Jaden Jun is Assistant Professor (Research), University of Pittsburgh, Pharmaceutical Sciences, School of Pharmacy, Pittsburgh, PA –Aug. 2018-Present
As an organic/medicinal chemist, my expertise, training, motivation, and leadership will lead the research project successfully. I have more than fifteen years organic synthetic and medicinal chemistry experience of with US government (NIH), large pharmaceutical industry (GSK), and academic research related to anti-cancer and HIV drugs. As an organic/medicinal synthetic scientist on serval different university- and NIH-funded grants, and I have been focused on innovative research in the field of applied novel drug discovery, particularly relating to oncology targets. In addition, I successfully lead the projects on different research topics, collaborated with other scientists and collaborators from different areas globally, and published several peer-reviewed papers from projects. The above experience has afforded outstanding skills in multi-step synthesis, small molecule design, problem-solving, and team building.
My major Research Focus
1. Development of small-molecule inhibitors for p62-multiple myeloma (MM)
2. Development of sultam moiety-based new allosteric modulators for CB2
3. CB2-kidney probes: Novel small molecule development for renal fibrosis
- PhD
Education & Training
[1] Jun, J. J.; Xie, X.-Q., Implementation of Diverse Synthetic and Strategic Approaches to Biologically Active Sulfamides. ChemistrySelect, 2021. 6, 430-469. https://doi.org/10.1002/slct.202004765
[2] Jun, J. J.; Xie, X.-Q., Design, and Synthesis of Potential Modulators Targeting p62-ZZ Domain. (Manuscript near completion, Experimental Section completed).
[3] Jun, J. J.; Duscharla, D.; Ummanni, R.; Hanson, P. R.; Malhotra, S. V. Investigation on the Anti-Cancer Activity of Symmetric and Unsymmetric Cyclic Sulfamides. ACS Med. Chem. Lett. 2021, 12, 202-210.
[4] Bian, Y.; Jun, J. J.; Cuyler, J.; Xie, X.-Q., Covalent allosteric modulation: An emerging strategy for GPCRs drug discovery. Eur. J. Med. Chem. 2020, 112690.
https://www.sciencedirect.com/science/article/abs/pii/S0223523420306620
[5] Bian, Y.; Jing, Y.; Wang, L.; Ma, S.; Jun, J. J.; Xie, X.-Q., Prediction of orthosteric and allosteric regulations on cannabinoid receptors using supervised machine learning classifiers. Molecular Pharmaceutics 2019, 16, 2605-2615. PMID:31013097. https://pubs.acs.org/doi/full/10.1021/acs.molpharmaceut.9b00182
[6] Bian, Y.; Jing, Y.; Wang, L.; Ma, S.; Jun, J. J.; Xie, X.-Q., Deep convolutional generative adversarial network (dcGAN) models for the de novo design of small molecules targeting cannabinoid receptors. Molecular Pharmaceutics 2019, 16, 4451-4460. PMID:31589460. https://pubs.acs.org/doi/10.1021/acs.molpharmaceut.9b00500
[7] Jun, J. H.; Kumar, V.; Dexheimer, T. S.; Gupta, S.; Wedlich, I.; Nguyen, T.; Nicholas, M.; Gussio, R.; Pommier, Y.; Malhotra, S. V. Synthesis, anti-cancer screening and tyrosyl-DNA phosphodiesterase 1 (Tdp1) inhibition activity of novel piperidinyl sulfamides. Eur. J. Pharm. Sci. 2018, 111, 337-348. https://doi.org/10.1016/j.ejps.2017.10.017
[8] Jun, J. H.; Hur, M. Y.; Jha, J. S.; Asad, N.; Samarakoon, T. Atkinson, T. R.; Hanson, P. R. β-Keto-Sultam Analogs of Tetramic Acids via Intramolecular Dieckmann-Type Condensation. (Manuscript near completion, Experimental Section completed).
