screens using a diazotizing reagent.

Meng G, Guo T, Ma T, Zhang J, Shen Y, Sharpless KB, Dong J.

Nature. 2019 Oct;574(7776):86-89. doi: 10.1038/s41586-019-1589-1. Epub 2019 Oct 2.


SuFEx-enabled, agnostic discovery of covalent inhibitors of human neutrophil elastase.

Zheng Q, Woehl JL, Kitamura S, Santos-Martins D, Smedley CJ, Li G, Forli S, Moses JE, Wolan DW, Sharpless KB.

Proc Natl Acad Sci U S A. 2019 Sep 17;116(38):18808-18814. doi: 10.1073/pnas.1909972116. Epub 2019 Sep 4.


Assessment of ionizable, zwitterionic oximes as reactivating antidotal agents for organophosphate exposure.

Taylor P, Yan-Jye S, Momper J, Hou W, Camacho-Hernandez GA, Radic' Z, Rosenberg Y, Kovarik Z, Sit R, Sharpless KB.

Chem Biol Interact. 2019 Aug 1;308:194-197. doi: 10.1016/j.cbi.2019.05.015. Epub 2019 May 14. Review.


Biocompatible SuFEx Click Chemistry: Thionyl Tetrafluoride (SOF4 )-Derived Connective Hubs for Bioconjugation to DNA and Proteins.

Liu F, Wang H, Li S, Bare GAL, Chen X, Wang C, Moses JE, Wu P, Sharpless KB.

Angew Chem Int Ed Engl. 2019 Jun 11;58(24):8029-8033. doi: 10.1002/anie.201902489. Epub 2019 May 8.


Bacterial glycosyltransferase-mediated cell-surface chemoenzymatic glycan modification.

Hong S, Shi Y, Wu NC, Grande G, Douthit L, Wang H, Zhou W, Sharpless KB, Wilson IA, Xie J, Wu P.

Nat Commun. 2019 Apr 17;10(1):1799. doi: 10.1038/s41467-019-09608-w.


Counteracting tabun inhibition by reactivation by pyridinium aldoximes that interact with active center gorge mutants of acetylcholinesterase.

Kovarik Z, Maček Hrvat N, Kalisiak J, Katalinić M, Sit RK, Zorbaz T, Radić Z, Fokin VV, Sharpless KB, Taylor P.

Toxicol Appl Pharmacol. 2019 Jun 1;372:40-46. doi: 10.1016/j.taap.2019.04.007. Epub 2019 Apr 9.


Bifluoride Ion Mediated SuFEx Trifluoromethylation of Sulfonyl Fluorides and Iminosulfur Oxydifluorides.

Smedley CJ, Zheng Q, Gao B, Li S, Molino A, Duivenvoorden HM, Parker BS, Wilson DJD, Sharpless KB, Moses JE.

Angew Chem Int Ed Engl. 2019 Mar 26;58(14):4552-4556. doi: 10.1002/anie.201813761. Epub 2019 Feb 27.


Reversal of Tabun Toxicity Enabled by a Triazole-Annulated Oxime Library-Reactivators of Acetylcholinesterase.

Kovarik Z, Kalisiak J, Hrvat NM, Katalinić M, Zorbaz T, Žunec S, Green C, Radić Z, Fokin VV, Sharpless KB, Taylor P.

Chemistry. 2019 Mar 15;25(16):4100-4114. doi: 10.1002/chem.201805051. Epub 2019 Feb 14.


Pharmacology, Pharmacokinetics, and Tissue Disposition of Zwitterionic Hydroxyiminoacetamido Alkylamines as Reactivating Antidotes for Organophosphate Exposure.

Sit RK, Kovarik Z, Maček Hrvat N, Žunec S, Green C, Fokin VV, Sharpless KB, Radić Z, Taylor P.

J Pharmacol Exp Ther. 2018 Nov;367(2):363-372. doi: 10.1124/jpet.118.249383. Epub 2018 Sep 6.


Quantitative and Orthogonal Formation and Reactivity of SuFEx Platforms.

