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Publications and Patents

H. Nůsková, F. Garcia-Cortizo, L.S. Schwenker, T. Sachsenheimer, E. Diakonov, M. Tiebe, M. Schneider, J. Lohbeck, C. Reid, A. Kopp-Schneider, D. Helm, B. Brügger, A.K. Miller, A. A. Teleman "Competition for cysteine acylation by C16:0 and C18:0 derived lipids is a global phenomenon in the proteome" J. Biol. Chem. 2023, In Press.

S. Lechner, R.R. Steimbach, L. Wang, M.L. Deline, Y.-C. Chang, T. Fromme, M. Klingenspor, P. Matthias, A.K. Miller, G. Medard, B. Kuster "Chemoproteomic target deconvolution reveals histone deacetylases as targets of (R)-lipoic acid" Nat. Comm. 202314, 3548.

J. Samarin, P. Fabrowski, R. Kurilov, H. Nuskova, J. Hummel-Eisenbeiss, H. Pink, N. Li, V. Weru, H. Alborzinia, U. Yildiz, L. Grob, M. Taubert, M. Czech, M. Morgen, C. Brandstädter, K. Becker, L. Mao, A.K. Jayavelu, A. Goncalves, U. Uhrig, J. Seiler, Y. Lyu, S. Diederichs, U. Klingmüller, M. Muckenthaler, A. Kopp-Schneider, A. Teleman, A.K. Miller, N. Gunkel "Low level of antioxidant capacity biomarkers but not target overexpression predicts vulnerability to ROS-inducing drugsRedox Biol. 202362, 102639.

M. Fresnais, I. Jung, U.B. Klein, A.K. Miller, S. Turcan, W. E. Haefeli, J. Burhenne and R. Longuespée "Important Requirements for Desorption/Ionization Mass Spectrometric Measurements of Temozolomide-Induced 2′-Deoxyguanosine Methylations in DNACancers 2023, 15, 716.

U. Barayeu, D. Schilling, M. Eid, T. N. X. da Silva, L. Schlicker, N. Mitreska, C. Zapp, F. Gräter, A. K. Miller, R. Kappl, A. Schulze, J. P. F. Angeli, T. P. Dick "Hydropersulfides inhibit lipid peroxidation and ferroptosis by scavenging radicalsNat. Chem. Biol. 202319, 28–37.

G. Triller, E.P. Vlachou, H. Hashemi, M. van Straaten, J. Zeelen, Y. Kelemen, C. Baehr, C.L. Marker, S. Ruf, A. Svirina, S. Kruse, A. Baumann, A.K. Miller, M. Bartel, M. Pravetoni, C.E. Stebbins, F.N. Papavasiliou, J.P. Verdi "A trypanosome-derived immunotherapeutics platform elicits potent high-affinity antibodies, negating the effects of the synthetic opioid fentanyl" Cell Reports 2023, 42, 112049.

L. Zhang, S. Lovell, E. De Vita, P.K.A. Jagtap. L. Daniel, G. Goya, S, Kjaer, A. Borg, J. Hennig, A.K. Miller, E.W. Tate "A KLK6 activity-based probe reveals a role for KLK6 activity in pancreatic cancer cell invasion" J. Am. Chem. Soc. 2022, 144, 22493–22504.

R.R. Steimbach, C.J. Herbst-Gervasoni, S. Lechner, T.M. Stewart, G. Klinke, J. Ridinger, M.N.E. Geraldy, G. Tihanyi,  J.R. Foley, U. Uhrig, G. Poschet, R.A. Casero Jr., G. Medard, I. Oehme, D.W. Christianson, N. Gunkel, A.K. Miller "Aza-SAHA Derivatives are Selective Histone Deacetylase 10 Chemical Probes That Inhibit Polyamine Deacetylation and Phenocopy HDAC10 Knockout" J. Am. Chem. Soc. 2022, 144, 18861-18875. [ChemRxiv]

L. Muckenthaler, O. Marques, S. Colucci, J. Kunz, P. Fabrowski, T. Bast, S. Altamura, B. Höchsmann, H. Schrezenmeier, M. Langlotz, P. Richter-Pechanska, T. Rausch, N. Hofmeister-Mielke, N. Gunkel, M.W. Hentze, A.E. Kulozik, M.U. Muckenthaler "Consitutional PIGA mutations cause a novel subtype of hemochromatosis in patients with neurologic dysfunctionBlood 2022139, 1418–1422.

A. Baumann, D. Isak, J. Lohbeck, P.K.A. Jagtap, J. Hennig, A. K. Miller "Scalable synthesis and structural characterization of reversible KLK6 inhibitors" RSC Advances 2022, 12, 26989–26993. [Correction]

T. M. Stewart, J. R. Foley, C. E. Holbert, G. Klinke, G. Poschet, R. R. Steimbach, A. K. Miller , R. A. Casero Jr "Histone deacetylase 10 liberates spermidine to support polyamine homeostasis and tumor cell growth" J. Biol. Chem. 2022, 298, 102407.

