2024
Al Subeh, Z.Y.; Pierre, H.C.; Bockbrader, R.H.; Tokarski, R.J. II; Maldonado, A.C.; Haughan, M.A.; Rangel Grimaldo, M.E.; Pearce, C.J.; Burdette, J.E.; Fuchs, J.R.*; Oberlies, N.H.* Semisynthetic Derivatives of the Fungal Metabolite Eupenifeldin via Targeting the Tropolone Hydroxy Groups. Bioorg. Med. Chem. Lett. 2024, accepted for publication 7/1/24. (*co-corresponding authors).
Pierre, H.C.; Amrine, C.S.M.; Doyle, M.G.; Salvi, A.; Raja, H.A.; Chekan, J.R.; Huntsman, A.C.; Fuchs, J.R.; Liu, K.; Burdette, J.E.; Pearce, C.J.; Oberlies, N.H. Verticillins: fungal epipolythiodioxopiperazine alkaloids with chemotherapeutic potential. Nat. Prod. Rep. 2024, Advance Article.
Dinh, T.; Tber, Z.; Rey, J.S.; Mengshetti, S.; Annamalai, A.S.; Haney, R.; Briganti, L.; Amblard, F.; Fuchs, J.R.; Cherepanov, P.; Kim, K.; Schinazi, R.F.; Perilla, J.R.; Kim, B.; Kvaratskhelia, M.
The structural and mechanistic bases for the viral resistance to allosteric HIV-1 integrase inhibitor pirmitegravir. bioRxiv 2024, doi: 10.1101/2024.01.26.577387. [Preprint]
Deblais, L.; Drozd, M.; Kumar, A.; Antwi, J.; Fuchs, J.; Khupse, R.; Helmy, Y.A.; Rajashekara, G. Identification of novel small molecule inhibitors of twin arginine translocation (Tat) pathway
and their effect on the control of Campylobacter jejuni in chickens. Front. Micorobiol. 2024, 15:1342573.
2023
Mukherjee, D.; Chakraborty, S.; Bercz, L.; D’Alesio, L.; Wedig, J.; Torok, M.A.; Pfau, T.; Lathrop, H.; Jasani, S.; Guenther, A.; McGue, J.; Adu-Ampratwum, D.; Fuchs, J.R.; Frankel, T.L.; Pietrzak, M.; Culp, S.; Strohecker, A.M.; Skardal, A.; Mace, T.A. Tomatidine targets ATF4-dependent signaling and induces ferroptosis to limit pancreatic cancer progression. iScience 2023, 26: 107408.
Ayinde, O.R.; Sharpe, C.; Stahl, E.; Tokarski, R.J. 2nd; Lerma, J.R.; Muthusamy, N.; Byrd, J.C.; Fuchs, J.R. Examination of the Impact of Triazole Position within Linkers on Solubility and Lipophilicity of a CDK9 Degrader Series. ACS Med. Chem. Lett. 2023, 14, 936-942.
Mize, B.K.; Salvi, A.; Ren, Y.; Burdette, J.E.; Fuchs, J.R. Discovery and development of botanical natural products and their analogues as therapeutics for ovarian cancer. Nat. Prod. Rep. 2023, 40, 1250-1270.
Chen, Z.; Ayinde, O.R.; Fuchs, J.R.; Sun, H.; Ning, X. G2Retro as a two-step graph generative models for retrosynthesis prediction. Commun. Chem. 2023, 6: 102.
Kaweesa, E.N.; Bazioli, J.M.; Pierre, H.C.; Lantvit, D.D.; Kulp, S.K.; Hill, K.L.; Phelps, M.A.; Coss, C.C.; Fuchs, J.R.; Pearce, C.J.; Oberlies, N.H.; Burdette, J.E. Exploration of Verticillins in High-Grade Serous Ovarian Cancer and Evaluation of Multiple Formulations in Preclinical In Vitro and In Vivo Models. Mol. Pharm. 2023, 20, 3049-3059.
