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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)

Nat Rev Chem: 1-24DOI: 10.1038/s41570-021-00313-1

Improved broad-spectrum antibiotics against Gram-negative pathogens via darobactin biosynthetic pathway engineering

Groß S, Panter F, Pogorevc D, Seyfert C, Deckarm S, Bader C, Herrmann J, Müller R (2021)

Chemical ScienceDOI: 10.1039/d1sc02725e

In vivo and in vitro reconstitution of unique key steps in cystobactamid antibiotic biosynthesis

Groß S, Schnell B, Haack P, Auerbach D, Müller R (2021)

Nat Commun 12 (1)DOI: 10.1038/s41467-021-21848-3

The sandarazols are cryptic and structurally unique plasmid encoded toxins from a rare myxobacterium

Panter F, Bader C, Müller R (2021)

Angewandte Chemie (International ed. in English)DOI: 10.1002/anie.202014671

Citatronic Acid and Derivates thereof for use as a medicament

Pessler F., Chen F., Winterhoff M., Büssow K., Blankenfeldt W., Elgaher W. A. M., Hirsch A. K. H. (2021)

Patent (EP21202816.1)

Citatronic Acid and Derivates thereof for use as a medicament

Pessler F., Chen F., Winterhoff M., Büssow K., Blankenfeldt W., Elgaher W. A. M., Hirsch A. K. H. (2021)

Patent (EP21202816.1)

Design, synthesis, and biological evaluation of novel benzimidazole derivatives as sphingosine kinase 1 inhibitor

Khairat S, Omar M, Ragab F, Roy S, Turab Naqvi A, Abdelsamie A, Hirsch A, Galal S, Hassan M, El Diwani H (2021)

Archiv der Pharmazie 354 (9)DOI: 10.1002/ardp.202100080

Physiologically Based Pharmacokinetic/Pharmacodynamic Model for the Treatment of Dengue Infections Applied to the Broad Spectrum Antiviral Soraphen A

Rox K, Heyner M, Krull J, Harmrolfs K, Rinne V, Hokkanen J, Perez Vilaro G, Díez J, Müller R, Kröger A, Sugiyama Y, Brönstrup M (2021)

ACS Pharmacol. Transl. Sci.DOI: 10.1021/acsptsci.1c00078

Identification of N,N-arylalkyl-picolinamide derivatives targeting the RNA-binding protein HuR, by combining biophysical fragment-screening and molecular hybridization

Della Volpe S, Linciano P, Listro R, Tumminelli E, Amadio M, Bonomo I, Elgaher W, Adam S, Hirsch A, Boeckler F, …, Rossi D, Collina S (2021)

Bioorganic chemistry 116DOI: 10.1016/j.bioorg.2021.105305

Expanding the Myxochelin Natural Product Family by Nicotinic Acid Containing Congeners

Frank N, Széles M, Akone S, Rasheed S, Hüttel S, Frewert S, Hamed M, Herrmann J, Schuler S, Hirsch A, Müller R (2021)

Molecules 26 (16)DOI: 10.3390/molecules26164929

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

Crystalline sponge affinity screening: A fast tool for soaking condition optimization without the need of X-ray diffraction analysis

Rosenberger L, Essen C, Khutia A, Kühn C, Georgi K, Hirsch A, Hartmann R, Badolo L (2021)

European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences 164DOI: 10.1016/j.ejps.2021.105884

Non-Carbohydrate Glycomimetics as Inhibitors of Calcium(II)-Binding Lectins

Kuhaudomlarp S, Siebs E, Shanina E, Topin J, Joachim I, da Silva Figueiredo Celestino Gomes P, Varrot A, Rognan D, Rademacher C, Imberty A, Titz A (2021)

Angew. Chem. Int. Ed. 60 (15): 8104-8114DOI: 10.1002/anie.202013217

The exo-β-N-acetylmuramidase NamZ from Bacillus subtilis is the founding member of a family of exo-lytic peptidoglycan hexosaminidases

Müller M, Calvert M, Hottmann I, Kluj R, Teufel T, Balbuchta K, Engelbrecht A, Selim K, Xu Q, Borisova M, Titz A, Mayer C (2021)

