Dr. Martin Empting
Über
Dr. Martin Empting studierte Chemie an der Technischen Universität Darmstadt. Nach seinem Diplom, das mit dem Preis der "Dr. Anton-Keller-Stiftung" ausgezeichnet wurde, promovierte er bei Prof. Dr. Harald Kolmar. Im Jahr 2013 schloss er seine Promotion mit summa cum laude ab und wurde für seine Dissertation mit dem Schwerpunkt peptidische Wirkstoffkandidaten und biomimetische Konzepte mit dem Preis der Familie Bottling-Stiftung ausgezeichnet. Nach einem Postdoc bei Prof. Dr. Rolf W. Hartmann am Helmholtz-Institut für Pharmazeutische Forschung Saarland (HIPS), wo er sich mit dem Design und der Optimierung neuartiger Antiinfektiva gegen Gram-negative Bakterien beschäftigte, forscht er nun selbstständig. Im Februar 2022 schloss er seine Habilitation im Fach "Pharmazeutische und Medizinische Chemie" ab und wurde Leiter der HZI-Gruppe "Antivirale & Antivirulenz-Wirkstoffe". Sein zentrales Ziel ist es, neuartige synthetische Wirkstoffmoleküle für die Entwicklung dringend benötigter antiinfektiver Therapien zu entwickeln.
2024
Drug repurposing screen identifies lonafarnib as respiratory syncytial virus fusion protein inhibitor
Sake S, Zhang X, Rajak M, Urbanek-Quaing M, Carpentier A, Gunesch A, Grethe C, Matthaei A, Rückert J, Galloux M, …, Haid S, Pietschmann T (2024)
Nat. Commun. 15 (1)DOI: 10.1038/s41467-024-45241-y
2023
Disrupting Kaposi's Sarcoma-Associated Herpesvirus (KSHV) Latent Replication with a Small Molecule Inhibitor
Berwanger A, Stein S, Kany A, Gartner M, Loretz B, Lehr C, Hirsch A, Schulz T, Empting M (2023)
Journal of medicinal chemistry 66 (15): 10782-10790DOI: 10.1021/acs.jmedchem.3c00990
Towards Translation of PqsR Inverse Agonists: From In Vitro Efficacy Optimization to In Vivo Proof-of-Principle
Hamed M, Abdelsamie A, Rox K, Schütz C, Kany A, Röhrig T, Schmelz S, Blankenfeldt W, Arce-Rodriguez A, Borrero-de Acuña J, …, Hartmann R, Empting M (2023)
Adv. Sci. (Online)DOI: 10.1002/advs.202204443
2022
Respiratory Syncytial Virus Two-Step Infection Screen Reveals Inhibitors of Early and Late Life Cycle Stages
Sake S, Kosch C, Blockus S, Haid S, Gunesch A, Zhang X, Friesland M, Trummer S, Grethe C, Kühnel A, …, Schulz T, Pietschmann T (2022)
Antimicrobial agents and chemotherapyDOI: 10.1128/aac.01032-22
Transferring Microclusters of P. aeruginosa Biofilms to the Air-Liquid Interface of Bronchial Epithelial Cells for Repeated Deposition of Aerosolized Tobramycin
Horstmann J, Laric A, Boese A, Yildiz D, Röhrig T, Empting M, Frank N, Krug D, Müller R, Schneider-Daum N, Souza Carvalho-Wodarz C, Lehr C (2022)
ACS infectious diseases 8 (1): 137-149DOI: 10.1021/acsinfecdis.1c00444
2021
New PqsR Inverse Agonist
Schütz C, Empting M, Ahmed S, Hamed M, Hartmann R, Röhrig T, Kany A, Hirsch A (2021)
Patent A61K31/4439; A61K31/506; A61P31/04; C07D401/12; C07D403/12; (WO2021136803A1)
New PqsR Inverse Agonist
Schütz C, Empting M, Ahmed S, Hamed M, Hartmann R, Röhrig T, Kany A, Hirsch A (2021)
Patent A61K31/4439; A61K31/506; A61P31/04; C07D401/12; C07D403/12; (WO2021136803A1)
Novel PqsR Inverse Agonists
Hamed M, Ahmed S, Empting. M., Schütz C, Hartmann R, Röhrig T, Kany A, Hirsch A (2021)
Patent A61K31/4439; A61P31/04; C07D401/14; C07D417/14; (WO2021136805A1)