Tokarski, R.J. 2nd; Sharpe, C.M.; Huntsman, A.C.; Mize, B.K.; Ayinde, O.R.; Stahl, E.H.; Lerma, J.R.; Reed, A.; Carmichael, B.; Muthusamy, N; Byrd, J.C.; Fuchs, J.R. Bifunctional degraders of cyclin dependent kinase 9 (CDK9): Probing the relationship between linker length, properties, and selective protein degradation. Eur. J. Med. Chem. 2023, 254: 115342.
Helmy, Y.A.; Kathayat, D.; Closs, G. Jr; Galgozy, K.; Fuchs, J.R.; Rajashekara, G. Efficacy of quorum sensing and growth inhibitors alone and in combination against avian pathogenic Escherichia coli infection in chickens. Poult. Sci. 2023, 102: 102543.
2022
Bester S.M.; Adu-Ampratwum, D.; Annamalai, A.S.; Wei, G.; Briganti, L.; Murphy, B.C.; Haney, R.; Fuchs, J.R.; Kvaratskhelia, M. Structural and Mechanistic Bases of Viral Resistance to HIV-1 Capsid Inhibitor Lenacapavir. mBio 2022, 13:e0180422.
Helmy, Y.A.; Kathayat, D.; Deblais, L.; Srivastava, V.; Closs, G. Jr; Tokarski, R.J. 2nd; Ayinde, O.; Fuchs, J.R.; Rajashekara, G. Evaluation of Novel Quorum Sensing Inhibitors Targeting Auto-Inducer 2 (AI-2) for the Control of Avian Pathogenic Escherichia coli Infections in Chickens Microbiol. Spectr. 2022, 10: e0028622.
Aldrich, L.N.; Burdette, J.E; Carcache de Blanco, E.; Coss, C.C.; Eustaquio, A.S.; Fuchs, J.R.; Kinghorn, A.D.; MacFarlane, A.; Mize, B.K.; Oberlies, N.H.; Orjala, J.; Pearce, C.J.; Phelps, M.A.; Rakotondraibe, L.H.; Ren, Y.; Soejarto, D.D.; Stockwell, B.R.; Yalowich, J.C.; Zhang, X. Discovery of Anticancer Agents of Diverse Natural Origin. J. Nat. Prod. 2022, 85, 702-719.
Adu-Ampratwum, D.; Pan, Y.; Koneru, P.C.; Antwi, J.; Hoyte, A.C.; Kessl, J.; Griffin, P.R.; Kvaratskhelia, M.; Fuchs, J.R.; Larue, R.C. Identification and Optimization of a Novel HIV-1 Integrase Inhibitor. ACS Omega 2022, 7, 4482-4491.
Salvi, A.; Young, A.N.; Huntsman, A.C.; Pergande, M.R.; Korkmaz, M.A.; Rathnayake, R.A.; Mize, B.K.; Kinghorn, A.D.; Zhang, X.; Ratia, K.; Schirle, M.; Thomas, J.R.; Brittain, S.M.; Shelton, C.; Aldrich, L.N.; Cologna, S.M.; Fuchs, J.R.; Burdette, J.E. PHY34 inhibits autophagy through V-ATPase V0A2 subunit inhibition and CAS/CSE1L nuclear cargo trafficking in high grade serous ovarian cancer. Cell Death Dis. 2022, 13: 45.
Varikuti, S.; Shelton, A.B.; Kotha, S.R.; Gurney, T.; Gupta, G.; Hund, T.J.; Fuchs, J.R.; Kinghorn, A.D.; Srivastava, N.; Satoskar, A.R.; Parinandi, N.L. Pentalinonsterol, a Phytosterol from Pentalinon andrieuxii, is Immunomodulatory through Phospholipase A2 in Macrophages toward its Antileishmanial Action. Cell Biochem. Biophys. 2022, 80, 45-61.
2021
Amrine, C.S.M.; Huntsman, A.C.; Doyle, M.G.; Burdette, J.E.; Pearce, C.J.; Fuchs, J.R.*; Oberlies, N.H.* Semisynthetic derivatives of the verticillin class of natural products through acylation of the C11 hydroxyl group. ACS Med. Chem. Lett. 2021, 12, 625-630. (*co-corresponding authors).