[9] Jun, J. H.; Asad, N.; Cassity, A. J.; Windmon, N. M.; Jeon, K. O.; Diepenbrock, A. J.; Hanson. P. R. Synthesis of Exo-Vinyl Bicyclic Sultams via Pd-Catalyzed Intramolecular C-Vinylation of 1,2,3-Triazoles. (Manuscript near completion, Experimental Section completed).
[10] Jun, J. H.; Clay, C.; Jha, J. S.; Cassity, A. J.; Hanson, P. R. Novel Electrophilic Probes and Known Drugs: Synthesis, Development, and Reactivity Profiling Studies. (Manuscript in preparation).
[11] Jun, J. H.; Jay S. Jha, J. S.; Hanson, P. R. Synthesis of Cysteine-reactive Macrocyclic β-Keto-Vinyl Sultams: Methods to and Reactivity Profiling of Novel Macrocidin-like Tetramic Acid Analogs. (Manuscript in preparation).
[12] Jun, J. H.; Javed, S.; Ndi, C.; Hanson, P. R. (Joëlle Prunet Ed), Synthesis of P-, S-, Si-, B-, and Se-Heterocycles via Ring-Closing Metathesis. Book title: Synthesis of Heterocycles by Metathesis Reaction (Series title: Topics in Heterocyclic Chemistry), Springer, Berlin Heidelberg, 2016, pp 319–379.
https://link.springer.com/chapter/10.1007/7081_2015_162
[13] Sharma, G. V. M.; Ramesh, A.; Singh, A.; Srikanth, G.; Jayaram, V.; Duscharla, D.; Jun, J. H.; Ummanni, R.; Malhotra, S. V. Imidazole Derivatives Show Anticancer Potential by Inducing Apoptosis and Cellular Senescence. Med. Chem. Comm. 2014, 5, 1751–1760. https://doi.org/10.1039/C4MD00277F
[14] Duan, M.; Kazmierski, W. M.; Tallant, M.; Jun, J. H.; Edelstein, M.; Ferris, R.; Todd, D.; Wheelan, P.; Xiong, Z. Discovery of a Novel Series of Cyclic Urea as Potent CCR5 Antagonists. Bioorg. Med. Chem. Lett. 2011, 21, 6381–6385. https://doi.org/10.1016/j.bmcl.2011.08.096
[15] Hancock, C. N.; Stockwin, L. H.; Han B.; Divelbiss, R. D.; Jun, J. H.; Malhotra, S. V.; Hollingshead, M. G.; Newton, D. L. A Copper Chelate of Thiosemicarbazone NSC 689534 Induces Oxidative/ER Stress and Inhibits Tumor Growth in vitro and in vivo. Free Radic. Biol. Med. 2011, 50, 110–121. PMID: 20971185
https://doi.org/10.1016/j.freeradbiomed.2010.10.696
[16] Jeon, K. O.; Jun, J. H.; Yu, J. S.; Lee, C. K. Mass Spectroscopical Properties of Benzoyl Derivatives of Five-Membered Monoheterocycles and Determination of Aromaticity Indices. Bull. Korean Chem. Soc. 2004, 25, 1840–1844. https://doi.org/10.5012/bkcs.2004.25.12.1840
[17] Jun, J. H.; Dougherty, J. M.; Jimĕnez, M. D. S.; Hanson, P. R. New Strategies to Symmetric and Unsymmetric Cyclic Sulfamide Analogs of DMP 323; A “Sulfur Linchpin”/RCM Approach. Tetrahedron 2003, 59, 8901–8912. https://doi.org/10.1016/j.tet.2003.04.001
[18] Jeon, K. O.; Jun, J. H.; Yu, J. S.; Lee, C. K. Infrared and Nuclear Magnetic Resonance Properties of Benzoyl Derivatives of Five-Membered Monoheterocycles and Determination of Aromaticity Indices. J. Het. Chem. 2003, 40, 763–771. https://doi.org/10.1002/jhet.5570400504
[19] Lee, C. K.; Jun, J. H.; Yu, J. S. Synthesis and Nuclear Magnetic Resonance Spectroscopic Studies of 1-Arylpyrroles. J. Het. Chem. 2000, 37, 15–24. https://doi.org/10.1002/jhet.5570370104
[20] Lee, C. K.; Kim, E. J.; Jun, J. H. Determination of Relative Reactivities of Free Hydroxyl Groups in β-Cyclodextrin, Amylose, and Cellulose by Reductive-Cleavage Method. Bull. Korean Chem. Soc. 1999, 20, 1153–1158.
