Dr. Jörg Haupenthal
Über
Dr. Jörg Haupenthal ist Diplom-Biologe und Wissenschaftler in der Abteilung Wirkstoffdesign und Optimierung 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. Neben zahlreichen administrativen Aufgaben leitet er gemeinsam mit Prof. Dr. Anna K.H. Hirsch ein Projekt zur Entwicklung neuer LasB-Inhibitoren gegen Pseudomonas aeruginosa 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 Autor und Mitautor von mehr als 70 begutachteten wissenschaftlichen Publikationen – darunter in hochrangigen Zeitschriften wie Advanced Science, JACS, ACS Central Science und Angewandte Chemie – mit über 1.800 Zitierungen.
2025
Dipeptidic Phosphonates: Potent Inhibitors of Pseudomonas aeruginosa Elastase B Showing Efficacy in a Murine Keratitis Model
Kiefer A, Schütz C, Englisch C, Kolling D, Speicher S, Kany A, Shafiei R, Wadood N, Aljohmani A, Wirschem N, …, Haupenthal J, Hirsch A (2025)
Adv. Sci.DOI: 10.1002/advs.202411807
2024
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 (2024)
Angewandte Chemie (Weinheim an der Bergstrasse, Germany) 136 (4)DOI: 10.1002/ange.202308131
Development of Fragment-Based Inhibitors of the Bacterial Deacetylase LpxC with Low Nanomolar Activity
Mielniczuk S, Hoff K, Baselious F, Li Y, Haupenthal J, Kany A, Riedner M, Rohde H, Rox K, Hirsch A, …, Sippl W, Holl R (2024)
Journal of medicinal chemistry 67 (19): 17363-17391DOI: 10.1021/acs.jmedchem.4c01262
Spray drying of a zinc complexing agent for inhalation therapy of pulmonary fibrosis
Stella J, Abdelaal M, Kamal M, Shehu K, Alhayek A, Haupenthal J, Hirsch A, Schneider M (2024)
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences 202DOI: 10.1016/j.ejps.2024.106891
Expression and characterization of pantothenate energy-coupling factor transporters as an anti-infective drug target
Shams A, Bousis S, Diamanti E, Elgaher W, Zeimetz L, Haupenthal J, slotboom d, Hirsch A (2024)
Protein Sci. 33 (11)DOI: 10.1002/pro.5195
Target-Directed Dynamic Combinatorial Chemistry Affords Binders of Mycobacterium tuberculosis IspE
Braun-Cornejo M, Ornago C, Sonawane V, Haupenthal J, Kany A, Diamanti E, Jézéquel G, Reiling N, Blankenfeldt W, Maas P, Hirsch A (2024)
ACS omegaDOI: 10.1021/acsomega.4c05537
Dual inhibitors of Pseudomonas aeruginosa virulence factors LecA and LasB
Metelkina O, Konstantinovic J, Klein A, Shafiei R, Fares M, Alhayek A, Yahiaoui S, Elgaher W, Haupenthal J, Titz* A, Hirsch* A (2024)
Chem. Sci. 15DOI: 10.1039/D4SC02703E
Target repurposing unravels avermectins and derivatives as novel antibiotics inhibiting energy-coupling factor transporters (ECFTs)
Haupenthal J, Rafehi M, Kany A, Lespine A, Stefan K, Hirsch* A, Stefan* S (2024)
Arch. Pharm.DOI: 10.1002/ardp.202400267
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
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)
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
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
2017
Bacterial RNAP Inhibitors: Synthesis and Evaluation of Prodrugs of Aryl‐ureidothiophene‐carboxylic acids
Ruthenbeck A, Elgaher W, Haupenthal J, Hartmann R, Meier C (2017)
ChemistrySelect 2 (35): 11899-11905DOI: 10.1002/slct.201702574
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
Surface plasmon resonance--more than a screening technology: insights in the binding mode of σ70:core RNAP inhibitors
Hüsecken K, Hinsberger S, Elgaher W, Haupenthal J, Hartmann R (2014)
Future medicinal chemistry 6 (14): 1551-65DOI: 10.4155/fmc.14.105
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
2013
Expanding the scaffold for bacterial RNA polymerase inhibitors: design, synthesis and structure–activity relationships of ureido-heterocyclic-carboxylic acids
Elgaher W, Fruth M, Groh M, Haupenthal J, Hartmann R (2013)
RSC Adv 4 (5): 2177-2194DOI: 10.1039/C3RA45820B