The Journal of biological chemistry 296DOI: 10.1016/j.jbc.2021.100519

Sesbanimide R, a Novel Cytotoxic Polyketide Produced by Magnetotactic Bacteria

Awal R, Haack P, Bader C, Riese C, Schüler D, Müller R (2021)

mBio 12 (3)DOI: 10.1128/mBio.00591-21

Drug delivery to the inflamed intestinal mucosa- targeting technologies and human cell culture models for better therapies of IBD

Olga H, Shetab Boushehri Maryam A, Shalaby Karim S, Brigitta L, Alf L, Claus-Michael L (2021)

Advanced Drug Delivery ReviewsDOI: 10.1016/j.addr.2021.113828

Spray-dried lactose-leucine microparticles for pulmonary delivery of antimycobacterial nanopharmaceuticals

Thiyagarajan D, Huck B, Nothdurft B, Koch M, Rudolph D, Rutschmann M, Feldmann C, Hozsa C, Furch M, Besecke K, …, Loretz B, Lehr C (2021)

Drug delivery and translational research 11 (4): 1766-1778DOI: 10.1007/s13346-021-01011-7

Microbiota and cancer: In vitro and in vivo models to evaluate nanomedicines

Ladaycia A, Loretz B, Passirani C, Lehr C, Lepeltier E (2021)

Advanced Drug Delivery Reviews 170: 44-70DOI: 10.1016/j.addr.2020.12.015

Development and evaluation of a quality control system based on transdermal electrical resistance for skin barrier function in vitro

Knoth K, Zäh R, Veldung B, Burgio D, Wiegand B, Smola H, Bock U, Lehr C, Hittinger M, Groß H (2021)

Skin research and technology : official journal of International Society for Bioengineering and the Skin (ISBS) [and] International Society for Digital Imaging of Skin (ISDIS) [and] International Society for Skin Imaging (ISSI)DOI: 10.1111/srt.12998

Surfactant-Free Glibenclamide Nanoparticles: Formulation, Characterization and Evaluation of Interactions with Biological Barriers

Arrua E, Hartwig O, Ho D, Loretz B, Murgia X, Salomon C, Lehr C (2021)

Pharmaceutical research 38 (6): 1081-1092DOI: 10.1007/s11095-021-03056-2

Testing of aerosolized ciprofloxacin nanocarriers on cystic fibrosis airway cells infected with P. aeruginosa biofilms

Juntke J, Murgia X, Günday Türeli N, Türeli A, Thorn C, Schneider M, Schneider-Daum N, Souza Carvalho-Wodarz C, Lehr C (2021)

Drug delivery and translational research 11 (4): 1752-1765DOI: 10.1007/s13346-021-01002-8

Second-generation lung-on-a-chip with an array of stretchable alveoli made with a biological membrane

Zamprogno P, Wüthrich S, Achenbach S, Thoma G, Stucki J, Hobi N, Schneider-Daum N, Lehr C, Huwer H, Geiser T, Schmid R, Guenat O (2021)

Communications Biology 4 (1)DOI: 10.1038/s42003-021-01695-0

Drug delivery for fighting infectious diseases: a global perspective

Loretz B, Oh Y, Hudson S, Gu Z, Lehr C (2021)

Drug delivery and translational research 11 (4): 1316-1322DOI: 10.1007/s13346-021-01009-1

Fucosylated lipid nanocarriers loaded with antibiotics efficiently inhibit mycobacterial propagation in human myeloid cells

Durán V, Grabski E, Hozsa C, Becker J, Yasar H, Monteiro J, Costa B, Koller N, Lueder Y, Wiegmann B, …, Graalmann T, Kalinke U (2021)

Journal of controlled release : official journal of the Controlled Release Society 334: 201-212DOI: 10.1016/j.jconrel.2021.04.012

Tobramycin Liquid Crystal Nanoparticles Eradicate Cystic Fibrosis-Related Pseudomonas aeruginosa Biofilms

