Research

Publications and Patents

Publications

De Vita, E., Smits, N., van den Hurk, H., Beck, E.M., Hewitt, J., Baillie, G., Russell, E., Pannifer, A., Hamon, V., Morrison, A., McElroy, S.P., Jones, P., Ignatenko, N.A., Gunkel, N., Miller, A.K. "Synthesis and Structure–Activity Relationships of N-(4-Benzamidino)-Oxazolidinones–Potent and Selective Inhibitors of Kallikrein-Related Peptidase 6" ChemRxiv Preprint DOI: 10.26434/chemrxiv.9788276.v1

Geraldy, M., Morgen, M., Sehr, P., Steimbach, R.R., Ridinger, J., Oehme, I., Witt, O., Malz, M., Nogueira, M.S., Koch, O., Gunkel, N., Miller, A.K. "Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated" J. Med. Chem. 2019, 62, 4426–4443.
Originally uploaded as a preprint at ChemRxiv. ChemRxiv Preprint; DOI: doi.org/10.26434/chemrxiv.7406618.v1

De Vita, E., Schüler, P., Lovell, S., Lohbeck, J., Kullmann, S., Rabinovich, E., Sananes, A., Heßling, B., Hamon, V., Papo, N., Heß, J., Tate, E.W., Gunkel, N., and Miller, A.K. “Depsipeptides featuring a neutral P1 are potent inhibitors of kallikrein-related peptidase 6 with on-target cellular activity” J. Med. Chem. 2018, 61, 8859–8874.

Kolbinger, F.R., Koeneke, E. Ridinger, J., Heimburg, T., Bayer, T., Sippl, W., Jung, M., Gunkel, N. Miller, A.K., Witt, O., Oehme, I. “The HDAC6/8/10 inhibitor TH34 induces DNA damage-mediated cell death in human high-grade neuroblastoma cell lines” Archives of Toxicology, 2018, 92, 2649–2664.

Ridinger, J., Koeneke, E., Kolbinger, F.R., Koerholz, K., Mahboobi, S., Gunkel, N., Miller, A.K., Peterziel, H., Hamacher-Brady, A., Witt, O., Oehme, I. “Dual role of HDAC10 in lysosomal exocytosis and DNA repair promotes neuroblastoma chemoresistance” Scientific Reports 2018, 8, 10039.

Sananes, A., Cohen, I., Shahar, A., Hockla, A., De Vita, E., Miller, A.K., Radisky, E., Papo, N. “A selective, proteolysis-resistant inhibitor of kallikrein-related peptidase 6 (KLK6) for cancer therapy, developed by combinatorial engineering” J. Biol. Chem. 2018, 293, 12663–12680.

Longuespée, R., Wefers, A.K., De Vita, E., Miller, A.K., Reuss, D.E., Wick, W., Herold-Mende, C., Kriegsmann, M., Schirmacher, P., von Deimling, A., Pusch, S. “Rapid detection of 2-hydroxyglutarate in frozen sections of IDH mutant tumors by MALDI-TOF mass spectrometry” Acta Neuropathol. Commun. 2018, 6, 21.

Moraru, A., Wiederstein, J., Pfaff, D., Fleming, T., Miller, A.K., Nawroth, P., Teleman, A.A.“Elevated levels of the reactive metabolite methylglyoxal recapitulate progression of Type 2 Diabetes” Cell Metabolism, 2018, 27, 926–934.

Holland-Letz, T., Gunkel, N., Amtmann, E., Kopp-Schneider, A. “Parametric modeling and optimal experimental designs for estimating isobolograms for drug interactions in toxicology” J. Biopharm. Stat. 2018, 28, 763–777.

Miller, A.K., Brönstrup, M. “Drug Innovation in Academia: A Helmholtz Drug Research Initiative Conference” ChemMedChem 2017, 12, 1652-1654.

Lohbeck, J., Miller, A.K. "Practical synthesis of a phthalimide-based Cereblon ligand to enable PROTAC development” Bioorg. Med. Chem. Lett. 2016, 26, 5260-5262.

Morgen, M., Jöst, C., Malz, M., Janowski, R., Niessing, D., Klein, C.D., Gunkel, N., Miller, A.K. “Spiroepoxytriazoles Are Fumagillin-like Irreversible Inhibitors of MetAP2 with Potent Cellular Activity” ACS Chem Biol. 2016, 11, 1001-1011.

Fritzching, B., Zhou-Suckow, Z., Trojanek, J.B., Schubert, S.C., Schatterny, J., Hirtz, S., Agrawal, R., Muley, T., Kahn, N., Sticht, C., Gunkel, N., Welte, T., Randell, S.H., Länger, F., Schnabel, P., Herth, F.J.F., Mall, M.A. "Hypoxic epithelial necrosis triggers neutrophilic inflammation via IL-1 receptor signaling in cystic fibrosis lung disease." Am. J. Respir. Crit. Care Med. 2015, 191, 902–913.

