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Dr. Jörg Haupenthal

Über

Dr. rer. nat. Jörg Haupenthal ist Diplom-Biologe und Wissenschaftler in der Abteilung von Prof. Dr. Anna Hirsch am HIPS. Nach einer mehrjährigen Tätigkeit in der Krebsforschung begann er sich ab dem Jahr 2009 mit der Entwicklung neuartiger Antiinfektiva zu befassen. Im Rahmen der biologischen Evaluierung solcher Substanzen unter verschiedensten Bedingungen (in vivo, ex vivo, in vitro) betreut er Masterstudenten und Doktoranden. Zudem koordiniert er die biologische Testung durch mehrere Technische Mitarbeiter. Gemeinsam mit Prof. Dr. Anna K.H. Hirsch leitet er ein Projekt zur Entwicklung neuer Pseudomonas aeruginosa LasB Inhibitoren, zur Behandlung akuter Infektionen der Lunge und der Augen. Dieses Projekt wurde und wird durch namhafte Drittmittel gefördert, darunter CARB-X, INCATE und das BMBF. Jörg Haupenthal ist biologischer Sicherheitsbeauftragter der Abteilung „Wirkstoffdesign und Optimierung“ und Strahlenschutzbeauftragter des HIPS. Er ist Autor und Mitautor von über 60 wissenschaftlichen Publikationen mit mehr als 1.600 Zitierungen.


2024

Development and evaluation of 2,4-disubstituted-5-aryl pyrimidine derivatives as antibacterial agents

Khalifa H, Rasheed S, Haupenthal J, Herrmann J, Mandour Y, Abadi A, Engel M, Müller R, Hirsch A, Abdel-Halim M, Hamed M (2024)

Archiv der PharmazieDOI: 10.1002/ardp.202300656

2023

Inhibitors of the Elastase LasB for the Treatment of Pseudomonas aeruginosa Lung Infections

Konstantinovic J, Kany A, Alhayek A, Abdelsamie A, Sikandar A, Voos K, Yao Y, Andreas A, Shafiei R, Loretz B, …, Haupenthal J, Hirsch A (2023)

ACS Cent. Sci. 9 (12): 2205-2215DOI: 10.1021/acscentsci.3c01102

Clean Synthetic Strategies to Biologically Active Molecules from Lignin: A Green Path to Drug Discovery

Afanasenko A, Wu X, Santi A, Elgaher W, Kany A, Shafiei R, Schulze M, Schulz T, Haupenthal J, Hirsch A, Barta K (2023)

Angew. Chem. Int. Ed.DOI: 10.1002/anie.202308131

Exploring the Translational Gap of a Novel Class of Escherichia coli IspE Inhibitors

Ropponen H, Diamanti E, Johannsen S, Illarionov B, Hamid R, Jaki M, Sass P, Fischer M, Haupenthal J, Hirsch A (2023)

ChemMedChemDOI: 10.1002/cmdc.202300346

Inhibitors of the Elastase LasB for the treatment of Pseudomonas aeruginosa lung infections

Konstantinovic J, Kany A, Alhayek A, Abdelsamie A, Sikandar A, Voos K, Yao Y, Andreas A, Shafiei R, Loretz B, …, Haupenthal J, Hirsch A (2023)

DOI: 10.26434/chemrxiv-2023-bszcb

Facile Production of the Pseudomonas aeruginosa Virulence Factor LasB in E. coli for Structure-Based Drug Design

Kolling D, Haupenthal J, Hirsch A, Köhnke J (2023)

ChemBioChemDOI: 10.1002/cbic.202300185

Not Every Hit-Identification Technique Works on 1-Deoxy-d-Xylulose 5-Phosphate Synthase (DXPS): Making the Most of a Virtual Screening Campaign

Johannsen S, Gierse R, Olshanova A, Smerznak E, Laggner C, Eschweiler L, Adeli Z, Hamid R, Alhayek A, Reiling N, Haupenthal J, Hirsch A (2023)

ChemMedChemDOI: 10.1002/cmdc.202200590

2022

Discovery of the First Selective Nanomolar Inhibitors of ERAP2 by Kinetic Target‐Guided Synthesis