Thorn C, Carvalho-Wodarz C, Horstmann J, Lehr C, Prestidge C, Thomas N (2021)

Small (Weinheim an der Bergstrasse, Germany) 17 (24)DOI: 10.1002/smll.202100531

Decoding (patho-)physiology of the lung by advanced in vitro models for developing novel anti-infectives therapies

Montefusco-Pereira C, Carvalho-Wodarz C, Seeger J, Kloft C, Michelet R, Lehr C (2021)

Drug Discovery Today 26 (1): 148-163DOI: 10.1016/j.drudis.2020.10.016

Analysis and Optimization of Two Film-Coated Tablet Production Processes by Computer Simulation: A Case Study

Hering S, Schäuble N, Buck T, Loretz B, Rillmann T, Stieneker F, Lehr C (2021)

Processes 9 (1)DOI: 10.3390/pr9010067

Formulation and evaluation of transdermal nanogel for delivery of artemether

Nnamani P, Ugwu A, Nnadi O, Kenechukwu F, Ofokansi K, Attama A, Lehr C (2021)

Drug delivery and translational research 11 (4): 1655-1674DOI: 10.1007/s13346-021-00951-4

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

A pulmonary mucus surrogate for investigating antibiotic permeation and activity against Pseudomonas aeruginosa biofilms

Frisch S, Boese A, Huck B, Horstmann J, Ho D, Schwarzkopf K, Murgia X, Loretz B, Souza Carvalho-Wodarz C, Lehr C (2021)

The Journal of antimicrobial chemotherapy 76 (6): 1472-1479DOI: 10.1093/jac/dkab068

A Custom-Made Device for Reproducibly Depositing Pre-metered Doses of Nebulized Drugs on Pulmonary Cells in vitro

Horstmann J, Thorn C, Carius P, Graef F, Murgia X, Souza Carvalho-Wodarz C, Lehr C (2021)

Frontiers in Bioengineering and Biotechnology 9DOI: 10.3389/fbioe.2021.643491

Extracellular vesicles as antigen carriers for novel vaccination avenues

Mehanny M, Lehr C, Fuhrmann G (2021)

Advanced Drug Delivery Reviews 173: 164-180DOI: 10.1016/j.addr.2021.03.016

Extracellular vesicles as novel assay tools to study cellular interactions of anti-infective compounds - A perspective

Richter R, Lehr C (2021)

Advanced Drug Delivery Reviews 173: 492-503DOI: 10.1016/j.addr.2021.04.010

Disease Models: Lung Models for Testing Drugs Against Inflammation and Infection

Carius P, Horstmann J, Souza Carvalho-Wodarz C, Lehr C (2021)

Handbook of experimental pharmacology 265: 157-186DOI: 10.1007/164_2020_366

Eap-functionalized liposomes as a bioinspired delivery system for oral delivery of colistin to treat intracellular Salmonella infection

Menina S (2021)


Zebrafish: An Attractive Model to Study Staphylococcus aureus Infection and Its Use as a Drug Discovery Tool

Rasheed S, Fries F, Müller R, Herrmann J (2021)

Pharmaceuticals 14 (6)DOI: 10.3390/ph14060594

“Clicking“ fragment leads to novel dual-binding cholinesterase inhibitors

Moleda Z, Zawadzka A, Czarnocki Z, Monjas L, Hirsch A, Budzianowski A, Maurin J (2021)

Bioorg Med ChemDOI: 10.1016/j.bmc.2021.116269

Structure and biosynthesis of sorangipyranone - A new γ-dihydropyrone from the myxobacterial strain MSr12020

Okoth D, Hug J, Mándi A, Kurtán T, Garcia R, Müller R (2021)

Journal of Industrial Microbiology & BiotechnologyDOI: 10.1093/jimb/kuab029

Front Cover: 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

miRMaster 2.0: multi-species non-coding RNA sequencing analyses at scale

Fehlmann T, Kern F, Laham O, Backes C, Solomon J, Hirsch P, Volz C, Müller R, Keller A (2021)

Nucleic Acids ResDOI: 10.1093/nar/gkab268

Search for the Active Ingredients from a 2-Aminothiazole DMSO Stock Solution with Antimalarial Activity