Novel PqsR Inverse Agonists
Hamed M, Ahmed S, Empting. M., Schütz C, Hartmann R, Röhrig T, Kany A, Hirsch A (2021)
Patent A61K31/4439; A61P31/04; C07D401/14; C07D417/14; (WO2021136805A1)
Towards the sustainable discovery and development of new antibiotics
Miethke M, Pieroni M, Weber T, Brönstrup M, Hammann P, Halby L, Arimondo P, Glaser P, Aigle B, Bode H, …, Moser H, Müller R (2021)
Nature reviews. Chemistry 5 (10): 726-749DOI: 10.1038/s41570-021-00313-1
A New PqsR Inverse Agonist Potentiates Tobramycin Efficacy to Eradicate Pseudomonas aeruginosa Biofilms
Schütz C, Ho D, Hamed M, Abdelsamie A, Röhrig T, Herr C, Kany A, Rox K, Schmelz S, Siebenbürger L, …, Lehr C, Empting M (2021)
Advanced science (Weinheim, Baden-Wurttemberg, Germany) 8 (12)DOI: 10.1002/advs.202004369
2020
Micro-rheological properties of lung homogenates correlate with infection severity in a mouse model of Pseudomonas aeruginosa lung infection
Murgia X, Kany A, Herr C, Ho D, Rossi C, Bals R, Lehr C, Hirsch A, Hartmann R, Empting M, Röhrig T (2020)
Scientific Reports 10 (1)DOI: 10.1038/s41598-020-73459-5
Squalenyl Hydrogen Sulfate Nanoparticles for Simultaneous Delivery of Tobramycin and an Alkylquinolone Quorum Sensing Inhibitor Enable the Eradication of P. aeruginosa Biofilm Infections
Ho D, Murgia X, Rossi C, Christmann R, Hüfner de Mello Martins A, Koch M, Andreas A, Herrmann J, Müller R, Empting M, …, Couvreur P, Lehr C (2020)
Angewandte Chemie (International ed. in English)DOI: 10.1002/anie.202001407
Tracheal brush cells release acetylcholine in response to bitter tastants for paracrine and autocrine signaling
Hollenhorst M, Jurastow I, Nandigama R, Appenzeller S, Li L, Vogel J, Wiederhold S, Althaus M, Empting M, Altmüller J, …, Saliba A, Krasteva-Christ G (2020)
FASEB j. 34 (1): 316-332DOI: 10.1096/fj.201901314RR
Restriction-Free Construction of a Phage-Presented Very Short Macrocyclic Peptide Library
Jakob V, Helmsing S, Hust M, Empting M (2020)
Methods in molecular biology (Clifton, N.J.) 2070: 95-113DOI: 10.1007/978-1-4939-9853-1_6
Discovery of Novel Latency-Associated Nuclear Antigen Inhibitors as Antiviral Agents Against Kaposi's Sarcoma-Associated Herpesvirus
Kirsch P, Jakob V, Elgaher W, Walt C, Oberhausen K, Schulz T, Empting M (2020)
ACS chemical biology 15 (2): 388-395DOI: 10.1021/acschembio.9b00845
Novel PqsR Inverse Agonists
Hamed M, Ahmed S, Empting. M., Schütz C, Hartmann R, Röhrig T, Kany A, Hirsch A (2020)
Patent (EP20150119)
2019
Concepts and Core Principles of Fragment-Based Drug Design
Kirsch P, Hartman A, Hirsch A, Empting M (2019)
Molecules (Basel, Switzerland) 24 (23)DOI: 10.3390/molecules24234309
Synthesis of New Cyclomarin Derivatives and Their Biological Evaluation towards Mycobacterium Tuberculosis and Plasmodium Falciparum
Kiefer A, Bader C, Held J, Esser A, Rybniker J, Empting M, Müller R, Kazmaier U (2019)
Chem. Eur. J. 25 (37): 8894-8902DOI: 10.1002/chem.201901640
Hit evaluation of an α-helical peptide: Ala-scan, truncation and sidechain-to-sidechain macrocyclization of an RNA polymerase Inhibitor
Kamal M, Habib M, Haupenthal J, Hartmann R, Empting M (2019)
Biol. Chem. 400 (3): 333-342DOI: 10.1515/hsz-2018-0333