https://pdfs.semanticscholar.org/e421/69e1d0fdfb0d71bf9cce1df400043eff6…
[21] Ka, J.-W.; Jun, J. H.; Lee, C. K.; Lee, C.-H. Kinetic of Site Selective Deuterium Exchange in the Substituted Pyrroles and Synthesis of Partially Deuterated Porphyrins Therefrom. Bull. Korean Chem. Soc. 1998, 19, 488–491.
https://www.koreascience.or.kr/article/JAKO199813464469030.page
[22] Lee, C. K.; Jun, J. H.; Seo, Y. H. Transglycosylation of Permethylated Methyl D-Glycopyranosides in the Presence of Trimethylsilyl Trifluoromethanesulfonate. Bull. Korean Chem. Soc. 1998, 19, 1233–1238.
https://koreascience.kr/article/JAKO199813464468161.page
[23] Lee, C. K.; Kim, E. J.; Jun, J. H.; Yu, J. S. Mechanism of the Reductive Cleavage Reaction of Permethylated Methyl D-Glycopyranosides. Ann. RCNBMA 1997, 6, 93–100.
[2] Clay, C. D.; Jun, J. H.; Cassity, A. J.; Jha, J. S.; Hanson, P. R. Use of 19F NMR to Monitor Thiol Reactions of Sultams, Sulfonamides, and Known Drugs. 254th National Meeting of the American Chemical Society, Washington, DC, Aug 20-24, 2017, Poster ORGN-423.
[3] Cassity, A. J.; Jun, J. H.; Windmon, N.; Asad, N.; Diepenbrock, A.; Clay, C. D. Hanson P. R. Intramolecular C-H Functionalization for the Synthesis of Structurally Unique Triazole-Fused Vinyl Sultams. 254th National Meeting of the American Chemical Society, Washington, DC, Aug 20-24, 2017, Poster ORGN-139.
[4] Clay, C. D.; Jun, J. H.; Hanson, P. R. Synthesis of Novel Electrophilic Probes: Reactivity Profiling with Sultams, Sulfonamides, and Known Drugs. 51st Midwest Regional Meeting of the American Chemical Society, Manhattan, KS, United States, Oct 26-28, 2016, MWRM-376.
[5] Jun, J. H.; Cassity, A. J.; Jha, J. S.; Clay, C. D.; Hanson, P. R. Novel Electrophilic Probes: Synthesis, Development and Reactivity Profiling Studies. 51st Midwest Regional Meeting of the American Chemical Society, Manhattan, KS, United States, Oct 26-28, 2016, MWRM-373.
[6] Clay, C. D.; Jun, J. H.; Hanson, P. R. Synthesis of Novel Electrophilic Probes: Reactivity Profiling with Sultams, Sulfonamides and Known Drugs.51st Midwest Regional Meeting of the American Chemical Society, Manhattan, KS, United States, Oct 26-28, 2016, MWRM-376.
[7] Faisal, S.; Zang, Q.; Jun, J. H.; Maity, P.; Kearney, P. C.; Stoianova, D.; Hanson, P. R. High-Load, Hybrid ROMP Reagents: Development and Applications in Facilitated Synthetic Protocols. 51st Midwest Regional Meeting of the American Chemical Society, Manhattan, KS, United States, Oct 26-28, 2016, talk, MWRM-151.
