De Brabander JK, Dong X, Liang Q, Pan Y-Z, Wang X, Kuo Y-C, Chiang W-C, Zhang X, Williams N, Rizo J, Levine B (2022) Novel Bcl-2 Inhibitors Selectively Disrupt the Autophagy-Specific Bcl-2⎯Beclin 1 Protein⎯Protein Interaction. ACS Chem. Biol. ; https://doi.org/10.1021/acsmedchemlett.2c00309
Povedano JM, Li V, Lake KE, Bai X, Rallabandi R, Kim J, Xie Y, De Brabander JK, McFadden DG (2022) TK216 targets microtubules in Ewing sarcoma cells. Cell Chem. Biol., 29, 1325-1332; https://doi.org/10.1016/j.chembiol.2022.06.002; PMID: 35803262; PMC939468
Yin J, Kang Y, McGrath A, Chapman K, Sjodt M, Kimura E, Okabe A, Koike T, Miyanohana Y, Shimizu Y, Rallabandi R, Lian P, Bai X, Flinspach M, De Brabander JK, Rosenbaum DM (2022) Molecular mechanism of the wake-promoting agent TAK-925. Nature Commun. 13, Article number: 2902. https://doi.org/10.1038/S41467-022-30601-3; PMID: 35614071; PMC9133036
Hollibaugh R, Yu X, De Brabander JK (2020) A convergent approach toward fidaxomicin: Synthesis of the fully glycosylated northern and southern fragments. Tetrahedron, 76, 131673; https://doi.org/10.1016/j.tet.2020.131673; PMID: 33191957; PMC7665079
Povedano JM, Rallabandi R, Bai X, Ye X, Liou J, Chen H, Kim J, Xie Y, Posner B, Rice B, De Brabander JK, McFadden DG (2020) A Multipronged Approach Establishes Covalent Modification of b-Tubulin as the Mode of Action of Benzamide Anti-Cancer Toxins. Med. Chem., 63, 14054-14066; https://doi.org/10.1021/acs.jmedchem.0c01482; PMID: 33180487; PMC7707623
Jung H, Takeshima T, Nakagawa T, MacMillan KS, Wynn RM, Wang H, Sakiyama H, Wei S, Li Y, Bruick RK, Posner BA, De Brabander JK, Uyeda K (2020) The Structure of Importin α and the nuclear localization peptide of ChREBP, and small compound inhibitors of ChREBP-Importin α interactions. J., 477, 3253-3269; https://doi.org/10.1042/BCJ20200520; PMID: 32776146; PMC7489895
Theodoropoulos PC, Wang W, Budhipramono A, Thompson B; Madhusudhan N, Mitsche MA, McDonald JG; De Brabander JK, Nijhawan D (2020) A Medicinal Chemistry-Driven Approach Identified the Sterol Isomerase EBP as the Molecular Target of TASIN Colorectal Cancer Toxins. Am. Chem. Soc., 142, 6128-6138; https://doi.org/10.1021/jacs.9b13407; PMID: 32163279; PMC7236545
Long T, Qi X, Hassan A, Liang Q, De Brabander JK, Li X (2020) Structural basis for itraconazole-mediated NPC1 inhibition. Commun. 11:151; https://doi.org/10.1038/s41467-019-13917-5; PMCID: PMC6952396
Wang W, Zhang L, Morlock L, Williams NS, Shay JW, De Brabander JK (2019) Design and Synthesis of TASIN Analogs Specifically Targeting Colorectal Cancer Cell Lines with Mutant Adenomatous Polyposis Coli (APC). Med. Chem., 62, 5217-5241; https://doi.org/10.1021/acs.jmedchem.9b00532; PMID: 31070915; PMC725524
Gong J, Li W, Fu P, MacMillan J, De Brabander JK (2019) Isolation, Structure, and Total Synthesis of the Marine Macrolide Mangrolide D. Lett., 21, 2957-2961; https://doi.org/10.1021/acs.orglett.9b01126; PMID: 30957503; PMC6526702
Shi Y, Lim SK, Liang Q, Iyer SV, Wang H-Y, Wang Z, Xie X, Chen Y-J, Tabar V, Gutin P, Williams N, De Brabander JK, Parada LF (2019) Vulnerability of glioma to a novel proton gradient dependent oxidative phosphorylation inhibitor. Nature, 567, 341-346; https://doi.org/10.1038/s41586-019-0993-x; PMID: 30842654