Fragment-Based Discovery of a Qualified Hit Targeting the Latency-Associated Nuclear Antigen of the Oncogenic Kaposi's Sarcoma-Associated Herpesvirus/Human Herpesvirus 8
Kirsch P, Jakob V, Oberhausen K, Stein S, Cucarro I, Schulz T, Empting M (2019)
Journal of medicinal chemistry 62 (8): 3924-3939DOI: 10.1021/acs.jmedchem.8b01827
2018
In Vitro Model of the Gram-Negative Bacterial Cell Envelope for Investigation of Anti-Infective Permeation Kinetics
Graef F, Richter R, Fetz V, Murgia X, Rossi C, Schneider-Daum N, Allegretta G, Elgaher W, Haupenthal J, Empting M, …, Gordon S, Lehr C (2018)
ACS infectious diseases 4 (8): 1188-1196DOI: 10.1021/acsinfecdis.7b00165
Generation of Semi-Synthetic Shark IgNAR Single-Domain Antibody Libraries
Grzeschik J, Könning D, Hinz S, Krah S, Schröter C, Empting M, Kolmar H, Zielonka S (2018)
Methods in molecular biology (Clifton, N.J.) 1701: 147-167DOI: 10.1007/978-1-4939-7447-4_8
The Alkylquinolone Repertoire of Pseudomonas aeruginosa is Linked to Structural Flexibility of the FabH-like 2-Heptyl-3-hydroxy-4(1H)-quinolone (PQS) Biosynthesis Enzyme PqsBC
Witzgall F, Depke T, Hoffmann M, Empting M, Brönstrup M, Müller R, Blankenfeldt W (2018)
Chembiochem : a European journal of chemical biology 19 (14): 1531-1544DOI: 10.1002/cbic.201800153
Tackling Pseudomonas aeruginosa Virulence by a Hydroxamic Acid-Based LasB Inhibitor
Kany A, Sikandar A, Yahiaoui S, Haupenthal J, Walter I, Empting M, Köhnke J, Hartmann R (2018)
ACS chemical biology 13 (9): 2449-2455DOI: 10.1021/acschembio.8b00257
Aspherical and Spherical InvA497-Functionalized Nanocarriers for Intracellular Delivery of Anti-Infective Agents
Castoldi A, Empting M, Rossi C, Mayr K, Dersch P, Hartmann R, Müller R, Gordon S, Lehr C (2018)
Pharm Res 36 (1)DOI: 10.1007/s11095-018-2521-3
Targeting the Pseudomonas quinolone signal quorum sensing system for the discovery of novel anti-infective pathoblockers
Schütz C, Empting M (2018)
Beilstein journal of organic chemistry 14: 2627-2645DOI: 10.3762/bjoc.14.241
2017
In-depth Profiling of MvfR-Regulated Small Molecules in Pseudomonas aeruginosa after Quorum Sensing Inhibitor Treatment
Allegretta G, Maurer C, Eberhard J, Maura D, Hartmann R, Rahme L, Empting M (2017)
Frontiers in microbiology 8DOI: 10.3389/fmicb.2017.00924
Semi-synthetic vNAR libraries screened against therapeutic antibodies primarily deliver anti-idiotypic binders
Könning D, Rhiel L, Empting M, Grzeschik J, Sellmann C, Schröter C, Zielonka S, Dickgießer S, Pirzer T, Yanakieva D, Becker S, Kolmar H (2017)
Sci. Rep. 7 (1)DOI: 10.1038/s41598-017-10513-9
Camelid and shark single domain antibodies: structural features and therapeutic potential
Könning D, Zielonka S, Grzeschik J, Empting M, Valldorf B, Krah S, Schröter C, Sellmann C, Hock B, Kolmar H (2017)
Current opinion in structural biology 45: 10-16DOI: 10.1016/j.sbi.2016.10.019
2016
Single-domain antibodies for biomedical applications
Krah S, Schröter C, Zielonka S, Empting M, Valldorf B, Kolmar H (2016)
Immunopharmacol. Immunotoxicol. 38 (1): 21-8DOI: 10.3109/08923973.2015.1102934
Application of Dual Inhibition Concept within Looped Autoregulatory Systems toward Antivirulence Agents against Pseudomonas aeruginosa Infections
Thomann A, Mello Martins A, Brengel C, Empting M, Hartmann R (2016)