[8] Jun, J. H.; Cassity, A. J.; Jha, J. S.; Loh, J.; Asad, N.; Samarakoon T.; Hanson, P. R. One-pot, Sequential Ring Opening and SNAr: From Aziridine to 10- and 11-Membered Benzo-Fused Sultams. 251th National Meeting of the American Chemical Society, San Diego, CA, Mar 13-17, 2016, Poster ORGN-769.
[9] Jun, J. H.; Hur, M. Y.; Atkinson, T.; Hanson, P. R. Novel Sultam Analogs of Tetramic Acid via Intramolecular Dieckmann Condensation.2015 Midwest Regional Meeting of American Chemical Society, St. Joseph, MO, Oct 21-24, 2015, Poster 237.
[10] Cassity, A. J.; Jun, J. H.; Asad, N.; Windmon, N.; Diepenbrock, A.; Hanson, P. R. Synthesis of Vinyl Sultams via Pd-Catalyzed Intramolecular C-Vinylation of Triazoles. 2015 Midwest Regional Meeting of American Chemical Society, St. Joseph, MO, Oct 21-24, 2015, Poster 240.
[11] Cassity, A. J.; Jun, J. H.; Asad, N.; Windmon, N.; Diepenbrock, A.; Hanson, P. R. Intramolecular C-Vinylation to Novel Triazole-Fused Vinyl Sultams. 53rd Annual MIKI Meeting-in-Miniature, Lawrence, KS, Apr 10-12, 2015, Poster 11.
[12] Jun, J. H.; Hur, M. Y.; Atkinson, T.; Hanson, P. R. An Efficient and Concise Synthesis of Novel β-Keto-Sultams: Tetramic Acid Analogs. 53rd Annual MIKI Meeting-in-Miniature, Lawrence, KS, Apr 10-12, 2015, Poster 35.
[13] Jun, J. H.; Hur, M. Y.; Atkinson, T.; Hanson, P. R. Synthesis of Novel β-Keto-Sultams: Tetramic Acid Analogs and Their Derivatives. 249th National Meeting of the American Chemical Society, Denver, CO, Mar 22-26, 2015, Poster ORGN-588.
[14] Cassity, A. J.; Jun, J. H.; Asad, N.; Windmon, N.; Diepenbrock, A.; Hanson, P. R. C-Arylation of Triazoles: Synthesis of Novel Vinyl Triazole-Fused Sultams. 249th National Meeting of the American Chemical Society, Denver, CO, Mar 22-26, 2015, Poster ORGN-530.
[15] Gumpena, R.; Marapaka, A.; Allanki, A. D.; Sijwali, P. S.; Addlagatta, A.; Jun, J. H.; Hanson, P. R.; Malhotra, S. V. Design and Synthesis of Piperidinyl Sulfamides Against Malarial Aminopeptidase N, with Micromolar Efficacy Against the Parasite. 247th National Meeting of the American Chemical Society, Dallas, TX, Mar 16-20, 2014, Poster MEDI-269.
[16] Jun, J. H.; Duscharla, D.; Ummanni, R.; Hanson, P. R.; Malhotra, S. V. Synthesis and Antitumor Activity of Piperidinyl Sulfamides. 247th National Meeting of the American Chemical Society, Dallas, TX, Mar 16-20, 2014, Poster MEDI-108.
[17] Addlagatta, A.; Gumpena, R.; Marapaka, A.; Allanki, A. D.; Jun, J. H.; Sijwali, P. S.; Malhotra, S. V. Study of Quinoxaline-Based New Compounds Against Aminopeptidase N, and Plasmodium Falciparum Malarial Parasite. 247th National Meeting of the American Chemical Society, Dallas, TX, Mar 16-20, 2014, Poster MEDI-65.
[18] Thakur, A.; Jun, J. H.; Velez, G.; Christian E.; Zayas, B.; Rawat, D.; Malhotra, S. V. Synthesis and Anticancer Activity of C5-Curcuminoids. 246th National Meeting of the American Chemical Society, Indianapolis, IN, Sep 8-12, 2013, Poster MEDI-105.
