个人简介

PROFESSIONAL EXPERIENCE 2022 – present Professor, Department of Chemistry, NC State University 2022 – present Director, Integrative Sciences Initiative, NC State University 2020 – present Co-Director, Comparative Medicine Institute, NC State University 2018 – 2022 Associate Professor, Department of Chemistry, NC State University 2018 – present Founder, President and CEO of Synoxa Sciences, Inc 2018 – 2020 Associate Director, Emerging and Infectious Diseases (CMI, NC State) 2018 – 2020 Leader, Natural Products to Drugs Initiative (CMI, NC State) 2016 – present Member, Executive Advisory Board (CMI, NC State) 2013 – present Member, Comparative Medicine Institute (CMI) (NC State) 2012 – 2018 Assistant Professor, Department of Chemistry, NC State University 2009 – 2011 The Scripps Research Institute, La Jolla, CA NIH NRSA Postdoctoral Fellow Worked as part of a team that developed an amidine analog of vancomycin that overcomes bacterial resistance. Mentor: Professor Dale L. Boger EDUCATION 2003 – 2008 University of Pittsburgh, Pittsburgh, PA Ph.D. in Organic Chemistry Developed several novel metal mediated reactions and applied them to the synthesis of biologically active molecules. Worked on the total synthesis of tuberostemonone. Advisor: Professor Peter Wipf 1999 – 2003 University of Pittsburgh, Pittsburgh, PA B.S. in Chemistry (Bioscience Option) with Honors Synthesized and demonstrated the efficacy of a chiral ligand for the addition of diethyl zinc to aldehydes. Advisor: Professor Peter Wipf

研究领域

Organic Chemistry

Natural Products Synthesis Natural products and their analogues have provided the basis for countless biologically important drugs or probe molecules and continue to provide unique opportunities for synthetic chemistry, medicinal chemistry and chemical biology to explore. We believe that innovative syntheses of newly discovered or historically significant natural products or natural product-like scaffolds will enable the development of novel biologically active agents for drug discovery and effective probes for biological study. During the course of this work our constant aim is to push forward the efficiency, scalability and novelty of complex molecule synthesis and provide ample materials for a variety of evaluations both internally and through collaborations with experts in biology and related fields. Target molecules include alkaloids, oxazolidinone heterocycles and peptide/polyketide hybrids. Methods Development The pursuit of complex molecules requires innovative approaches to new molecular scaffolds, improved routes to traditional motifs and asymmetric methods for complex stereocenter installation. In addition to the constant challenges posed en route to natural products we are focused on a number of methods, including novel approaches to heterocycles such as thiazolines and oxazolidinones, chemoselective C-H oxidation and C=O reduction, electrochemistry, and asymmetric amine and guanidine synthesis. Medicinal Chemistry, Chemical Biology and Drug Discovery Natural product medicinal chemistry and related chemical biology studies are a final aim for all projects that are undertaken in our lab. Targeted analogue synthesis aimed at simplified, potent compounds will enable the exploration of biological processes and activities that can potentially be further developed into chemical probes or therapeutic agents. In addition to in-vitro studies, many of which are conducted in our lab, we aim to collaborate with experts in the biological sciences to further advance the impact of our synthetic products. Major areas of focus include anti-bacterial and anti-fungal agents (infection), anti-tumor agents (cancer) and chemical probes to study protein-protein interactions and enzyme inhibition. Key interactions with NC State’s Comparative Medicine Institute enable many of our collaborative efforts which have now resulted in several commercialization opportunities.