S. Jänner (*), D. Isak (*), Y. Li, K.N. Houk, A.K. Miller "Bioinspired Asymmetric Total Synthesis of Emeriones A–C" Ang. Chem. Int. Ed. 2022, 61, e202205878. (*) = Equal contribution [ChemRxiv]

Highlighted in Chemistry Views

D. Herp, J. Ridinger, D. Robaa, S. A. Shinsky, K. Schmidtkunz, T. Z. Yesiloglu, T. Bayer, R.R. Steimbach, C.J. Herbst-Gervasoni, A. Merz, C. Romier, P. Sehr, N. Gunkel, A. K. Miller, D. W. Christianson, I. Oehme, W. Sippl, M. Jung "First Fluorescent Acetylspermidine Deacetylation Assay for HDAC10 Identifies Selective Inhibitors with Cellular Target Engagement" ChemBioChem 2022, 23, e202200180.

D. Schilling, U. Barayeu, R.R. Steimbach, D. Talwar, A.K. Miller, T. Dick "Commonly Used Alkylating Agents Limit Persulfide Detection by Converting Protein Persulfides into Thioethers" Ang. Chem. Int. Ed. 2022, 61, e202203684.

S. Lechner, M.I.P. Malgapo, C. Grätz, R.R. Steimbach...A.K.Miller, M.W. Pfaffl, M.E. Linder, B. Kuster, G. Medard "Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target" Nat. Chem. Biol. 2022, 18, 812-820.

B.-O Gohlke, F. Zincke, A. Eckert, D. Kobelt, S. Preissner, J.M. Liebeskind, N. Gunkel, K. Putzker, J. Lewis, S. Preissner, B. Kortüm, W. Walther, C. Mura, P.E. Bourne, U. Stein, R. Preissner "Real-world Evidence for Preventative Effects of Statins on Cancer Incidence: A Trans-Atlantic Analysis" Clin. Transl. Med. 2022, 12, e726.

H.Yoon, E.M. Triplet, W.L. Simon, C.-I. Choi, L.S. Kleppe, E. De Vita, A.K. Miller, I.A. Scarisbrick "Blocking Kallikrein 6 promotes developmental myelination" Glia 2022, 70, 430–450.

R.R. Steimbach, G. Tihanyi, M. Géraldy, A. Wzorek, A.K. Miller, K.D. Klika "Can an Intermediate Rate of Nitrogen Inversion Affect Drug Efficacy?" Symmetry 2021, 13, 1753.

S. Tönges, K. Masagounder, F. Lenich, J. Gutekunst, M. Tönges, J. Lohbeck, A.K.Miller, F. Böhl, F. Lyko "Evaluating Invasive Marbled Crayfish as a Potential Livestock for Sustainable Aquaculture" Front. Ecol. Evol. 2021, 9, 651981.

H. Nůsková, M.V. Serebryakova, A. Ferrer-Caelles, T. Sachsenheimer, C. Lüchtenborg, A.K. Miller, B. Bruegger, L.V. Kordyukova, A.A. Teleman "Stearic acid blunts growth-factor signaling via oleoylation of GNAI proteins" Nat. Comm. 2021, 12, 4590.

M. Morgen, P. Fabrowki, E. Amtmann, N. Gunkel, A.K. Miller "Inclusion Complexes of Gold(I)-Dithiocarbamates with ß-Cyclodextrin: A Journey from Drug Repurposing towards Drug Discovery" Chem. Eur. J. 2021, 27, 12156–12165.

M. Morgen, J. Lohbeck, A. K. Miller "Preparation of 1-Benzyl-7-methylene-1,5,6,7-tetrahydro-4H-benzo[d]imidazol-4-one" OrgSyn 2021, 98, 315–342.

M. Morgen, J. Lohbeck, A. K. Miller "Mild mono-Acylation of 4,5-Diiodoimidazole: Preparation of 1-(5-Iodo-1H-imidazole-4-yl)pent-4-en-1-one" OrgSyn 2021, 98, 171–193.

C. J. Herbst-Gervasoni, R. R. Steimbach, M. Morgen, A. K. Miller, D. W. Christianson "Structural Basis for the Selective Inhibition of HDAC10, the Cytosolic Polyamine Deacetylase" ACS Chem. Biol. 2020, 15, 2154–2163.

A. Baumann, A. Wzorek, V. A. Soloshonok, K. D. Klika, A. K. Miller "Potentially Mistaking Enantiomers for Different Compounds Due to the Self-Induced Diastereomeric Anisochronism (SIDA) Phenomenon" Symmetry 2020, 12, 1106.

M. Morgen, R. R. Steimbach, M. Géraldy, L. Hellweg, P. Sehr, J. Ridinger, O. Witt , I. Oehme, C. J. Herbst‐Gervasoni, J. D. Osko, N. J. Porter, D. W. Christianson, N. Gunkel, A. K. Miller "Design and Synthesis of Dihydroxamic Acids as HDAC6/8/10 Inhibitors" ChemMedChem 2020, 15, 1163–1174.

Chen, X., Chen, X., Steimbach, R.R., Wu, T., Li, H., Dan, W., Shi, P., Cao, C., Li, D., Miller, A.K., Gao, J., Zhu, Y. "Novel 2, 5-Diketopiperazine Derivatives as Potent Selective Histone Deacetylase 6 Inhibitors: Rational Design, Synthesis and Antiproliferative Activity" Eur. J. Med. Chem. 2020, 187, 111950.

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" ChemMedChem 2020, 15, 79-95.

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.

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" Sci. Rep. 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 Metab. 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.

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.

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.

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

Patents

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