[19] Jun, J. H.; Hanson, P. R.; Ummanni, R.; Malhotra, S. V. Design, Synthesis, and In Vitro Cytotoxicity Evaluation of Seven-Membered Cyclic Sulfamides. 246th National Meeting of the American Chemical Society, Indianapolis, IN, Sep 8-12, 2013, Poster MEDI-134.
[20] Sharma, G. V.; Srikanth, G.; Ramesh, A.; Jayaram, V.; Singh, A.; Duscharla, D.; Ummanni, R.; Jun, J. H.; Malhotra, S. V. Synthesis and Investigation of the Anticancer Activity of Imidazole-Based New Compounds. 246th National Meeting of the American Chemical Society, Indianapolis, IN, Sep 8-12, 2013, Poster MEDI-104.
[21] Jun, J. H.; Malhotra, S. V. Application of Microwave Chemistry in the Etherification of Heterocyclic Compounds by Nucleophilic Aromatic Substitutions Reactions (SNAr). 242th National Meeting of the American Chemical Society, Denver, CO, Aug 28–Sep 1, 2011, Poster 117.
[22] Jun, J. H.; Dexheimer, T. S.; Weidlich, I. E.; Nicklaus, M. C.; Pommier, Y. Sulfamide Based Inhibitors of Tyrosyl-DNA Phosphodiesterase 1 (Tdp1). Fifteenth Annual Spring Research Festival at the National Cancer Institute, Frederick, MD, Apr 27-28, 2011, Poster DR5.
[23] Jun, J. H.; Dexheimer, T. S.; Weidlich, I. E.; Nicklaus, M. C.; Pommier, Y.; Malhotra, S. V. Sulfamide Based Inhibitors of Tyrosyl-DNA Phosphodiesterase 1 (Tdp1). 240th National Meeting of the American Chemical Society, Boston, MA, Aug 22–26, 2010; Poster 666.
[24] Malhotra, S. V.; Pommier, Y.; Jun, J. H.; Dexheimer, T. S.; Gupta, S. Newly Developed Piperidinyl Sulfamides as Tyrosyl-DNA Phosphodiesterase 1 (Tdp1) Inhibitors.238th National Meeting of the American Chemical Society, Washington, DC, Aug 16–20, 2009; Talk 538.
[25] Hancock C. N.; Stockwin L. H.; Han B.; Divelbiss R.; Jun, J. H.; Malhotra S. V.; Hollingshead M. G.; Newton D. L. The Novel Copper Thiosemicarbazone NSC 689534 Induces Oxidative and Endoplasmic Reticulum Stress and Inhibits Tumor Proliferation In Vitro and In Vivo. Thirteenth Annual Spring Research Festival at the National Cancer Institute at Frederick and Ft. MD, Apr 29–30, 2009.
[26] Jun, J. H.; Jimĕnez, M. D. S.; Dougherty, J. M.; Hanson, P. R. Synthetic Routes to Diverse S-Heterocyclic Libraries. 229th National Meeting of the American Chemical Society, San Diego, CA, Mar 13-17, 2005; Poster 206.
[27] Jimĕnez, M. D. S.; Dougherty, J. M.; Jun, J. H.; Hanson, P. R. Ring-Closing Metathesis Approaches to Sulfamides and Analogs. 40th Midwest Regional Meeting of the American Chemical Society, Joplin, MO, Oct 26-29, 2005; Poster 126.
[28] Jun, J. H.; Jimĕnez, M. D. S.; Hanson, P. R.; Evans J. Synthetic Routes to Diverse Cyclic Sulfamides. 39th Midwest Regional Meeting of the American Chemical Society, Manhattan, KS, Oct 20-22, 2004; Poster 115.
[29] Jun, J. H.; Jimĕnez, M. D. S.; Hanson, P. R. New Strategies to S-Heterocycles. 38th Midwest Regional Meeting of the American Chemical Society, Columbia, MO, Nov 5-7, 2003; Poster 255.