Camberlein V, Fléau C, Sierocki P, Li L, Gealageas R, Bosc D, Guillaume V, Warenghem S, Leroux F, Rosell M, …, Bouvier M, Deprez-Poulain R (2022)

Angew. Chemie 134 (39)DOI: 10.1002/ange.202203560

Synthesis, biological evaluation, and molecular docking studies of aldotetronic acid-based LpxC inhibitors

Wimmer S, Hoff K, Martin B, Grewer M, Denni L, Lascorz Massanet R, Raimondi M, Bülbül E, Melesina J, Hotop S, …, Sippl W, Holl R (2022)

Bioorganic chemistry 131DOI: 10.1016/j.bioorg.2022.106331

An Efficient Way to Screen Inhibitors of Energy-Coupling Factor (ECF) Transporters in a Bacterial Uptake Assay

Bousis S, Winkler S, Haupenthal J, Fulco F, Diamanti E, Hirsch A (2022)

International journal of molecular sciences 23 (5)DOI: 10.3390/ijms23052637

Discovery and Characterization of Synthesized and FDA-Approved Inhibitors of Clostridial and Bacillary Collagenases

Alhayek A, Abdelsamie A, Schönauer E, Camberlein V, Hutterer E, Posselt G, Serwanja J, Blöchl C, Huber C, Haupenthal J, …, Wessler S, Hirsch A (2022)

Journal of medicinal chemistry 65 (19): 12933-12955DOI: 10.1021/acs.jmedchem.2c00785

Discovery of novel drug-like antitubercular hits targeting the MEP pathway enzyme DXPS by strategic application of ligand-based virtual screening

Di Zhu, Johannsen S, Masini T, Simonin C, Haupenthal J, Illarionov B, Andreas A, Awale M, Gierse R, van der Laan T, …, Reymond J, Hirsch A (2022)

Chem. Sci. 13 (36): 10686-10698DOI: 10.1039/D2SC02371G

The Structures and Binding Modes of Small-Molecule Inhibitors of Pseudomonas aeruginosa Elastase LasB

Camberlein V, Jézéquel G, Haupenthal J, Hirsch A (2022)

Antibiotics 11 (8)DOI: 10.3390/antibiotics11081060

Structure-Guided Optimization of Small-Molecule Folate Uptake Inhibitors Targeting the Energy-Coupling Factor Transporters

Kiefer A, Bousis S, Hamed M, Diamanti E, Haupenthal J, Hirsch A (2022)

J. Med. Chem.DOI: 10.1021/acs.jmedchem.1c02114

N-Aryl-2-iso-butylmercaptoacetamides: the discovery of highly potent and selective inhibitors of Pseudomonas aeruginosa virulence factor LasB and Clostridium histolyticum virulence factor ColH

Voos K, Yahiaoui S, Konstantinovic J, Schönauer E, Alhayek A, Sikandar A, Si Chaib K, Ramspoth T, Rox K, Haupenthal J, …, Ducho C, Hirsch A (2022)

ChemRxivDOI: 10.26434/chemrxiv-2022-fjrqr

Structure-Based Design of α-Substituted Mercaptoacetamides as Inhibitors of the Virulence Factor LasB from Pseudomonas aeruginosa

Kaya C, Walter I, Alhayek A, Shafiei R, Jézéquel G, Andreas A, Konstantinovic J, Schönauer E, Sikandar A, Haupenthal J, …, Hartmann R, Hirsch A (2022)

ACS Infect. Dis.DOI: 10.1021/acsinfecdis.1c00628

N-Aryl Mercaptopropionamides as Broad-Spectrum Inhibitors of Metallo-β-Lactamases

Kaya C, Konstantinovic J, Kany A, Andreas A, Kramer J, Brunst S, Weizel L, Rotter M, Frank D, Yahiaoui S, …, Wichelhaus T, Hirsch A (2022)

Journal of medicinal chemistry 65 (5): 3913-3922DOI: 10.1021/acs.jmedchem.1c01755

Inhibition of Collagenase Q1 of Bacillus cereus as a Novel Antivirulence Strategy for the Treatment of Skin‐Wound Infections

Alhayek A, Khan E, Schönauer E, Däinghaus T, Shafiei R, Voos K, Han M, Ducho C, Posselt G, Wessler S, …, del Campo A, Hirsch A (2022)