2020
Zhang, Y.; Tan, C.Y.; Spjut, R.W.; Fuchs, J.R.; Kinghorn, A.D.; Rakotondraibe, L.H. Specialized metabolites of the United States lichen Niebla homalea and their antiproliferative activities. Phytochemistry 2020, 180, 112521.
Bester, S.M.; Wei, G.; Zhao, H.; Adu-Ampratwum, D.; Iqbal, N.; Courouble, V.V.; Francis, A.C.; Annamalai, A.S.; Singh, P.K.; Shkriabai, N.; Van Blerkom, P.; Morrison, J.; Poeschla, E.M.; Engelman, A.N.; Melikyan, G.B.; Griffin, P.R.; Fuchs, J.R.; Asturias, F.J.; Kvaratskhelia, M. Structural and mechanistic bases for a potent HIV-1 capsid inhibitor. Science 2020, 370, 360-364.
May, D.S.; Crnkovic, C.M.; Krunic, A.; Wilson, T.A.; Fuchs, J.R.; Orjala, J.E. 15N Stable Isotope Labeling and Comparative Metabolomics Facilitates Genome Mining in Cultured Cyanobacteria. ACS Chem. Biol. 2020, 15, 758-765.
2019
Fosu, S.C.; Hambira, C.M.; Chen, A.D.; Fuchs, J.R.; Nagib, D.A. Site-selective C-H functionalization of (hetero)arenes via transient, non-symmetric iodanes. Chem – Cell Press, 2019, 5, 417-428.
Wilson, T.A.; Koneru, P.C.; Rebensburg, S.V.; Lindenberger, J.J.; Kobe, M.J.; Cockroft, N.T.; Adu-Ampratwum, D.; Larue, R.C.; Kvaratskhelia, M.; Fuchs, J.R. An isoquinoline scaffold as a novel class of allosteric HIV-1 integrase inhibitors. ACS Med. Chem. Lett. 2019, 10, 215-220.
Ren, Y.; Carcache de Blanco, E.J.; Fuchs, J.R.; Soejarto, D.D.; Burdette, J.E.; Swanson, S.M.; Kinghorn, A.D. Potential anticancer agents characterized from selected tropical plants. J. Nat. Prod. 2019, 82, 657-679.
Aqel, S.I.; Kraus, E.E.; Jena, N.; Kumari, V.; Granitto, M.C.; Mao, L.; Farinas, M.F.; Zhao, E.Y.; Perottino, G.; Pei, W.; Lovett-Racke, A.E.; Racke, M.K.; Fuchs, J.R.; Li, C.; Yang, Y. Novel small molecule IL-6 inhibitor suppresses autoreactive Th17 development and promotes Treg development. Clinical & Experimental Immunology 2019, 196, 215-225.
Deblais, L.; Helmy, Y.A.; Kumar, A.; Antwi, J.; Kathayat, D.; Acuna, U.M.; Huang, H.C.; Carcache de Blanco, E.J.; Fuchs, J.R.; Rajashekara, G. Novel narrow spectrum benzyl thiophene sulfonamide derivatives to control Campylobacter. J. Antibiot. 2019, 72, 555-565.
Koneru, P.C.; Francis, A.C.; Deng, N.; Rebensburg, S.V.; Hoyte, A.C.; Lindenberger, J.; Adu-Ampratwum, D.; Larue, R.C.; Wempe, M.F.; Engelman, A.N.; Lyumkis, D.; Fuchs, J.R.; Levy, R.M.; Melikyan, G.B.; Kvaratskhelia, M. HIV-1 integrase tetramers are the antiviral target of pyridine-based allosteric integrase inhibitors. eLife 2019, 8:e46344.
Zahid, M.S.H.; Johnson, M.M.; Tokarski II, R.J.; Satoskar, A.R.; Fuchs, J.R.; Bachelder, E.M.; Ainslie, K.M. Evaluation of synergy between host and pathogen-directed therapies against intracellular Leishmania donovani. IJP: Drugs and Drug Resistance 2019, 10, 125-132.