Ropponen H, Bader C, Diamanti E, Illarionov B, Rottmann M, Fischer M, Witschel M, Müller R, Hirsch A (2021)

ChemMedChemDOI: 10.1002/cmdc.202100067

Synergizing the potential of bacterial genomics and metabolomics to find novel antibiotics

Panter F, Bader C, Müller R (2021)

Chemical ScienceDOI: 10.1039/d0sc06919a

Targeting cellular fatty acid synthesis limits T helper and innate lymphoid cell function during intestinal inflammation and infection

Mamareli P, Kruse F, Lu C, Guderian M, Floess S, Rox K, Allan D, Carlyle J, Brönstrup M, Müller R, …, Sparwasser T, Lochner M (2021)

Mucosal Immunol. 14 (1): 164-176DOI: 10.1038/s41385-020-0285-7

Ribosome-Targeting Antibiotics Impair T Cell Effector Function and Ameliorate Autoimmunity by Blocking Mitochondrial Protein Synthesis

Almeida L, Dhillon-LaBrooy A, Castro C, Adossa N, Carriche G, Guderian M, Lippens S, Dennerlein S, Hesse C, Lambrecht B, …, Moita L, Sparwasser T (2021)

Immunity 54 (1): 68-83DOI: 10.1016/j.immuni.2020.11.001

Stimulation of Probiotic Bacteria Induces Release of Membrane Vesicles with Augmented Anti-inflammatory Activity

Müller L, Kuhn T, Koch M, Fuhrmann G (2021)

ACS Appl. Bio Mater.DOI: 10.1021/acsabm.0c01136

Mastering the Gram-Negative Bacterial Barrier - Chemical Approaches to Increase Bacterial Bioavailability of Antibiotics

Ropponen H, Richter R, Hirsch A, Lehr C (2021)

Advanced Drug Delivery ReviewsDOI: 10.1016/j.addr.2021.02.014

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

Natural products in drug discovery: advances and opportunities

Atanasov A, Zotchev S, Dirsch V, Supuran C (2021)

Nature reviews. Drug discoveryDOI: 10.1038/s41573-020-00114-z

Enhancing glycan stability via site-selective fluorination: modulating substrate orientation by molecular design

Axer A, Jumde R, Adam S, Faust A, Schäfers M, Fobker M, Koehnke J, Hirsch A, Gilmour R (2021)

Chem. Sci. 12 (4): 1286-1294DOI: 10.1039/D0SC04297H

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

Inhibitors of Pseudomonas aeruginosa virulence factor LasB

Kaya, C., Konstantinovic, J., Voos, K., Walter, I., Kany, A.M., …, Hirsch, Anna K. H. (2021)

Patent (EP20192608.6)

Expanding the Scope of Detectable Microbial Natural Products by Complementary Analytical Methods and Cultivation Systems

Bader C, Haack P, Panter F, Krug D, Müller R (2021)

Journal of natural productsDOI: 10.1021/acs.jnatprod.0c00942

Identification of a 1-deoxy-D-xylulose-5-phosphate synthase (DXS) mutant with improved crystallographic properties

Gierse R, Reddem E, Alhayek A, Baitinger D, Hamid Z, Jakobi H, Laber B, Lange G, Hirsch A, Groves (2021)

Biochemical and Biophysical Research Communications 539DOI: 10.1016/j.bbrc.2020.12.069

Kibdelosporangium persicum sp. nov., a new member of the Actinomycetes from a hot desert in Iran

Safaei N, Nouioui I, Mast Y, Zaburannyi N, Rohde M, Schumann P, Müller R, Wink J (2021)

Int J Syst Evol MicrobiolDOI: 10.1099/ijsem.0.004625


Supercritical Fluid Extraction Enhances Discovery of Secondary Metabolites from Myxobacteria

Bader C, Neuber M, Panter F, Krug D, Müller R (2020)

Analytical chemistryDOI: 10.1021/acs.analchem.0c02995

An ambruticin-sensing complex modulates Myxococcus xanthus development and mediates myxobacterial interspecies communication