Adv. Therap.DOI: 10.1002/adtp.202100222

Bacteriomimetic Liposomes Improve Antibiotic Activity of a Novel Energy-Coupling Factor Transporter Inhibitor

Drost M, Diamanti E, Fuhrmann K, Goes A, Shams A, Haupenthal J, Koch M, Hirsch A, Fuhrmann G (2022)

Pharmaceutics 14 (1)DOI: 10.3390/pharmaceutics14010004

Inhibitors of Pseudomonas aeruginosa virulence factor LasB

Ducho C, Hartmann R, Haupenthal J, Hirsch A, Kany A, Kaya C, Konstantinovic J, Voos K, Walter I, Yahiaoui S, …, Jumde R, Kiefer A (2022)

Patent A61K31/095; A61K31/10; A61K31/167; A61K31/4184; A61K31/426; A61K31/428; A61K31/4406; A61P31/04; C07C323/60; C07D213/74; C07D235/30; C07D277/46; C07D277/82; C07D333/36; C07F9/38; C07F9/40; (WO2022043322A1)

2021

N-Phenyl-3-Mercaptopropanamide Derivatives as Metallo-Beta-Lactamase Inhibitors for the Treatment of Bacterial Infections

Hartmann R, Konstantinovic J, Haupenthal J, Hirsch A, Kany A, Kaya C, Yahiaoui S, Wichelhaus T, Proschak E (2021)

Patent A61K31/5375; A61P31/04; C07C233/15; C07C233/25; C07C233/33; C07C233/43; C07C233/54; C07C319/02; C07C323/52; C07D295/22; (‌‌WO2021191219A1)

N-Phenyl-3-Mercaptopropanamide Derivatives as Metallo-Beta-Lactamase Inhibitors for the Treatment of Bacterial Infections

Hartmann R, Konstantinovic J, Haupenthal J, Hirsch A, Kany A, Kaya C, Yahiaoui S, Wichelhaus T, Proschak E (2021)

Patent A61K31/5375; A61P31/04; C07C233/15; C07C233/25; C07C233/33; C07C233/43; C07C233/54; C07C319/02; C07C323/52; C07D295/22; (‌‌WO2021191219A1)

Substrate-Inspired Fragment Merging and Growing Affords Efficacious LasB Inhibitors

Kaya C, Walter I, Yahiaoui S, Sikandar A, Alhayek A, Konstantinovic J, Kany A, Haupenthal J, Köhnke J, Hartmann R, Hirsch A (2021)

Angewandte Chemie (International ed. in English)DOI: 10.1002/anie.202112295

Targeting the energy-coupling factor (ECF) transporters: identification of new tool compounds

Diamanti E, Setyawati I, Bousis S, Souza P, mojas l, Swier l, Haupenthal J, Gibson P, Volz C, stanek w, …, slotboom d, Hirsch A (2021)

ChemRxivDOI: 10.26434/chemrxiv-2021-xq08b-v2

N-Aryl mercaptoacetamides as potential multi-target inhibitors of metallo-β-lactamases (MBLs) and the virulence factor LasB from Pseudomonas aeruginosa

Yahiaoui S, Voos K, Haupenthal J, Wichelhaus T, Frank D, Weizel L, Rotter M, Brunst S, Kramer J, Proschak E, Ducho C, Hirsch A (2021)

RSC Med. Chem.DOI: 10.1039/D1MD00187F

Phosphonate as a Stable Zinc‐Binding Group for “Pathoblocker” Inhibitors of Clostridial Collagenase H (ColH) (ChemMedChem 8/2021)

Voos K, Schönauer E, Alhayek A, Haupenthal J, Andreas A, Müller R, Hartmann R, Brandstetter H, Hirsch A, Ducho C (2021)

ChemMedChem 16 (8): 1198-1198DOI: 10.1002/cmdc.202100229

Hit-optimization using target-directed dynamic combinatorial chemistry: Development of inhibitors of the anti-infective target 1-deoxy-D-xylulose-5-phosphate synthase

Jumde R, Guadigni M, Gierse R, Alhayek A, Di Zhu, Hamid Z, Johannsen S, Elgaher W, Neusens P, Nehls C, …, Reiling N, Hirsch A (2021)