Cockroft, N.T.; Cheng, X.; Fuchs, J.R. STarFish: A stacked ensemble target fishing approach and its application to natural products. J. Chem. Inf. Model. 2019, 59, 4906-4920.
2018
Wilson, T.A.; Tokarski, R.J.; Sullivan, P.; Demoret, R.M.; Orjala, J.; Rakotondraibe, L.H.; Fuchs, J.R. Total Synthesis of Scytonemide A Employing Weinreb AM Solid-Phase Resin. J. Nat. Prod. 2018, 81 (3), 534-542.
Woodard, J.L.; Huntsman, A.C.; Patel, P.A.; Chai, H.B.; Kanagasabai, R.; Karmahapatra, S.; Young, A.N.; Ren, Y.; Cole, M.S.; Herrera, D.; Yalowich, J.C.; Kinghorn, A.D.; Burdette, J.E.; Fuchs, J.R. Synthesis and antiproliferative activity of derivatives of the phyllanthusmin class of arylnaphthalene lignan lactones. Bioorg. Med. Chem. 2018, 26 (9), 2354-2364.
Young, A.N.; Herrera, D.; Huntsman, A.C.; Korkmaz, M.A.; Lantvit, D.D.; Mazumder, S.; Kolli, S.; Coss, C.C.; King, S.; Wang, H.; Swanson, S.M.; Kinghorn, A.D.; Zhang, X.; Phelps, M.A.; Aldrich, L.N.; Fuchs, J.R.; Burdette, J.E. Phyllanthusmin derivatives induce apoptosis and reduce tumor burden in high grade serous ovarian cancer by late-stage autophagy inhibition. Mol. Cancer Ther. 2018, 17, 2123-2135.
Crnkovic, C.M.; Krunic, A.; May, D.S.; Wilson, T.A.; Kao, D.; Burdette, J.E.; Fuchs, J.R.; Oberlies, N.H.; Orjala, J. Calthrixamides A and B from the cultured cyanobacterium Calothrix sp. UIC 10520. J. Nat. Prod. 2018, 81,2083-2090.
Moshiri, J.; Kaur, D.; Hambira, C.M.; Sandala, J.L.; Koopman, J.A.; Fuchs, J.R.; Gunn, J.S. Identification of a small molecule anti-biofilm agent against Salmonella enterica. Front. Microbiol. 2018, 9, 2804.
2017
Oghumu, S.; Varikuti, S.; Saljoughian, N.; Terrazas, C.; Huntsman, A.C.; Parinandi, N.L.; Fuchs, J.R.; Kinghorn, A.D.; Satoskar, A.R. Pentalinonsterol, a Constituent of Pentalinon andrieuxii, Possesses Potent Immunomodulatory Activity and Primes T Cell Immune Responses. J. Nat. Prod. 2017, 80 (9), 2515-2523.
Hoyte, A.C.; Jamin, A.V.; Koneru, P.C.; Kobe, M.J.; Larue, R.C.; Fuchs, J.R.; Engelman, A.N.; Kvaratskhelia, M. Resistance to pyridine-based inhibitor KF116 reveals an unexpected role of integrase in HIV-1 Gag-Pol polyprotein proteolytic processing. J. Biol. Chem. 2017, 292 (48), 19814-19825.
Wan, Z.; Rajashekara, G.; Fuchs, J.; Carcache de Blanco, E.; Pascall, M.A. (2017). Incorporation of selected antimicrobial small molecule compounds into Tapioca starch and the effects on thickness, moisture and oxygen mass transfer, and mechanical properties of the films. STARCH-STARKE, 70 (5-6), 1700060-1700060.
2016
Wu, J.; Keng, V.W.; Patmore, D.M.; Kendall, J.J.; Patel, A.V.; Jousma, E.: Jessen, W.J.; Choi, K.; Tschida, B.R.; Silverstein, K.A.; Fan, D.; Schwartz, E.B.; Fuchs, J.R.; Zou, Y.; Kim, M.O.; Dombi, E.; Levy, D.E.; Huang, G.; Cancelas, J.A.; Stemmer-Rachamimov, A.O.; Spinner, R.J.; Largaespada, D.A.; Ratner, N. Insertional mutagenesis identifies a STAT3/Arid1b/B-catenin pathway driving neurofiboma initiation. Cell Rep. 2016, 14(8): 1979-90.