ACS chemical biology 11 (5): 1279-86DOI: 10.1021/acschembio.6b00117
Structure-Activity Relationships of 2-Sufonylpyrimidines as Quorum-Sensing Inhibitors to Tackle Biofilm Formation and eDNA Release of Pseudomonas aeruginosa
Thomann A, Brengel C, Börger C, Kail D, Steinbach A, Empting M, Hartmann R (2016)
ChemMedChem 11 (22): 2522-2533DOI: 10.1002/cmdc.201600419
Novel Strategies for the Treatment of Pseudomonas aeruginosa Infections
Wagner S, Sommer R, Hinsberger S, Lu C, Hartmann R, Empting M, Titz A (2016)
Journal of medicinal chemistry 59 (13): 5929-69DOI: 10.1021/acs.jmedchem.5b01698
Discovery of the first small-molecule CsrA-RNA interaction inhibitors using biophysical screening technologies
Maurer C, Fruth M, Empting M, Avrutina O, Hossmann J, Nadmid S, Gorges J, Herrmann J, Kazmaier U, Dersch P, Muller R, Hartmann R (2016)
Future medicinal chemistry 8 (9): 931-47DOI: 10.4155/fmc-2016-0033
Dissecting the Multiple Roles of PqsE in Pseudomonas aeruginosa Virulence by Discovery of Small Tool Compounds
Zender M, Witzgall F, Drees S, Weidel E, Maurer C, Fetzner S, Blankenfeldt W, Empting M, Hartmann R (2016)
ACS chemical biologyDOI: 10.1021/acschembio.6b00156
2015
Towards the evaluation in an animal disease model: Fluorinated 17β-HSD1 inhibitors showing strong activity towards both the human and the rat enzyme
Abdelsamie A, Bey E, Gargano E, van Koppen C, Empting M, Frotscher M (2015)
European journal of medicinal chemistry 103: 56-68DOI: 10.1016/j.ejmech.2015.08.030
Exploring the chemical space of ureidothiophene-2-carboxylic acids as inhibitors of the quorum sensing enzyme PqsD from Pseudomonas aeruginosa
Sahner J, Empting M, Kamal A, Weidel E, Groh M, Börger C, Hartmann R (2015)
European journal of medicinal chemistry 96: 14-21DOI: 10.1016/j.ejmech.2015.04.007
Engineering a Constrained Peptidic Scaffold towards Potent and Selective Furin Inhibitors
Fittler H, Depp A, Avrutina O, Dahms S, Than M, Empting M, Kolmar H (2015)
Chembiochem : a European journal of chemical biology 16 (17): 2441-4DOI: 10.1002/cbic.201500447
Catechol-based substrates of chalcone synthase as a scaffold for novel inhibitors of PqsD
Allegretta G, Weidel E, Empting M, Hartmann R (2015)
European journal of medicinal chemistry 90: 351-9DOI: 10.1016/j.ejmech.2014.11.055
2014
Potent inhibitors of human matriptase-1 based on the scaffold of sunflower trypsin inhibitor
Fittler H, Avrutina O, Empting M, Kolmar H (2014)
Journal of peptide science : an official publication of the European Peptide Society 20 (6): 415-20DOI: 10.1002/psc.2629
Design and synthesis of a library of lead-like 2,4-bisheterocyclic substituted thiophenes as selective Dyrk/Clk inhibitors
Schmitt C, Kail D, Mariano M, Empting M, Weber N, Paul T, Hartmann R, Engel M (2014)
PLoS ONE 9 (3)DOI: 10.1371/journal.pone.0087851
Inhibition of 17β-HSD1: SAR of bicyclic substituted hydroxyphenylmethanones and discovery of new potent inhibitors with thioether linker
Abdelsamie A, Bey E, Hanke N, Empting M, Hartmann R, Frotscher M (2014)
European journal of medicinal chemistry 82: 394-406DOI: 10.1016/j.ejmech.2014.05.074
Composing compound libraries for hit discovery--rationality-driven preselection or random choice by structural diversity?