近期论文

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Total Synthesis of Bipolamine I Qiu, X.; Pierce, J. G. J. Am. Chem. Soc. 2022, submitted. Tissue-Reactive Drugs Enable Materials-Free Local Depots Pandit, S.; Palvai, S. K.; Massaro, N.P.; Pierce, J. G.; Brudno, Y. J. Cont. Rel. 2022, 323, 142. Restoring Carboxylates on Highly Modified Alginates Improves Gelation, Tissue Retention and Systemic Capture. Moody, C.; Brown, A.; Massaro, N. P.; Patel, A.; Zheng, H.; Pierce, J.G.; Brudno, Y. Acta Biomaterialia 2022, 138, 208. Synthesis of the Spirocyclic g-Lactam Core of the Ansalactams. Liang, Z.; Lin, Y-C.; Pierce, J. G. Org. Lett. 2021, 23, 9559. Rapid Synthesis of the Core Scaffold of Crinane and Haemanthamine through a Multi-Component Approach. Massaro, N. P.; Pierce, J. G. Tetrahedron Lett. 2021, In Press. (Invited Submission in honor of Dale L. Boger’s Tetrahedron Prize for Creativity in Organic Chemistry) Leveraging Marine Natural Products as a Platform to Tackle Bacterial Resistance and Persistence. Valdes-Pena, M. A.; Massaro, N. P.; Lin Y. C.; Pierce, J. G. Acc. Chem. Res. 2021, 54, 1866. Design, synthesis, and evaluation of substrate – analogue inhibitors of Trypanosoma cruzi ribose 5-phosphate isomerase type B. Gonzalez, S. N; Mills, J. J.; Maugeri, D.; Olaya, C.; Laguera, B. L.; Enders, J. R.; Sherman, J.; Rodriguez, A.; Pierce, J. G.; Cazzulo, J. J.; D’Antonio, E. L. Bioorg. Med. Chem. Lett. 2021, 32, 127723. Stereoselective, Multicomponent Approach to Quaternary Substituted Hydroindole Scaffolds. Massaro, N. P.; Pierce, J. G. Org. Lett., 2020, 22, 5079. Genetic Determinants of Salmonella Resistance to the Anti-Biofilm Effects of a Synthetic 4-Oxazolidinone Analog. Griewisch, K. F.; Pierce, J. G.; Elfenbein, J. R. Appl. Environ. Microbiol. 2020, 86, e01120-20. Concise Synthesis and Antimicrobial Evaluation of the Guanidinium Alkaloid Batzelladine D: Development of a Stereodivergent Strategy. Lin, Y.-C.; Ribaucourt, A.; Moazami, Y.; Pierce, J. G. J. Am. Chem. Soc., 2020, 142, 9850. Stereocontrolled Synthesis of Melokhanine E via an Intramolecular Formal [3+2] Cycloaddition. Cholewczynski, A. E.; Williams, P. C.; Pierce, J. G. Org. Lett. 2020, 22, 714. ChemRxiv preprint: https://doi.org/10.26434/chemrxiv.10022858.v1 5-Benzylidene-4-Oxazolidinones are Synergistic with Antibiotics for the Treatment of Staphylococcus Aureus Biofilms. Frohock, B.; Gilbertie, J. M.; Daiker, J. C.; Schnabel, L. V.; Pierce, J. G. ChemBioChem, 2020, 21, 933. VIP Paper and Journal Cover. ChemRxiv Preprint: https://doi.org/10.26434/chemrxiv.9759302.v1 Expanded Structure-Activity Studies of Lipoxazolidinone Antibiotics. Robinson, K.; Mills, J. J.; Pierce, J. G. ACS Med. Chem. Lett., 2019, 10, 374. ChemRxiv preprint: https://doi.org/10.26434/chemrxiv.6103607.v1 Accidental intoxications in toddlers: lack of cross-reactivity of vilazodone and its urinary metabolite M17 with drug of abuse screening immunoassays. Martinez-Brokaw, C. D.; Radke, J. B.; Pierce, J. G.; Ehlers, A.; Ekins, S.; Wood, K. E.; Maakestad, J.; Rymer, J. A.; Tamama, K.; Krasowski, M. D. BMC Clin. Path. 2019, 19, 2. In Vitro Evaluation of a Novel Synthetic Bilirubin Analog as an Antioxidant and Cytoprotective Agent for Pancreatic Islet Transplantation. Luckring, E. J.; Parker, P. D.; Hani, H.; Grace, M. H.; Lila, M. A.; Pierce, J. G.; Adin, C. A. Cell Transplant 2020, 29, 1. Synthesis and Biological Activity of Lipoxazolidinone A. Mills, J. J.; Robinson, K.; Zehnder, T. E.; Pierce, J. G. Angew. Chem. Int. Ed. 2018, 130, 8818. 3-Hydroxy-1,5-dihydro-2H-pyrrol-2-ones as Novel Antibacterial Scaffolds Against Methicillin-Resistant Staphlyococcus aureus Cusumano, A. Q.; Pierce, J. G. Bioorg. Med. Chem. Lett. 2018, 28, 2732. (Invited Submission for issue in Honor of Dale L. Boger). Coupling of Thioamides with 4-Bromoacrotonate Esters and Subsequent Conjugate Addition for the Rapid One-Pot Synthesis of Functionalized Thiazolines. Parker, P. D.; Ge, Y.; Pierce, J. G. Tetrahedron Lett., 2018, 59, 277. Synthesis of Quaternary-Substituted Thiazolines via Halocyclization of S-Allyl Thioimidate Salts. Parker, P. D.; Lemercier, B. C.; Pierce, J. G. J. Org. Chem. 2018, 83, 12 (Featured Article & Front Cover). Mast cell degranulation and calcium influx are inhibited by an Echinacea purpurea extract and the alkylamide dodeca-2E,4E-dienoic acid isobutylamide. Gulledge, T. V.; Collette, N. M.; Moazami, Y.; Juzumaite, M.; Tong, S.; Mackey, E.; Moeser, A. J.; Pierce, J. G.; Cech, N. B.; Laster, S. M. J Ethnopharmacol. 2018, 212, 166.