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27 results on '"Kong, Jongrock"'

3. A chemoenzymatic strategy for site-selective functionalization of native peptides and proteins

Author

Fryszkowska, Anna, primary, An, Chihui, additional, Alvizo, Oscar, additional, Banerjee, Goutami, additional, Canada, Keith A., additional, Cao, Yang, additional, DeMong, Duane, additional, Devine, Paul N., additional, Duan, Da, additional, Elgart, David M., additional, Farasat, Iman, additional, Gauthier, Donald R., additional, Guidry, Erin N., additional, Jia, Xiujuan, additional, Kong, Jongrock, additional, Kruse, Nikki, additional, Lexa, Katrina W., additional, Makarov, Alexey A., additional, Mann, Benjamin F., additional, Milczek, Erika M., additional, Mitchell, Vesna, additional, Nazor, Jovana, additional, Neri, Claudia, additional, Orr, Robert K., additional, Orth, Peter, additional, Phillips, Eric M., additional, Riggins, James N., additional, Schafer, Wes A., additional, Silverman, Steven M., additional, Strulson, Christopher A., additional, Subramanian, Nandhitha, additional, Voladri, Rama, additional, Yang, Hao, additional, Yang, Jie, additional, Yi, Xiang, additional, Zhang, Xiyun, additional, and Zhong, Wendy, additional

Published
2022
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5. Engineered Ribosyl-1-Kinase Enables Concise Synthesis of Molnupiravir, an Antiviral for COVID-19

Author

McIntosh, John A., primary, Benkovics, Tamas, additional, Silverman, Steven M., additional, Huffman, Mark A., additional, Kong, Jongrock, additional, Maligres, Peter E., additional, Itoh, Tetsuji, additional, Yang, Hao, additional, Verma, Deeptak, additional, Pan, Weilan, additional, Ho, Hsing-I, additional, Vroom, Jonathan, additional, Knight, Anders M., additional, Hurtak, Jessica A., additional, Klapars, Artis, additional, Fryszkowska, Anna, additional, Morris, William J., additional, Strotman, Neil A., additional, Murphy, Grant S., additional, Maloney, Kevin M., additional, and Fier, Patrick S., additional

Published
2021
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7. Evolving to an Ideal Synthesis of Molnupiravir, an Investigational Treatment for COVID-19

Author

Benkovics, Tamas, primary, McIntosh, John, additional, Silverman, Steven, additional, Kong, Jongrock, additional, Maligres, Peter, additional, Itoh, Tetsuji, additional, Yang, Hao, additional, Huffman, Mark, additional, Verma, Deeptak, additional, Pan, Weilan, additional, Ho, Hsing-I, additional, Vroom, Jonathan, additional, Knight, Anders, additional, Hurtak, Jessica, additional, Morris, William, additional, Strotman, Neil, additional, Murphy, Grant, additional, Maloney, Kevin, additional, and Fier, Patrick, additional

Published
2020
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9. Discovery of [11C]MK-6884: A Positron Emission Tomography (PET) Imaging Agent for the Study of M4Muscarinic Receptor Positive Allosteric Modulators (PAMs) in Neurodegenerative Diseases

Author

Tong, Ling, primary, Li, Wenping, additional, Lo, Michael Man-Chu, additional, Gao, Xiaolei, additional, Wai, Jenny Miu-Chen, additional, Rudd, Michael, additional, Tellers, David, additional, Joshi, Aniket, additional, Zeng, Zhizhen, additional, Miller, Patricia, additional, Salinas, Cristian, additional, Riffel, Kerry, additional, Haley, Hyking, additional, Purcell, Mona, additional, Holahan, Marie, additional, Gantert, Liza, additional, Schubert, Jeffrey W., additional, Jones, Kristen, additional, Mulhearn, James, additional, Egbertson, Melissa, additional, Meng, Zhaoyang, additional, Hanney, Barbara, additional, Gomez, Robert, additional, Harrison, Scott T., additional, McQuade, Paul, additional, Bueters, Tjerk, additional, Uslaner, Jason, additional, Morrow, John, additional, Thomson, Fiona, additional, Kong, Jongrock, additional, Liao, Jing, additional, Selyutin, Oleg, additional, Bao, Jianming, additional, Hastings, Nicholas B., additional, Agrawal, Sony, additional, Magliaro, Brian C., additional, Monsma, Frederick J., additional, Smith, Michelle D., additional, Risso, Stefania, additional, Hesk, David, additional, Hostetler, Eric, additional, and Mazzola, Robert, additional

Published
2020
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12. Enantioselective Synthesis of 4′-Ethynyl-2-fluoro-2′-deoxyadenosine (EFdA) via Enzymatic Desymmetrization

Author

McLaughlin, Mark, primary, Kong, Jongrock, additional, Belyk, Kevin M., additional, Chen, Billy, additional, Gibson, Andrew W., additional, Keen, Stephen P., additional, Lieberman, David R., additional, Milczek, Erika M., additional, Moore, Jeffrey C., additional, Murray, David, additional, Peng, Feng, additional, Qi, Ji, additional, Reamer, Robert A., additional, Song, Zhiguo J., additional, Tan, Lushi, additional, Wang, Lin, additional, and Williams, Michael J., additional

Published
2017
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21. TT DINUCLEOTIDES CONTAINING AN ISOXAZOLINE MOIETY: SYNTHESIS AND BINDING AFFINITY STUDY.