Bender CF, Paradise CL, Lynch VM, Yoshimoto FK, De Brabander JK (2018) A biosynthetically inspired synthesis of (–)-berkelic acid and analogs. Tetrahedron, 74, 909-919; https://doi.org/10.1016/j.tet.2018.01.021; (Tetrahedron Symposium-in-Print: “Biogenetic Considerations in Complex Synthesis”). PMID: 29867257. PMCID: PMC5983035
Bulanova D, Ianevski A, Bugai A, Akimov Y, Kuivanen S, Paavilainen H, Kakkola L, Nandania J, Turunen L, Ohman T, Ala-Hongisto H, Pesonen HM, Kuisma MS, Honkimaa A, Walton EL, Oksenych V, Lorey MB, Guschin D, Shim J, Kim J, Than TT, Chang SY, Hukkanen V, Kulesskiy E, Marjomaki VS, Julkunen I, Nyman TA, Matikainen S, Saarela JS, Sane F, Hober D, Gabriel G, De Brabander JK, Martikainen M, Windisch MP, Min J-Y, Aittokallio T, Bruzzone R, Vähä-Koskela M, Vapalahti O, Pulk A, Velagapudi V, Kainov DE (2017) Antiviral Properties of Chemical Inhibitors of Cellular Anti-Apoptotic Bcl-2 Proteins. Viruses, 9, 271; https://doi.org/10.3390/v9100271; PMCID: PMC5691623
Brockway AJ, Volkov OA, Cosner CC, MacMillan KS, Wring SA, Richardson TE, Peel M, Phillips MA, De Brabander JK (2017) Synthesis and evaluation of analogs of 5'-(((Z)-4-amino-2-butenyl)methylamino)-5'-deoxyadenosine (MDL 73811, or AbeAdo) – an inhibitor of S-adenosylmethionine decarboxylase with antitrypanosomal activity. Med. Chem. 25, 5433-5440; http://dx.doi.org/10.1016/j.bmc.2017.07.063; PMID: 28807574. PMCID: PMC5632197
Deng Y, Wang ZV, Gordillo R, An Y, Zhang C, Liang Q, Yoshino J, Cautivo KM, De Brabander J, Elmquist JK, Horton JD, Hill JA, Klein S, Schrerer PE (2017) An Adipo-Biliary-Uridine Axis that Regulates Energy Homeostasis. Science, 355 (6330), eaaf5375; https://doi.org/10.1126/science.aaf5375; PMID: 28302796
Kuivanen S, Bespalov MM, Nandania J, Ianevsky A, Velagapudi V, De Brabander JK, Kainov DE, Vapalahti O (2017) Obatoclax, saliphenylhalamide and gemcitabine inhibit Zika virus infection in vitro and differentially affect cellular signaling, transcription and metabolism; Antiviral Res. 139, 117-128; https://doi.org/10.1016/j.antiviral.2016.12.022; PMID: 28049006
Volkov OA, Cosner CC, Brockway AJ, Kramer M, Booker M, Zhong S, Ketcherside KA, Wei S, Longgood J, McCoy M, Richardson TE, Wring SA, Peel M, Klinger JD, Posner BA, De Brabander JK, Phillips MA (2017) Identification of Trypanosoma brucei AdoMetDC inhibitors using a high-throughput mass spectrometry based assay. ACS Dis., 7, 512-526; https://doi.org/10.1021/acsinfecdis.7b00022; PMCID: PMC5511061
Trinh MN, Lu F, Li X, Das A, Liang Q, De Brabander JK, Brown, MS, Goldstein JL (2017) Triazoles inhibit cholesterol export from lysosomes by binding to NPC1. Natl. Acad. Sc. USA, 114, 89-94; https://doi.org/10.1073/pnas.1619571114; PMID: 27994139. PMC5224357