Wu, X.; Tang, W.; Marquez, R.T.; Li, K.; Highfill, C.A.; He, F.; Lian, J.; Lin, J.; Fuchs, J.R.; Ji, M.; Li, L.; Xu, L. Overcoming chemo/radio-resistance of pancreatic cancer by inhibiting STAT3 signaling. Oncotarget 2016, 7(10): 11708-23.
Kumar, A.; Drozd, M.; Pina-Mimbela, R.; Xu, X.; Helmy, Y.A.; Antwi, J.; Fuchs, J.R.; Nislow, C.; Templeton, J.; Blackall, P.J.; Rajashekara, G. Novel anti-campylobacter compounds identified using high throughput screening of a pre-selected enriched small molecules library. Front. Microbiol. 2016, 7:405, 2016.
Feng, L.; Dharmarajan, V.; Serrao, E.; Hoyte, A.; Larue, R.C.; Slaughter, A.; Sharma, A.; Plumb, M.R.; Kessl, J.J.; Fuchs, J.R.; Bushman, F.D.; Engelman, A.N.; Griffin, P.R.; Kvaratskhelia, M. The competitive interplay between allosteric HIV-1 integrase inhibitor BI/D and LEDGF/p75 during the early stage of HIV-1 replication adversely affects inhibitor potency. ACS Chem. Biol. 2016, 11 (5), 1313-1321.
Kessl, J.J.; Kutluay, S.B.; Townsend, D.; Rebensburg, S.; Slaughter, A.; Larue, R.C.; Shkriabai, N.; Bakouche, N.; Fuchs, J.R.; Bieniasz, P.D.; Kvaratskhelia, M. HIV-1 integrase binds the viral RNA genome and is essential during virion morphogenesis. Cell 2016, 166(5), 1257-1268.
Patel, P.A.; Kvaratskhelia, N.; Mansour, Y.; Antwi, J.; Feng, L.; Koneru, P.; Kobe, M.J.; Jena, N.; Shi, G,; Mohamed, M.S.; Li, C.; Kessl, J.J.; Fuchs, J.R. Indole-based allosteric inhibitors of HIV-1 integrase. Bioorg. Med. Chem. Lett. 2016, 26(19), 4748-4752.
Kinghorn, A.D.; Carcache de Blanco, E.J.; Lucas, D.M.; Rakotondraibe, H.L.; Orjala, J.; Soejarto, D.D.; Oberlies, N.H.; Pearce, C.J.; Wani, M.C.; Stockwell, B.R.; Burdette, J.E.; Swanson, S.M.; Fuchs, J.R.; Phelps, M.A.; Xu, L.; Zhang, X.; Shen, Y.Y. Discovery of anticancer agents of diverse natural origin. Anticancer Res. 2016, 36(11), 5623-5637.
Deng, N.; Hoyte, A.; Mansour, Y.E.; Mohamed, M.S.; Fuchs, J.R.; Engelman, A.N.; Kvaratskhelia, M.; Levy, R. Allosteric HIV-1 integrase inhibitors promote aberrant protein multimerization by directly mediating inter-subunit interactions: Structural and thermodynamic modeling studies. Protein Science 2016, 25 (11), 1911-1917.
Patel, D.; Antwi, J.; Koneru, P.C.; Serrao, E.; Forli, S.; Kessl, J.J.; Feng, L.; Deng, N.; Levy, R.M.; Fuchs, J.R.; Olson, A.J.; Engelman, A.N.; Bauman, J.D.; Kvaratskhelia, M.; Arnold, E. A new class of allosteric HIV-1 integrase inhibitors identified by crystallographic fragment screening of the catalytic core domain. J. Biol. Chem. 2016, 291(45), 23569-23577.