Weidel E, Negri M, Empting M, Hinsberger S, Hartmann R (2014)
Future medicinal chemistry 6 (18): 2057-72DOI: 10.4155/fmc.14.142
From in vitro to in cellulo: structure-activity relationship of (2-nitrophenyl)methanol derivatives as inhibitors of PqsD in Pseudomonas aeruginosa
Storz M, Allegretta G, Kirsch B, Empting M, Hartmann R (2014)
Organic & biomolecular chemistry 12 (32): 6094-104DOI: 10.1039/c4ob00707g
2013
Combinatorial tuning of peptidic drug candidates: high-affinity matriptase inhibitors through incremental structure-guided optimization
Fittler H, Avrutina O, Glotzbach B, Empting M, Kolmar H (2013)
Org. Biomol. Chem. 11 (11): 1848-57DOI: 10.1039/c3ob27469a
PHIP-label: parahydrogen-induced polarization in propargylglycine-containing synthetic oligopeptides
Körner M, Sauer G, Heil A, Nasu D, Empting M, Tietze D, Voigt S, Weidler H, Gutmann T, Avrutina O, …, Ratajczyk T, Buntkowsky G (2013)
Chemical communications (Cambridge, England) 49 (71): 7839-41DOI: 10.1039/c3cc43978j
2012
From pico to nano: biofunctionalization of cube-octameric silsesquioxanes by peptides and miniproteins
Fabritz S, Hörner S, Könning D, Empting M, Reinwarth M, Dietz C, Glotzbach B, Frauendorf H, Kolmar H, Avrutina O (2012)
Org. Biomol. Chem. 10 (31): 6287-93DOI: 10.1039/c2ob25728a
Between two worlds: a comparative study on in vitro and in silico inhibition of trypsin and matriptase by redox-stable SFTI-1 variants at near physiological pH
Avrutina O, Fittler H, Glotzbach B, Kolmar H, Empting M (2012)
Org. Biomol. Chem. 10 (38): 7753-62DOI: 10.1039/c2ob26162f
Braces for the peptide backbone: insights into structure-activity relationships of protease inhibitor mimics with locked amide conformations
Tischler M, Nasu D, Empting M, Schmelz S, Heinz D, Rottmann P, Kolmar H, Buntkowsky G, Tietze D, Avrutina O (2012)
Angewandte Chemie (International ed. in English) 51 (15): 3708-12DOI: 10.1002/anie.201108983
2011
'Triazole bridge': disulfide-bond replacement by ruthenium-catalyzed formation of 1,5-disubstituted 1,2,3-triazoles
Empting M, Avrutina O, Meusinger R, Fabritz S, Reinwarth M, Biesalski M, Voigt S, Buntkowsky G, Kolmar H (2011)
Angewandte Chemie (International ed. in English) 50 (22): 5207-11DOI: 10.1002/anie.201008142
2010
Towards click bioconjugations on cube-octameric silsesquioxane scaffolds
Fabritz S, Heyl D, Bagutski V, Empting M, Rikowski E, Frauendorf H, Balog I, Fessner W, Schneider J, Avrutina O, Kolmar H (2010)
Org. Biomol. Chem. 8 (9): 2212-8DOI: 10.1039/b923393h
2009
Application of copper(I) catalyzed azide-alkyne 3+2 cycloaddition to the synthesis of template-assembled multivalent peptide conjugates
Avrutina O, Empting M, Fabritz S, Daneschdar M, Frauendorf H, Diederichsen U, Kolmar H (2009)
Org. Biomol. Chem. 7 (20): 4177-85DOI: 10.1039/b908261a