Gaelings L, Söderholm S, Bugai A, Fu Y, Nandania J, Schepens B, Lorey MB, Tynell J, Vande Ginste L, Le Goffic R, Miller MS, Kuisma M, Marjomäki V, De Brabander J, Matikainen S, Nyman TA, Bamford D, Saelens X, Julkunen I, Paavilainen H, Hukkanen V, Velagapudi V, Kainov DE (2017) Regulation of Kynurenine Biosynthesis during Influenza Virus Infection. The FEBS Journal 284, 222-236; https://doi.org/10.1111/febs.13966; PMID: 27860276. (Selected by the Editor in Chief as Editor’s Choice Paper: Boergeling Y, Ludwig S (2017) Targeting a metabolic pathway to fight the flu. The FEBS Journal 284, 218-221. Freely available in Virtual Issue of Editor’s Choice Papers at: http://onlinelibrary.wiley.com/doi/10.1111/febs.13997/epdf)
Eskiocak B, McMillan EA, Mendiratta S, Kollipara RK, Zhang H, Humphries CG, Wang C, Garcia-Rodriguez J, Ding M, Zaman A, Rosales TI, Eskiocak U, Smith MP, Sudderth J, Komurov K, DeBerardinis RJ, Wellbrock C, Davies MA, Wargo JA, Yu Y, De Brabander JK, Williams NS, Chin L, Rizos H, Long GV, Kittler R, White MA (2017) Biomarker Accessible and Chemically Addressable Mechanistic Subtypes of BRAF Melanoma. Cancer Discovery 7(8), 832-851; https://doi.org/10.1158/2159-8290.CD-16-0955; PMID: 28455392 PMCID: PMC5540806
Kissing S, Rudnik S, Damme M, Lüllmann-Rauch R, Ichihara A, Kornak U, Eskelinen E-L, Jabs S, Heeren J, De Brabander JK, Haas A, Saftig P (2017) Disruption of the vacuolar-type H+-ATPase complex in liver causes MTORC1-independent accumulation of autophagic vacuoles and lysosomes. Authophagy 13 (4), 670-685; http://dx.doi.org/10.1080/15548627.2017.1280216; PMCID: PMC5388235
Zhang L, Theodoropoulos PC, Eskiocak U, Wang W, Moon Y-A, Posner B, Williams NS, Wright WE, Kim SB, Nijhawan D, De Brabander JK, Shay JW (2016) Selective Targeting of Mutant Adenomatous Polyposis Coli (APC) in Colorectal Cancer. Science Translational Medicine 8, issue 361, pp. 361ra140; https://doi.org/10.1126/scitranslmed.aaf8127; PMID: 27798265 (Subject of commentary in ‘Nature Reviews Drug Discovery; Research Highlights, 2016, issue 15, pp 820-821; https://doi.org/10.1038/nrd.2016.247
Feng Y, Liu J, Carrasco YP, MacMillan JB, De Brabander JK (2016) Rifamycin Biosynthetic Congeners: Isolation and Total Synthesis of Rifsaliniketal and Total Synthesis of Salinisporamycin and Saliniketals A and B. Journal of the American Chemical Society 138, 7130-7142; https://doi.org/10.1021/jacs.6b03248; PMID: 27232659
Sato S, Jung H, Nakagawa T, Pawlosky R, Takeshima T, Lee W-R, Sakiyama H, Laxman S, Wynn RM, Tu B, MacMillan JB, De Brabander JK, Veech RL, Uyeda K (2016) Metabolite Regulation of Nuclear Localization of Carbohydrate Response Element-binding Protein (ChREBP). Role of AMP as an Allosteric Inhibitor. Biol. Chem. 291, 10515-10527; https://doi.org/10.1074/jbc.M115.708982; PMID: 26984404; PMCID: PMC4865902
Brockway AJ, Cosner CC, Volkov OA, Phillips MA, De Brabander JK (2016) Improved Synthesis of MDL 73811 – a Potent AdoMetDC Inhibitor and Anti-Trypanosomal Compound. Synthesis 48, 2065-2068; https://doi.org/10.1055/s-0035-1561608 ; PMID: 27482123; PMCID: PMC4966539
Vacuolar ATPase in Phagosome-Lysosome Fusion
Kissing, S.; Hermsen, C.; Repnik, U.; Nesset, C. K.; von Bargen, K.; Griffiths, G.; Ichihara, A.; Lee, B. S.; Schwake, M.; De Brabander, J.; Haas, A.; Saftig, P. J. Biol. Chem. 2015, 290, 14166.