Agharbaoui, F.E.; Hoyte, A.C.; Ferro, S.; Gitto, R.; Buemi, M.R.; Fuchs, J.R.; Kvaratskhelia, M.; De Luca, L. Computational and synthetic approaches for developing Lavendustin B derivatives as allosteric inhibitors of HIV-1 integrase. Eur. J. Med. Chem. 2016, 123, 673-683.
Lin, L.; Jou, D.; Wang, Y.; Ma, H.; Liu, T.; Fuchs, J.; Li, P.-K.; Lu, J.; Li, C.; Lin, J. STAT3 as a potential therapeutic target in ALDH+ and CD44+/CD24+ stem cell-like pancreatic cancer cells. Int. J. Oncol. 2016, 49(6), 2265-2274.
2015
Ren, Y.; Yuan, C.; Deng, Y.; Kanagasabai, R.; Ninh, T.N.; Tu, V.T.; Chai, H.B.; Soejarto, D.D.; Fuchs, J.R.; Yalowich, J.C.; Yu, J.; Kinghorn, A.D. Cytotoxic and natural killer cell stimulatory constituents of Phyllanthus songboiensis. Phytochemistry 2015, 111, 132-140.
Yan, J.; Wang, Q.; Zou, K.; Wnag, L.; Schwartz, E.B.; Fuchs, J.R.; Zheng, Z.; Wu, J. Inhibition of the JAK2/STAT3 signaling pathway exerts a therapeutic effect on osteosarcoma. Mol. Med. Rep. 2015, 12, 498-502.
Luo, S.; Kang, H.S.; Krunic, A.; Chen, W.L.; Yang, J.; Woodard, J.L.; Fuchs, J.R.; Cho, H.S.; Franzblau, S.G.; Swanson, S.M.; Orjala, J. Trichormamides C and D, antiproliferative cyclic lipopeptides from the cultured freshwater cyanobacterium cf. Oscillatoria sp. UIC 10045. Bioorg. Med. Chem. 2015, 23, 3153-3162.
Haque, A.; Rahman, M.A.; Fuchs, J.R.; Chen, Z.G.; Khuri, F.R.; Shin, D.M.; Amin, A.R. FLLL12 induces apoptosis in lung cancer cells through a p53/p73-independent but death receptor 5-dependetn pathway. Cancer Lett. 2015, 363, 166-175.
Fontana, J.: Jurado, K.A.; Cheng, N.; Ly, N.L.; Fuchs, J.R.; Gorelick, R.J.; Engelman, A.N.; Steven, A.C. Distribution and redistribution of HIV-1 nucleocapsid protein in immature, mature, and integrase-inhibited virions: a role for integrase in maturation. J. Virol. 2015, 89, 9765-9780.
Gupta, G.; Peine, K.J.; Abdelhamid, D.; Snider, H.; Shelton, A.B.; Rao, L.; Kotha, S.R.; Huntsman, A.C.; Varikuti, S.; Oghumu, S.; Naman, C.B.; Pan, L.; Parinandi, N.L.; Papenfuss, T.L.; Kinghorn, A.D.; Bachelder, E.M.; Ainslie, K.M.; Fuchs, J.R.; Satoskar, A.R. A novel sterol isolated from a plant used by Mayan traditional healers is effective in treatment of visceral leishmaniasis caused by Leishmania donovani. ACS Infect. Dis. 2015, 1 (10): 497-506.
Xu, X.; Kumar, A.; Deblais, L.; Pina-Mimbela, R.; Nislow, C.; Fuchs, J.R.; Miller, S.A.; Rajashekara, G. Discovery of novel small molecule modulators of Clavibacter michiganensis subsp. michiganensis. Front. Microbiol. 2015, 6, 1127.
Anisuzzaman, A.; Haque, A.; Rahman, M.A.; Wang, D.; Fuchs, J.R.; Hurwitz, S.J.; Liu, Y.; Sica, G.L.; Khuri, F.R.; Chen, Z.G.; Shin, D.M.; Amin, A.R. Preclinical in vitro, in vivo and pharmacokinetic evaluations of FLLL12 for the prevention and treatment of head and neck cancers. Cancer Prev. Res. 2015, 9 (1), 63-73.