Marcos-Torres F, Volz C, Müller R (2020)

Nat Commun 11 (1)DOI: 10.1038/s41467-020-19384-7

PLGA nanocapsules improve the delivery of clarithromycin to kill intracellular Staphylococcus aureus and Mycobacterium abscessus

Anversa Dimer F, Souza Carvalho-Wodarz C, Goes A, Cirnski K, Herrmann J, Schmitt V, Pätzold L, Abed N, Rossi C, Bischoff M, …, Müller R, Lehr C (2020)

Nanomedicine : nanotechnology, biology, and medicine 24DOI: 10.1016/j.nano.2019.102125

Protein‐Templated Hit Identification via an Ugi Four‐Component Reaction

Mancini F, Unver M, Elgaher W, Jumde V, Alhayek A, Lukat P, Herrmann J, Witte M, Köck M, Blankenfeldt W, Müller R, Hirsch A (2020)

Chem. Eur. J.DOI: 10.1002/chem.202002250

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

SphereCon-a method for precise estimation of residue relative solvent accessible area from limited structural information

Gress A, Kalinina O (2020)

Bioinformatics (Oxford, England) 36 (11): 3372-3378DOI: 10.1093/bioinformatics/btaa159

Probiomimetics-Novel Lactobacillus-Mimicking Microparticles Show Anti-Inflammatory and Barrier-Protecting Effects in Gastrointestinal Models

Kuhn T, Koch M, Fuhrmann G (2020)

Small (Weinheim an der Bergstrasse, Germany) 16 (40)DOI: 10.1002/smll.202003158

Novel PqsR Inverse Agonists

Hamed, M., Ahmed, S. A., Empting. M., Schütz, C., Hartmann, R. W., Röhrig, …, Hirsch, A. K. H. (2020)

Patent (EP20150119)

Novel PqsR Inverse Agonists

Hamed, M., Ahmed, S. A., Empting. M., Schütz, C., Hartmann, R. W., Röhrig, …, Hirsch, Anna K. H. (2020)

Patent (EP20150119)

Streptococcal Extracellular Membrane Vesicles Are Rapidly Internalized by Immune Cells and Alter Their Cytokine Release

Mehanny M, Koch M, Lehr C, Fuhrmann G (2020)

Frontiers in immunology 11DOI: 10.3389/fimmu.2020.00080

Dual-function chromogenic screening-based CRISPR/Cas9 genome editing system for actinomycetes

Wang Q, Xie F, Tong Y, Habisch R, Yang B, Zhang L, Müller R, Fu C (2020)

Applied Microbiology and Biotechnology 104 (1): 225-239DOI: 10.1007/s00253-019-10223-4

Tobacco Smoke and Inhaled Drugs Alter Expression and Activity of Multidrug Resistance-Associated Protein-1 (MRP1) in Human Distal Lung Epithelial Cells in vitro

Selo M, Delmas A, Springer L, Zoufal V, Sake J, Clerkin C, Huwer H, Schneider-Daum N, Lehr C, Nickel S, Langer O, Ehrhardt C (2020)

Frontiers in Bioengineering and Biotechnology 8DOI: 10.3389/fbioe.2020.01030

Towards a Continuous Manufacturing Process of Protein-Loaded Polymeric Nanoparticle Powders

Schiller S, Hanefeld A, Schneider M, Lehr C (2020)

AAPS PharmSciTech 21 (7)DOI: 10.1208/s12249-020-01814-w

A hydrogel-based in vitro assay for the fast prediction of antibiotic accumulation in Gram-negative bacteria

Richter R, Kamal M, García-Rivera M, Kaspar J, Junk M, Elgaher W, Srikakulam S, Gress A, Beckmann A, Grißmer A, …, Schneider-Daum N, Lehr C (2020)

Materials today. Bio 8DOI: 10.1016/j.mtbio.2020.100084

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

Modulating the Barrier Function of Human Alveolar Epithelial (hAELVi) Cell Monolayers as a Model of Inflammation