Author

Kong, JongRock, Kim, SangKook, Moon, ByungJo, Kim, SuJeong, and Kim, ByeangHyean

Subjects
*NUCLEOTIDES, *BIOSYNTHESIS, *NUCLEOTIDE sequence, *OLIGONUCLEOTIDES
Abstract

We have prepared four diastereomers of TT dinucleotides containing an isoxazoline moiety and four dodecanucleotides incorporating these TT dinucleotides in the middle of the DNA sequence. We also have determined the melting temperatures of these modified oligonucleotides (Tm values) by measuring change in UV absorbance. [ABSTRACT FROM AUTHOR]

Published
2001
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23. Rh-catalyzed reductive coupling under hydrogenation conditions and nucleophilic catalysis via phosphine conjugate addition

Author

Kong, Jongrock, 1972-

Abstract

At the threshold of the 21st centry, a new set of challenges is defined by the need to develop sustainable means of preparing chemical commodities demanded by society. Hence, such concepts as atom economy, step economy, and 'green chemistry' have become the requirements for the development of synthetic reactions. Hydrogenation is one of the most powerful catalytic methods which successfully satisfy the stated requirements of modern chemistry. Accordingly, catalytic hydrogenation has been tremendously utilized in industrial settings. The profound impact of hydrogenation portended a powerful approach to reductive carbon-carbon bond formation under hydrogenation conditions, resulting in the discovery of the Fischer-Tropsch process and hydroformylation. However, since this discovery, processes have restricted to the incorporation of a single carbon monoxide unit. Even though there are a few seminal contributions, systematic efforts toward the development of hydrogen-mediated carboncarbon bond forming processes beyond hydroformylation have been absent from the literature. In an exciting advance, the Krische group has shown that it is possible to reductively couple two or more organic molecules simply through their exposure to gaseous hydrogen in the presence of a metal catalyst. This finding has led to the development of a broad, new family of hydrogen-mediated C-C bond formation. Herein, related to hydrogen-mediated C-C bond formation, the overview of metal catalyzed intermolecular reductive coupling in the presence of reducing agents such as borane, silane, alane, metal, and hydrogen is presented. Chapter 2 describes systematic approaches to the development of hydrogen-mediated C-C bond formation and successful preliminary results achieved by our research group. Chapters 3 and 4 will describe the further extension of these hydrogen-mediated C-C bond formations including (1) hydrogen-mediated reductive couplings of conjugated alkynes with iminoacetates, (2) hydrogen-mediated reductive couplings of 1,3-enynes with [alpha]-ketoesters, and (3) hydrogen-mediated multicomponent reductive couplings. The development of catalytic systems for the nucleophilic activation of enones using phosphine catalysts has received attractive attention. Recently, an intramolecular variant of the Rauhut-Currier reaction was developed in our lab. To further extend nucleophilic phosphine catalysis, we have sought to develop new catalytic methodology via phosphine conjugate addition. Chapter 5 describes two new methodologies related to their area: (1) catalytic cycloallylation via nucleophilic phosphine catalysis and (2) allylic amination of Morita-Baylis-Hillman acetates.

Published
2007

24. Quantitation and characterization of serotype 6A activation for pneumococcal conjugate vaccine by cryo-EM and SEC methods.

Author

Lin, Mingxiang, Deng, James Z., Scapin, Giovanna, Yuan, Yue, Gomez-Llorente, Yacob, Tong, Weidong, Porambo, Richard, Kong, Jongrock, Ikemoto, Nori, Lancaster, Catherine, Kaelber, Jason, Winters, Michael, and Zhuang, Ping

Subjects
*GOLD nanoparticles, *GEL permeation chromatography, *POLYSACCHARIDES, *PNEUMOCOCCAL vaccines, *CARRIER proteins, *GLYCOLS
Abstract

Pneumococcal conjugate vaccines (PCV) typically consist of capsular polysaccharides from different S. pneumoniae serotypes which are covalently attached to carrier protein. A well-established process to manufacture PCV is through activating polysaccharide by oxidation of vicinal diols to aldehydes, followed by protein conjugation via reductive amination. Polysaccharide activation is a crucial step that affects vaccine product critical attributes including conjugate size and structure. Therefore, it is highly desired to have robust analytical methods to well characterize this activation process. In this study, using pneumococcal serotype 6A as the model, we present two complimentary analytical methods for characterization of activated polysaccharide. First, a size exclusion chromatography (SEC) method was developed for quantitative measurement of polysaccharide activation levels. This SEC method demonstrated good assay characteristics on accuracy, precision and linearity. Second, a gold nanoparticle labeled cryo-electron microscopy (Cryo-EM) technique was developed to visualize activation site distribution along polysaccharide chain and provide information on activation heterogeneity. These two complimentary methods can be utilized to control polysaccharide activation process and ensure consistent delivery of conjugate vaccine products. [ABSTRACT FROM AUTHOR]

Published
2024
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25. Discovery of [ 11 C]MK-6884: A Positron Emission Tomography (PET) Imaging Agent for the Study of M4Muscarinic Receptor Positive Allosteric Modulators (PAMs) in Neurodegenerative Diseases.