Gahtory D, Sen R, Pujari S, Li S, Zheng Q, Moses JE, Sharpless KB, Zuilhof H.

Chemistry. 2018 Jul 20;24(41):10550-10556. doi: 10.1002/chem.201802356. Epub 2018 Jun 27.


SuFEx Click Chemistry Enabled Late-Stage Drug Functionalization.

Liu Z, Li J, Li S, Li G, Sharpless KB, Wu P.

J Am Chem Soc. 2018 Feb 28;140(8):2919-2925. doi: 10.1021/jacs.7b12788. Epub 2018 Feb 16.


SuFEx Chemistry of Thionyl Tetrafluoride (SOF4 ) with Organolithium Nucleophiles: Synthesis of Sulfonimidoyl Fluorides, Sulfoximines, Sulfonimidamides, and Sulfonimidates.

Gao B, Li S, Wu P, Moses JE, Sharpless KB.

Angew Chem Int Ed Engl. 2018 Feb 12;57(7):1939-1943. doi: 10.1002/anie.201712145. Epub 2018 Jan 16.


A New Portal to SuFEx Click Chemistry: A Stable Fluorosulfuryl Imidazolium Salt Emerging as an "F-SO2 +" Donor of Unprecedented Reactivity, Selectivity, and Scope.

Guo T, Meng G, Zhan X, Yang Q, Ma T, Xu L, Sharpless KB, Dong J.

Angew Chem Int Ed Engl. 2018 Mar 1;57(10):2605-2610. doi: 10.1002/anie.201712429. Epub 2018 Jan 25.


"Inverse Drug Discovery" Strategy To Identify Proteins That Are Targeted by Latent Electrophiles As Exemplified by Aryl Fluorosulfates.

Mortenson DE, Brighty GJ, Plate L, Bare G, Chen W, Li S, Wang H, Cravatt BF, Forli S, Powers ET, Sharpless KB, Wilson IA, Kelly JW.

J Am Chem Soc. 2018 Jan 10;140(1):200-210. doi: 10.1021/jacs.7b08366. Epub 2017 Dec 21.


Bifluoride-catalysed sulfur(VI) fluoride exchange reaction for the synthesis of polysulfates and polysulfonates.

Gao B, Zhang L, Zheng Q, Zhou F, Klivansky LM, Lu J, Liu Y, Dong J, Wu P, Sharpless KB.

Nat Chem. 2017 Nov;9(11):1083-1088. doi: 10.1038/nchem.2796. Epub 2017 Jun 19.


SuFEx-Based Polysulfonate Formation from Ethenesulfonyl Fluoride-Amine Adducts.

Wang H, Zhou F, Ren G, Zheng Q, Chen H, Gao B, Klivansky L, Liu Y, Wu B, Xu Q, Lu J, Sharpless KB, Wu P.

Angew Chem Int Ed Engl. 2017 Sep 4;56(37):11203-11208. doi: 10.1002/anie.201701160. Epub 2017 May 18.


Click Chemistry-Facilitated Structural Diversification of Nitrothiazoles, Nitrofurans, and Nitropyrroles Enhances Antimicrobial Activity against Giardia lamblia.

Kim WJ, Korthals KA, Li S, Le C, Kalisiak J, Sharpless KB, Fokin VV, Miyamoto Y, Eckmann L.

Antimicrob Agents Chemother. 2017 May 24;61(6). pii: e02397-16. doi: 10.1128/AAC.02397-16. Print 2017 Jun.


Palladium-Catalyzed Fluorosulfonylvinylation of Organic Iodides.

Zha GF, Zheng Q, Leng J, Wu P, Qin HL, Sharpless KB.

Angew Chem Int Ed Engl. 2017 Apr 18;56(17):4849-4852. doi: 10.1002/anie.201701162. Epub 2017 Mar 29.


Multidimensional SuFEx Click Chemistry: Sequential Sulfur(VI) Fluoride Exchange Connections of Diverse Modules Launched From An SOF4 Hub.

Li S, Wu P, Moses JE, Sharpless KB.