[30] Jun, J. H.; Dougherty, J. M.; Jimĕnez, M. D. S.; Hanson, P. R. New Strategies to Symmetric and Unsymmetric Cyclic Sulfamide Analogs of DMP 323; A “Sulfur Linchpin”/RCM Approach. 226th National Meeting of the American Chemical Society, New York, NY, Sep 7-11, 2003; Poster 451.
[31] Jun, J. H.; Dougherty, J. M.; Jimĕnez, M. D. S.; Hanson, P. R. A Sulfur Lynchpin/RCM Strategy to Novel S-Heterocycles. 37th Midwest Regional Meeting of the American Chemical Society, Lawrence, KS, Oct 23-25, 2002; Poster 230.
[32] Jun, J. H.; Lee, C. K. Synthesis of Methyl 6-Deoxy-6-(1-Pyrroly) Glucopyranosides. 1999 Agricultural Biotechnology Symposium, The College of Agriculture & Life Science, Seoul National University, Suwon, Nov 27, 1999.
[33] Jun, J. H.; Lee, E. C.; Lee, C. K. New Recyclable Catalyst for Reductive Cleavage of Glycoside Linkage. 84th Annual Meeting of the Korean Chemical Society, Sunchon National University, Sunchon, Oct 22-23, 1999.
[34] Jun, J. H.; Lee, C. K. Preparation of 3-(m- and p-Substituted) Benzoylpyrroles. 83th Annual Meeting of the Korean Chemical Society, Kyung Hee University, Seoul, Apr 23-24, 1999.
[35] Jun, J. H.; Lee, C. K. Synthesis of Permethylated Methyl 6-Deoxy-6-(1-Pyrrolyl) Glucopyranosides and Their NMR Studies. 1998 Agricultural Biotechnology Symposium, The College of Agriculture & Life Science, Seoul National University, Suwon, Nov 5, 1998.
[36] Jun, J. H.; Lee, C. K. Synthesis of Permethylated Methyl 6-Deoxy-6-(1-Pyrrolyl) Glucopyranosides and Their NMR Studies. 82th Annual Meeting of the Korean Chemical Society, Sun Moon University, Chung Nam, A-San City, Oct 23-24, 1998.
[37] Jun, J. H.; Lee, C. K. NMR Studies of 2-Benzoyl and 2-Benzylpyrroles. 81th Annual Meeting of the Korean Chemical Society, Ewha Womans University, Seoul, Apr 24-25, 1998.
[38] Ka, J.-W.; Jun, J. H.; Lee, C. K.; Lee, C.-H. Kinetic of Site Selective Deuterium Exchange of the Substituted Pyrroles and Their Application to the Synthesis of Partially Deuterated Porphyrins. 80th Annual Meeting of the Korean Chemical Society, Keimyung University, Taegu, Oct 24-25, 1997.
[39] Jun, J. H.; Yu, J. S.; Lee, C. K. An NMR Studies of Benzoylpyrroles and Benzoylthiophenes. 80th Annual Meeting of the Korean Chemical Society, Keimyung University, Taegu, Oct 24-25, 1997.
[40] Yu, J. S.; Jun, J. H.; Lee, C. K. NMR Studies of Permethylated D-Glucopyranosides. 80th Annual Meeting of the Korean Chemical Society, Keimyung University, Taegu, Oct 24-25, 1997.
[41] Jun, J. H.; Lee, C. K. Mechanism of Transglycosylation of Permethylted Methyl D-Glycopyranosides with Alkoxytrimethylsilane in the Presence of Trimethylsilyl Trifluoromethanesulfonate. 1997 Agricultural Biotechnology Symposium, The College of Agriculture & Life Science, Seoul National University, Suwon, Aug 27, 1997.
[42] Yu, J. S.; Jun, J. H.; Lee, C. K. An NMR Spectroscopic Study of the Pyrrole Series. 79th Annual Meeting of the Korean Chemical Society, Korea University, Seoul, Apr 25-26, 1997.