Chemical ScienceDOI: 10.1039/D1SC00330E

Assessment of the rules related to gaining activity against Gram-negative bacteria

Ropponen H, Diamanti E, Siemens A, Illarionov B, Haupenthal J, Fischer M, Rottmann M, Witschel M, Hirsch A (2021)

RSC Med. Chem.DOI: 10.1039/D0MD00409J

Phosphonate as Stable Zinc-binding Group for Inhibitors of Clostridial Collagenase H (ColH) as Pathoblocker Agents

Voos K, Schönauer E, Alhayek A, Haupenthal J, Andreas A, Müller R, Hartmann R, Brandstetter H, Hirsch A, Ducho C (2021)

ChemMedChemDOI: 10.1002/cmdc.202000994

2020

Evaluation of Bacterial RNA Polymerase Inhibitors in a Staphylococcus aureus-Based Wound Infection Model in SKH1 Mice

Haupenthal J, Kautz Y, Elgaher W, Pätzold L, Röhrig T, Laschke M, Tschernig T, Hirsch A, Molodtsov V, Murakami K, Hartmann R, Bischoff M (2020)

ACS infectious diseases 6 (10): 2573-2581DOI: 10.1021/acsinfecdis.0c00034

Rapid Discovery of Aspartyl Protease Inhibitors Using an Anchoring Approach

Konstantinidou M, Magari F, Sutanto F, Haupenthal J, Jumde R, Ünver M, Heine A, Camacho C, Hirsch A, Klebe G, Dömling A (2020)

ChemMedChem 15 (8): 680-684DOI: 10.1002/cmdc.202000024

Synthesis and Biological Evaluation of Novel 2-Substituted ­Analogues of (–)-Pentenomycin I

Zisopoulou S, Bousis S, Haupenthal J, Herrmann J, Müller R, Hirsch A, Komiotis D, Gallos J, Stathakis C (2020)

Synlett 31 (05): 475-481DOI: 10.1055/s-0039-1690772

N -Aryl-3-mercaptosuccinimides as Antivirulence Agents Targeting Pseudomonas aeruginosa Elastase and Clostridium Collagenases

Konstantinovic J, Yahiaoui S, Alhayek A, Haupenthal J, Schönauer E, Andreas A, Kany A, Müller R, Koehnke J, Berger F, …, Brandstetter H, Hirsch A (2020)

J. Med. Chem. 63 (15): 8359-8368DOI: 10.1021/acs.jmedchem.0c00584

2019

Spray-drying of inhalable, multifunctional formulations for the treatment of biofilms formed in cystic fibrosis

Lababidi N, Ofosu Kissi E, Elgaher W, Sigal V, Haupenthal J, Schwarz B, Hirsch A, Rades T, Schneider M (2019)

Journal of Controlled Release 314: 62-71DOI: 10.1016/j.jconrel.2019.10.038

From Wood to Tetrahydro-2-benzazepines in Three Waste-Free Steps: Modular Synthesis of Biologically Active Lignin-Derived Scaffolds

Elangovan S, Afanasenko A, Haupenthal J, Sun Z, Liu Y, Hirsch A, Barta K (2019)

ACS Cent. Sci. 5 (10): 1707-1716DOI: 10.1021/acscentsci.9b00781

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

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

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

2016

Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors

Elgaher W, Sharma K, Haupenthal J, Saladini F, Pires M, Real E, Mely Y, Hartmann R (2016)

Journal of medicinal chemistryDOI: 10.1021/acs.jmedchem.6b00730

2015

Inhalable Clarithromycin Microparticles for Treatment of Respiratory Infections

Dimer F, De Souza Carvalho-Wodarz C, Haupenthal J, Hartmann R, Lehr C (2015)

Pharmaceutical research 32 (12): 3850-3861DOI: 10.1007/s11095-015-1745-8

2014

Benzamidobenzoic acids as potent PqsD inhibitors for the treatment of Pseudomonas aeruginosa infections

Hinsberger S, Jong J, Groh M, Haupenthal J, Hartmann R (2014)

European journal of medicinal chemistry 76: 343-51DOI: 10.1016/j.ejmech.2014.02.014