Seidensaal, K., Nollert, A., Feige, A.H., Muller, M., Fleming, T., Gunkel, N., Zaoui, K., Grabe, N., Weichert, W., Weber, K.J., Plinkert, P., Simon, C., Hess, J. “Impaired aldehyde dehydrogenase 1 subfamily member 2A-dependent retinoic acid signaling is related with a mesenchymal-like phenotype and an unfavorable prognosis of head and neck squamous cell carcinoma” Mol Cancer. 2015, 14, 204.

Senyilmaz, D., Virtue, S., Xu, X., Tan, C.Y., Griffin, J.L., Miller, A.K., Vidal-Puig, A., Teleman, A.A. “Regulation of mitochondrial morphology and function by stearoylation of TFR1” Nature 2015, 525, 124-128.

Klika, K.D., Schüler, P., Miller, A.K. “The C6 configuration and syn/anti conformational preference of the bisulfite adducts of deoxyuridine and deoxycytidine by NMR and DFT calculations” Tetrahedron: Asymmetry, 2014, 25, 1335-1339.

Pusch, S., Schweizer, L., Beck, A.C., Lehmler, J.M., Weissert, S., Balss, J., Miller, A.K., von Deimling, A. “D-2-Hydroxyglutarate producing neo-enzymatic activity inversely correlates with frequency of the type of isocitrate dehydrogenase 1 mutations found in glioma” Acta Neuropathol. Commun. 2014 , 2, 19.

Schüler P, Miller A.K. “Sequencing the sixth base (5-hydroxymethylcytosine): selective DNA oxidation enables base-pair resolution” Angew. Chem. Int. Ed. 2012, 51, 10704.

Miller, A.K. "Catalysis in the Total Synthesis of Bryostatin 16" Angew. Chem. Int. Ed. 2009, 48, 3221-3223.

Miller A.K.; Hughes, C. C.; Kennedy-Smith, J. J.; Gradl, S. N.; Trauner, D. "Total Synthesis of (-)-Heptemerone B and (-)-Guanacastepene E" J. Am. Chem. Soc. 2006, 128, 17057-17062.

Miller, A.K., Trauner, D. "Mapping the chemistry of highly unsaturated pyrone polyketides" Synlett 2006, 14, 2295-2316.

Hughes, C.C., Miller, A.K., Trauner, D. “An electrochemical approach to the guanacastepenes.” Org. Lett. 2005, 7, 3425–3428.

Barbarow, J., Miller, A.K., Trauner, D. "Biomimetic synthesis of elysiapyrones A and B." Org. Lett. 2005, 7, 2901–2903.

Liang, G., Miller, A.K., Trauner, D. "Stereoselective synthesis of cyercene A and the placidenes." Org. Lett. 2005, 7, 819–821.

Miller, A.K., Byun, D., Beaudry, C., Trauner, D. "The total synthesis of (–)-crispatene." Proc. Nat. Acad. Sci. 2004, 101, 12019–12023.

Miller, A.K., Banghart, M.R., Beaudry, C., Suh, J.M., Trauner, D. "Development of novel Lewis acid catalyzed cycloisomerizations: synthesis of bicyclo[3.1.0]hexenes and cyclopentenones." Tetrahedron, 2003, 59, 8919–8930.

Miller, A.K., Trauner, D. "Total synthesis of (±)-photodeoxytridachione using a Lewis acid catalyzed cyclization." Ang. Chem. Int. Ed. 2003, 42, 549–552.

Zhao, S.-H., Miller, A.K., Berger, J., Flippin, L.A. "Synthesis of arylpiperazines via palladium catalyzed aromatic amination reactions with unprotected piperazines." Tetrahedron Lett. 1996, 37, 4463–4466.

Patents

Amtmann, E., Gunkel, N., Miller, A., Morgen, M. "Compositions comprising dithiocarbamate and cyclodextrin with a source of heavy metal for treatment of tumors and other diseases." PCT Int. Appl. 2018, WO2018069525.

Miller, A., Schüler, P., De Vita, E. "Preparation of pyrazolylaminooxoethyl indolylacetates as human kallikrein-related peptidase 6 inhibitors for the treatment of diseases." PCT Int. Appl. 2018, WO2018065607.

Miller, A., Jöst, C., Klein, C. "Preparation of spiroepoxide tetrahydrobenzotriazoles useful as MetAP-II inhibitors." PCT. Int. Appl. 2014, WO2014044399.

Alanine, A., Flohr, A., Miller, A.K., Norcross, R.D., Claus, R. "Preparation of N-benzothiazol-2-yl amides having affinity toward the A2a adenosine receptor." PCT Int. Appl. 2001, WO2001097786

Berger, J., Flippin, L.A., Greenhouse, R., Jaime-Figueroa, S., Liu, Y., Miller, A.K., Putman, D.G., Weinhardt, K.K., Zhao, S.-H. "Preparation of 2-amino-4-aryppyrimidines as 5-HT2B antagonists." 1999, US5958934