Systematic Identification of Molecular Subtype-Selective Vulnerabilities in Non-Small-Cell Lung Cancer
Kim, H. S.; Mendiratta, S.; Kim, J.; Pecot, C. V.; Larsen, J. E.; Zubovych, I.; Seo, B. Y.; Kim, J.; Eskiocak, B.; Chung, H.; McMillan, E.; Wu, S.; De Brabander, J.; Komurov, K.; Toombs, J. E.; Wei, S.; Peyton, M.; Williams, N.; Gazdar, A. F.; Posner, B. A.; Brekken, R. A.; Sood, A. K.; Deberardinis, R. J.; Roth, M. G.; Minna, J. D.; White, M. A. Cell 2013, 155, 552.
Development of Proneurogenic, Neuroprotective Small Molecules
MacMillan, K. S.; Naidoo, J.; Liang, J.; Melito, L.; Williams, N. S.; Morlock, L.; Huntington, P. J.; Estill, S. J.; Longgood, J.; Becker, G. L.; McKnight, S. L.; Pieper, A. A.; De Brabander, J. K.; Ready, J. M. J. Am. Chem. Soc. 2011, 133, 1428.
Discovery of a Proneurogenic, Neuroprotective Chemical
Pieper, A. A.; Xie, S.; Capota, E.; Estill, S. J.; Zhong, J.; Long, J. M.; Becker, G. L.; Huntington, P.; Goldman, S. E.; Shen, C.-H.; Capota, M.; Britt, J. K.; Kotti, T.; Ure, K.; Brat, D. J.; Williams, N. S.; MacMillan, K.S.; Naidoo, J.; Melito, L.; Hsieh, J.; De Brabander, J. K.; Ready, J. M.; McKnight, S. L. Cell 2010, 142, 39.
(R)-Carvone as chiral template for the synthesis of some polyols
De Brabander, J. K.; Kulkarni, B. A.; Garcia-Lopez, R.; Vandewalle, M. Bulletin des Societes Chimiques Belges 1997, 106, 665.
Chemistry of the transition metals: application to organic synthesis
De Brabander, J. K. Chemie Magazine 1989, 15, 23.
The Protective Effect of Behavioral Activation on the Growth of a Syngeneic Tumor and Mortality in Socially Stressed Mice
De Brabander, B.; D'haeseleer, F.; De Brabander, M.; Distelmans, W.; Van Ginckel, R.; De Brabander, J. K. Eur. J. Psychiat., 1989, 3, 238.
Patents
Substituted benzimidazolium, pyrido-imidazolium, or pyrazino-imidazolium compounds as chemotherapeutics.
De Brabander, J. K.; Parada, L. F.; Lim, S. K.; Liang, Q.; Wang, H.-Y.; Shi, Y. Provisional Patent Appl. (Dec. 11, 2015); Serial Number 62/266,427.
Targeting emopamil binding protein (EBP) with small molecules that induce an abnormal feedback response by lowering endogenous cholesterol synthesis.
De Brabander, J. K.; Nijhawan, D.; Wang, W.; Theodoropoulos, P. Patent Appl. (July 5, 2015); Serial Number 62/189,069.
Benzamide or benzamine compounds useful as anticancer agents for the treatment of human cancers.
De Brabander, J. K.; Parada, L.; Dierick, S.; Lim, K. Patent Appl. (July 5, 2015); Serial Number 62/193,019.
Small-Molecule Agonists for Type-2 Orexin Receptor.
Yanagisawa, M.; De Brabander, J. K.; Kumagai, H. Patent Appl. (August 20, 2012); Serial Number 3/590,064. Issued as patent number US 8,871,794.