Metz J, Wiegand B, Schnur S, Knoth K, Schneider-Daum N, Groß H, Croston G, Reinheimer T, Lehr C, Hittinger M (2020)

Alternatives to laboratory animals : ATLA 48 (5-6): 252-267DOI: 10.1177/0261192920983015

Spray-dried multidrug particles for pulmonary co-delivery of antibiotics with N-acetylcysteine and curcumin-loaded PLGA-nanoparticles

Lababidi N, Montefusco-Pereira C, Souza Carvalho-Wodarz C, Lehr C, Schneider M (2020)

European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V 157: 200-210DOI: 10.1016/j.ejpb.2020.10.010

Synthesis and Biopharmaceutical Characterization of Amphiphilic Squalenyl Derivative Based Versatile Drug Delivery Platform

Ho D, Christmann R, Murgia X, Rossi C, Frisch S, Koch M, Schaefer U, Loretz B, Desmaele D, Couvreur P, Lehr C (2020)

Frontiers in chemistry 8DOI: 10.3389/fchem.2020.584242

Tofacitinib Loaded Squalenyl Nanoparticles for Targeted Follicular Delivery in Inflammatory Skin Diseases

Christmann R, Ho D, Wilzopolski J, Lee S, Koch M, Loretz B, Vogt T, Bäumer W, Schaefer U, Lehr C (2020)

Pharmaceutics 12 (12)DOI: 10.3390/pharmaceutics12121131

Predicting Bacterial Accumulation of Anti-infectives by Measuring Permeability across Surrogates of the Gram-negative Bacterial Cell Envelope

Richter R (2020)


Predicting Bacterial Accumulation of Anti-infectives by Measuring Permeability across Surrogates of the Gram-negative Bacterial Cell Envelope

Richter R (2020)


Semisynthesis and biological evaluation of amidochelocardin derivatives as broad-spectrum antibiotics

Grandclaudon C, Birudukota N, Elgaher W, Jumde R, Yahiaoui S, Arisetti N, Hennessen F, Hüttel S, Stadler M, Herrmann J, …, Hirsch A, Brönstrup M (2020)

European journal of medicinal chemistry 188DOI: 10.1016/j.ejmech.2019.112005

Discovery of Small-Molecule Stabilizers of 14-3-3 Protein-Protein Interactions via Dynamic Combinatorial Chemistry

Hartman A, Elgaher W, Hertrich N, Andrei S, Ottmann C, Hirsch A (2020)

ACS medicinal chemistry letters 11 (5): 1041-1046DOI: 10.1021/acsmedchemlett.9b00541

Characterization of bromelain indicates a molar excess of inhibitor vs. enzyme molecules, a Jacalin-like lectin and Maillard reaction products

Gross P, Seelert H, Meiser P, Müller R (2020)

Journal of pharmaceutical and biomedical analysis 181DOI: 10.1016/j.jpba.2019.113075

Synthetic and Biological Studies on New Urea and Triazole Containing Cystobactamid Derivatives

Planke T, Cirnski K, Herrmann J, Müller R, Kirschning A (2020)

Chem. Eur. J. 26 (19): 4289-4296DOI: 10.1002/chem.201904073

The glucocorticoid-induced leucine zipper mediates statin-induced muscle damage

Hoppstädter J, Valbuena Perez J, Linnenberger R, Dahlem C, Legroux T, Hecksteden A, Tse W, Flamini S, Andreas A, Herrmann J, …, Bruscoli S, Kiemer A (2020)

FASEB j. 34 (3): 4684-4701DOI: 10.1096/fj.201902557RRR

Myxobacteria-Derived Outer Membrane Vesicles: Potential Applicability Against Intracellular Infections

Goes A, Lapuhs P, Kuhn T, Schulz E, Richter R, Panter F, Dahlem C, Koch M, Garcia R, Kiemer A, Müller R, Fuhrmann G (2020)

Cells 9 (1)DOI: 10.3390/cells9010194

Toxicokinetics and toxicodynamics of the fentanyl homologs cyclopropanoyl-1-benzyl-4´-fluoro-4-anilinopiperidine and furanoyl-1-benzyl-4-anilinopiperidine