Angew Chem Int Ed Engl. 2017 Mar 6;56(11):2903-2908. doi: 10.1002/anie.201611048. Epub 2017 Feb 6.


Ethenesulfonyl Fluoride (ESF): An On-Water Procedure for the Kilogram-Scale Preparation.

Zheng Q, Dong J, Sharpless KB.

J Org Chem. 2016 Nov 18;81(22):11360-11362. Epub 2016 Nov 3.


A Heck-Matsuda Process for the Synthesis of β-Arylethenesulfonyl Fluorides: Selectively Addressable Bis-electrophiles for SuFEx Click Chemistry.

Qin HL, Zheng Q, Bare GA, Wu P, Sharpless KB.

Angew Chem Int Ed Engl. 2016 Nov 2;55(45):14155-14158. doi: 10.1002/anie.201608807. Epub 2016 Oct 10.


Reengineering Antibiotics to Combat Bacterial Resistance: Click Chemistry [1,2,3]-Triazole Vancomycin Dimers with Potent Activity against MRSA and VRE.

Silverman SM, Moses JE, Sharpless KB.

Chemistry. 2017 Jan 1;23(1):79-83. doi: 10.1002/chem.201604765. Epub 2016 Nov 11.


Arylfluorosulfates Inactivate Intracellular Lipid Binding Protein(s) through Chemoselective SuFEx Reaction with a Binding Site Tyr Residue.

Chen W, Dong J, Plate L, Mortenson DE, Brighty GJ, Li S, Liu Y, Galmozzi A, Lee PS, Hulce JJ, Cravatt BF, Saez E, Powers ET, Wilson IA, Sharpless KB, Kelly JW.

J Am Chem Soc. 2016 Jun 15;138(23):7353-64. doi: 10.1021/jacs.6b02960. Epub 2016 Jun 2.


Chemoselective Synthesis of Polysubstituted Pyridines from Heteroaryl Fluorosulfates.

Zhang E, Tang J, Li S, Wu P, Moses JE, Sharpless KB.

Chemistry. 2016 Apr 11;22(16):5692-7. doi: 10.1002/chem.201600167. Epub 2016 Mar 15.


Steric and Dynamic Parameters Influencing In Situ Cycloadditions to Form Triazole Inhibitors with Crystalline Acetylcholinesterase.

Bourne Y, Sharpless KB, Taylor P, Marchot P.

J Am Chem Soc. 2016 Feb 10;138(5):1611-21. doi: 10.1021/jacs.5b11384. Epub 2016 Jan 28.


Synthesis of Sulfotyrosine-Containing Peptides by Incorporating Fluorosulfated Tyrosine Using an Fmoc-Based Solid-Phase Strategy.

Chen W, Dong J, Li S, Liu Y, Wang Y, Yoon L, Wu P, Sharpless KB, Kelly JW.

Angew Chem Int Ed Engl. 2016 Jan 26;55(5):1835-8. doi: 10.1002/anie.201509016. Epub 2015 Dec 22.


In Situ Click Chemistry for the Identification of a Potent D-Amino Acid Oxidase Inhibitor.

Toguchi S, Hirose T, Yorita K, Fukui K, Sharpless KB, Ōmura S, Sunazuka T.

Chem Pharm Bull (Tokyo). 2016 Jul 1;64(7):695-703. doi: 10.1248/cpb.c15-00867. Epub 2015 Dec 18.


A fluorogenic aryl fluorosulfate for intraorganellar transthyretin imaging in living cells and in Caenorhabditis elegans.

Baranczak A, Liu Y, Connelly S, Du WG, Greiner ER, Genereux JC, Wiseman RL, Eisele YS, Bradbury NC, Dong J, Noodleman L, Sharpless KB, Wilson IA, Encalada SE, Kelly JW.

J Am Chem Soc. 2015 Jun 17;137(23):7404-14. doi: 10.1021/jacs.5b03042. Epub 2015 Jun 8.


Palladium-catalyzed, ligand-free Suzuki reaction in water using aryl fluorosulfates.