Small-Molecule Agonists for Type-2 Orexin Receptor.
Yanagisawa, M.; De Brabander, J. K.; Kumagai, H. Patent Appl. (June 4, 2009); Serial Number 12/478,753. Issued as patent number US 8,258,163.
Small Molecule Compounds Selective against Gram-Negative Bacterial Infections.
De Brabander, J. K.; MacMillan, J. B. Patent Appl. (May 13, 2014); Serial Number 61/992,642.
Compositions and Methods to Treat the Bihormonal Disorder in Diabetes.
Unger, R.; De Brabander, J.; Roth, M.; Evans, M. Patent Appl. Pub. Number US20150037361 A1 and WO2015017642A1.
Therapeutics Targeting Truncated Adenomatous Polyposis Coli (APC) Proteins.
De Brabander, J.; Shay, J. Patent Appl. (September 10, 2013); PCT/US14/0549.
Methods for Treating Parkinson’s Disease Using Pro-Neurogenic Compounds.
McKnight, S.L.; Pieper, A.A.; Ready, J.M.; De Brabander, J. Issued as patent number U.S. 8,877,797.
Methods of treating traumatic brain injury using pro-neurogenic compounds.
McKnight, S.L.; Pieper, A.A.; Ready, J.M.; De Brabander, J. Issued as patent number US 8,791,149 B2.
Methods of treating post- traumatic stress disorder using pro-neurogenic compounds.
McKnight, S.L.; Pieper, A.A.; Ready, J.M.; De Brabander, J. Issued as patent number US 8,748,473 B2.
Methods for treating amyotrophic lateral sclerosis using pro-neurogenic compounds.
McKnight, S.L.; Pieper, A.A.;Ready, J.M.; De Brabander, J. Issued as patent number US 8,735,440 B2.
Pro-neurogenic Compounds
McKnight, S. L.; Pieper, A.; Ready, J.; De Brabander, J. K. Patent Appl. (January 11, 2010); Serial Number 12/685,652. Issued as patent number US 8,362,277 and patent number US 8,604,074.
Palmerolides: Methods of Preparation and Derivatives
De Brabander, J. K.; Jiang, X.; Liu, B. Issued as patent number US 7,838,691.
Synthesis and Complete Stereochemical Assignment of Psymberin/Irciniastatin for use as Antitumor Compounds.
De Brabander, J. K.; Jiang, X. Issued as patent number US 7,429,616.
Dimeric Small Molecule Potentiators of Apoptosis.
Harran, P. G.; Wang, X.; De Brabander, J. K.; Li, L.; Thomas, R. M.; Suzuki, H. Issued as patent number US 7,309,792.
Synthesis of Peloruside A and Analogs Thereof for Use as Antitumor Agents.
De Brabander, J. K.; Liao, X. Issued as patent number US20040235939 A1, WO2004074249 A2.
Synthetic Salicylihalamides, Apicularens and Derivatives Thereof.
De Brabander, J. K.; Wu, Y. Issued as patent number US 6,617,348.
Müller KH, Kainov DE, El Bakkouri K, Saelens X, De Brabander JK, Kittel C, Samm E, de Landtsheer S, Muller CP (2011) The proton translocation domain of cellular vacuolar-ATPase provides a target for the treatment of influenza A virus infections.British Journal of Pharmacology 164, 344-357.
Takeshima T, Lee W-R, Sakiyama H, Laxman S, Wynn RM, Tu B, MacMillan JB, De Brabander JK, Veech RL, Uyeda K (2016) Metabolite Regulation of Nuclear Localization of Carbohydrate Response Element-binding Protein (ChREBP). Role of AMP as an Allosteric Inhibitor. Biol. Chem. First Published online March 16, 2016; doi:10.1074/jbc.M115.708982
Brockway AJ, Cosner CC, Volkov OA, Phillips MA, De Brabander JK (2016) Improved Synthesis of MDL 73811 – a Potent AdoMetDC Inhibitor and Anti-Trypanosomal Compound.Synthesis, accepted.