EN | DE

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.


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

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

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

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

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

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

2017

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

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

2016

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

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

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

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

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

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