Liang Q, Xing P, Huang Z, Dong J, Sharpless KB, Li X, Jiang B.

Org Lett. 2015 Apr 17;17(8):1942-5. doi: 10.1021/acs.orglett.5b00654. Epub 2015 Apr 9.


Tsutomu Katsuki (1946-2014).

Sharpless KB, Finn MG, Martín VS.

Angew Chem Int Ed Engl. 2015 Apr 13;54(16):4708. doi: 10.1002/anie.201501065. Epub 2015 Mar 12. No abstract available.


Sulfur(VI) fluoride exchange (SuFEx): another good reaction for click chemistry.

Dong J, Krasnova L, Finn MG, Sharpless KB.

Angew Chem Int Ed Engl. 2014 Sep 1;53(36):9430-48. doi: 10.1002/anie.201309399. Epub 2014 Aug 11.


SuFEx-based synthesis of polysulfates.

Dong J, Sharpless KB, Kwisnek L, Oakdale JS, Fokin VV.

Angew Chem Int Ed Engl. 2014 Sep 1;53(36):9466-9470. doi: 10.1002/anie.201403758. Epub 2014 Aug 5.


Imidazole aldoximes effective in assisting butyrylcholinesterase catalysis of organophosphate detoxification.

Sit RK, Fokin VV, Amitai G, Sharpless KB, Taylor P, Radić Z.

J Med Chem. 2014 Feb 27;57(4):1378-89. doi: 10.1021/jm401650z. Epub 2014 Feb 7.


Expanded therapeutic potential in activity space of next-generation 5-nitroimidazole antimicrobials with broad structural diversity.

Miyamoto Y, Kalisiak J, Korthals K, Lauwaet T, Cheung DY, Lozano R, Cobo ER, Upcroft P, Upcroft JA, Berg DE, Gillin FD, Fokin VV, Sharpless KB, Eckmann L.

Proc Natl Acad Sci U S A. 2013 Oct 22;110(43):17564-9. doi: 10.1073/pnas.1302664110. Epub 2013 Oct 7.


Observation of the controlled assembly of preclick components in the in situ click chemistry generation of a chitinase inhibitor.

Hirose T, Maita N, Gouda H, Koseki J, Yamamoto T, Sugawara A, Nakano H, Hirono S, Shiomi K, Watanabe T, Taniguchi H, Sharpless KB, Omura S, Sunazuka T.

Proc Natl Acad Sci U S A. 2013 Oct 1;110(40):15892-7. doi: 10.1073/pnas.1315049110. Epub 2013 Sep 16.


Automated docking with protein flexibility in the design of femtomolar "click chemistry" inhibitors of acetylcholinesterase.

Morris GM, Green LG, Radić Z, Taylor P, Sharpless KB, Olson AJ, Grynszpan F.

J Chem Inf Model. 2013 Apr 22;53(4):898-906. doi: 10.1021/ci300545a. Epub 2013 Mar 29.


Aromatic sulfonyl fluorides covalently kinetically stabilize transthyretin to prevent amyloidogenesis while affording a fluorescent conjugate.

Grimster NP, Connelly S, Baranczak A, Dong J, Krasnova LB, Sharpless KB, Powers ET, Wilson IA, Kelly JW.

J Am Chem Soc. 2013 Apr 17;135(15):5656-68. doi: 10.1021/ja311729d. Epub 2013 Feb 14.


Synthesis of selective agonists for the α7 nicotinic acetylcholine receptor with in situ click-chemistry on acetylcholine-binding protein templates.

Yamauchi JG, Gomez K, Grimster N, Dufouil M, Nemecz A, Fotsing JR, Ho KY, Talley TT, Sharpless KB, Fokin VV, Taylor P.

Mol Pharmacol. 2012 Oct;82(4):687-99. Epub 2012 Jul 11.


Generation of candidate ligands for nicotinic acetylcholine receptors via in situ click chemistry with a soluble acetylcholine binding protein template.

Grimster NP, Stump B, Fotsing JR, Weide T, Talley TT, Yamauchi JG, Nemecz Á, Kim C, Ho KY, Sharpless KB, Taylor P, Fokin VV.