Author

Tong L, Li W, Lo MM, Gao X, Wai JM, Rudd M, Tellers D, Joshi A, Zeng Z, Miller P, Salinas C, Riffel K, Haley H, Purcell M, Holahan M, Gantert L, Schubert JW, Jones K, Mulhearn J, Egbertson M, Meng Z, Hanney B, Gomez R, Harrison ST, McQuade P, Bueters T, Uslaner J, Morrow J, Thomson F, Kong J, Liao J, Selyutin O, Bao J, Hastings NB, Agrawal S, Magliaro BC, Monsma FJ Jr, Smith MD, Risso S, Hesk D, Hostetler E, and Mazzola R

Subjects
Animals, CHO Cells, Carbon Radioisotopes chemistry, Carbon Radioisotopes pharmacology, Cricetulus, Humans, Macaca mulatta, Muscarinic Agonists chemistry, Neurodegenerative Diseases diagnostic imaging, Neurodegenerative Diseases drug therapy, Neurodegenerative Diseases metabolism, Positron-Emission Tomography, Pyridines chemistry, Receptor, Muscarinic M4 metabolism, Allosteric Regulation drug effects, Muscarinic Agonists pharmacology, Pyridines pharmacology, Receptor, Muscarinic M4 agonists
Abstract

The measurement of receptor occupancy (RO) using positron emission tomography (PET) has been instrumental in guiding discovery and development of CNS directed therapeutics. We and others have investigated muscarinic acetylcholine receptor 4 (M4) positive allosteric modulators (PAMs) for the treatment of symptoms associated with neuropsychiatric disorders. In this article, we describe the synthesis, in vitro, and in vivo characterization of a series of central pyridine-related M4 PAMs that can be conveniently radiolabeled with carbon-11 as PET tracers for the in vivo imaging of an allosteric binding site of the M4 receptor. We first demonstrated its feasibility by mapping the receptor distribution in mouse brain and confirming that a lead molecule 1 binds selectively to the receptor only in the presence of the orthosteric agonist carbachol. Through a competitive binding affinity assay and a number of physiochemical properties filters, several related compounds were identified as candidates for in vivo evaluation. These candidates were then radiolabeled with 11 C and studied in vivo in rhesus monkeys. This research eventually led to the discovery of the clinical radiotracer candidate [ 11 C]MK-6884.

Published
2020
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26. Direct C-H Carbamoylation of Nitrogen-Containing Heterocycles.

Author

Jouffroy M and Kong J

Abstract

Nucleophilic radical additions at innately electrophilic C(sp 2 ) centers are perfectly suited for the direct functionalization of heterocycles. Using bench stable and commercially available alkyl oxamate and oxamic acid derivatives in combination with photoredox catalysis, a direct carbamoylation of heterocycles yielding amide functionalized pharmacophores in a single step is reported. The reaction conditions reported are compatible with structurally complex heterocyclic substrates of pharmaceutical interest. Notably, derivatives containing functional groups incompatible with standard amidation reactions, such as carboxylic acids and unprotected amines, were found to be amenable to this reaction paradigm., (© 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.)

Published
2019
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27. Enantioselective alpha-arylation of aldehydes via organo-SOMO catalysis. An ortho-selective arylation reaction based on an open-shell pathway.

Author

Conrad JC, Kong J, Laforteza BN, and MacMillan DW

Subjects
Catalysis, Indolizines chemical synthesis, Indolizines chemistry, Stereoisomerism, Substrate Specificity, Aldehydes chemistry
Abstract

The intramolecular alpha-arylation of aldehydes has been accomplished using singly occupied molecular orbital (SOMO) catalysis. Selective oxidation of chiral enamines (formed by the condensation of an aldehyde and a secondary amine catalyst) leads to the formation of a 3pi-electron radical species. These chiral SOMO-activated radical cations undergo enantioselective reaction with an array of pendent electron-rich aromatics and heterocycles thus efficiently providing cyclic alpha-aryl aldehyde products (10 examples: > or = 70% yield and > or = 90% ee). In accordance with our radical mechanism, when there is a choice between arylation at the ortho or para position of anisole substrates, we find that arylation proceeds selectively at the ortho position.

Published
2009
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