J Am Chem Soc. 2012 Apr 18;134(15):6732-40. doi: 10.1021/ja3001858. Epub 2012 Apr 6.


Refinement of structural leads for centrally acting oxime reactivators of phosphylated cholinesterases.

Radić Z, Sit RK, Kovarik Z, Berend S, Garcia E, Zhang L, Amitai G, Green C, Radić B, Fokin VV, Sharpless KB, Taylor P.

J Biol Chem. 2012 Apr 6;287(15):11798-809. doi: 10.1074/jbc.M111.333732. Epub 2012 Feb 16. Erratum in: J Biol Chem. 2012 Jun 1;287(23):19337.


Iterative in situ click chemistry assembles a branched capture agent and allosteric inhibitor for Akt1.

Millward SW, Henning RK, Kwong GA, Pitram S, Agnew HD, Deyle KM, Nag A, Hein J, Lee SS, Lim J, Pfeilsticker JA, Sharpless KB, Heath JR.

J Am Chem Soc. 2011 Nov 16;133(45):18280-8. doi: 10.1021/ja2064389. Epub 2011 Oct 24.


Oxime-assisted acetylcholinesterase catalytic scavengers of organophosphates that resist aging.

Cochran R, Kalisiak J, Küçükkilinç T, Radic Z, Garcia E, Zhang L, Ho KY, Amitai G, Kovarik Z, Fokin VV, Sharpless KB, Taylor P.

J Biol Chem. 2011 Aug 26;286(34):29718-24. doi: 10.1074/jbc.M111.264739. Epub 2011 Jul 5.


New structural scaffolds for centrally acting oxime reactivators of phosphylated cholinesterases.

Sit RK, Radić Z, Gerardi V, Zhang L, Garcia E, Katalinić M, Amitai G, Kovarik Z, Fokin VV, Sharpless KB, Taylor P.

J Biol Chem. 2011 Jun 3;286(22):19422-30. doi: 10.1074/jbc.M111.230656. Epub 2011 Apr 4.


Antiviral stilbene 1,2-diamines prevent initiation of hepatitis C virus RNA replication at the outset of infection.

Gastaminza P, Pitram SM, Dreux M, Krasnova LB, Whitten-Bauer C, Dong J, Chung J, Fokin VV, Sharpless KB, Chisari FV.

J Virol. 2011 Jun;85(11):5513-23. doi: 10.1128/JVI.02116-10. Epub 2011 Mar 23.


NH-1,2,3-Triazole-based Inhibitors of the VIM-2 Metallo-β-Lactamase: Synthesis and Structure-Activity Studies.

Weide T, Saldanha SA, Minond D, Spicer TP, Fotsing JR, Spaargaren M, Frère JM, Bebrone C, Sharpless KB, Hodder PS, Fokin VV.

ACS Med Chem Lett. 2010 Jul 8;1(4):150-154.


Interaction kinetics of oximes with native, phosphylated and aged human acetylcholinesterase.

Radić Z, Kalisiak J, Fokin VV, Sharpless KB, Taylor P.

Chem Biol Interact. 2010 Sep 6;187(1-3):163-6. doi: 10.1016/j.cbi.2010.04.014. Epub 2010 Apr 20.



Kwok SW, Hein JE, Fokin VV, Sharpless KB.

Heterocycles. 2008 Nov 1;76(2):1141-1154.


Copper(I)-catalyzed cycloaddition of organic azides and 1-iodoalkynes.

Hein JE, Tripp JC, Krasnova LB, Sharpless KB, Fokin VV.

Angew Chem Int Ed Engl. 2009;48(43):8018-21. doi: 10.1002/anie.200903558. No abstract available.


A sulfilimine bond identified in collagen IV.

Vanacore R, Ham AJ, Voehler M, Sanders CR, Conrads TP, Veenstra TD, Sharpless KB, Dawson PE, Hudson BG.

Science. 2009 Sep 4;325(5945):1230-4. doi: 10.1126/science.1176811.

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