Gampfer T, Wagmann L, Park Y, Cannaert A, Herrmann J, Fischmann S, Westphal F, Müller R, Stove C, Meyer M (2020)

Arch. Toxicol. 94 (6): 2009-2025DOI: 10.1007/s00204-020-02726-1

The ROK like protein of Myxococcus xanthus DK1622 acts as a pleiotropic transcriptional regulator for secondary metabolism

Izzat S, Rachid S, Ajdidi A, El-Nakady Y, Liu X, Ye B, Müller R (2020)

J. Biotechnol. 311: 25-34DOI: 10.1016/j.jbiotec.2020.02.005

Cystobactamid 507: Concise Synthesis, Mode of Action, and Optimization toward More Potent Antibiotics

Elgaher W, Hamed M, Baumann S, Herrmann J, Siebenbürger L, Krull J, Cirnski K, Kirschning A, Brönstrup M, Müller R, Hartmann R (2020)

Chem. Eur. J. 26 (32): 7219-7225DOI: 10.1002/chem.202000117

Dual-Seq reveals genome and transcriptome of Caedibacter taeniospiralis, obligate endosymbiont of Paramecium

Pirritano M, Zaburannyi N, Grosser K, Gasparoni G, Müller R, Simon M, Schrallhammer M (2020)

Sci. Rep. 10 (1)DOI: 10.1038/s41598-020-65894-1

Thioholgamide A, a New Anti-Proliferative Anti-Tumor Agent, Modulates Macrophage Polarization and Metabolism

Dahlem C, Siow W, Lopatniuk M, Tse W, Kessler S, Kirsch S, Hoppstädter J, Vollmar A, Müller R, Luzhetskyy A, Bartel K, Kiemer A (2020)

Cancers 12 (5)DOI: 10.3390/cancers12051288

Human microbial metabolite mimicry as a strategy to expand the chemical space of potential drugs

Li H, Ranhotra H, Mani S, Dvorák Z, Sokol H, Müller R (2020)

Drug Discov. Today 25 (9): 1575-1579DOI: 10.1016/j.drudis.2020.06.007

ClbR Is the Key Transcriptional Activator of Colibactin Gene Expression in Escherichia coli

Wallenstein A, Rehm N, Brinkmann M, Selle M, Bossuet-Greif N, Sauer D, Bunk B, Spröer C, Wami H, Homburg S, …, Müller R, Dobrindt U (2020)

mSphere 5 (4)DOI: 10.1128/mSphere.00591-20

Amidochelocardin Overcomes Resistance Mechanisms Exerted on Tetracyclines and Natural Chelocardin

Hennessen F, Miethke M, Zaburannyi N, Loose M, Lukežic T, Bernecker S, Hüttel S, Jansen R, Schmiedel J, Fritzenwanker M, …, Herrmann J, Müller R (2020)

Antibiotics 9 (9)DOI: 10.3390/antibiotics9090619

How to Study the Metabolism of New Psychoactive Substances for the Purpose of Toxicological Screenings-A Follow-Up Study Comparing Pooled Human Liver S9, HepaRG Cells, and Zebrafish Larvae

Wagmann L, Frankenfeld F, Park Y, Herrmann J, Fischmann S, Westphal F, Müller R, Flockerzi V, Meyer M (2020)

Frontiers in chemistry 8DOI: 10.3389/fchem.2020.00539

Natural Products Impacting DNA Methyltransferases and Histone Deacetylases

Akone S, Ntie-Kang F, Stuhldreier F, Ewonkem M, Noah A, Mouelle S, Müller R (2020)

Frontiers in pharmacology 11DOI: 10.3389/fphar.2020.00992

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

Editorial: Mechanisms of Prokaryotic Predation

Whitworth D, Jurkevitch E, Pérez J, Fuhrmann G, Koval S (2020)

Frontiers in microbiology 11DOI: 10.3389/fmicb.2020.02071

Heterologous expression of the atypical tetracycline chelocardin reveals the full set of genes required for its biosynthesis

Lukežic T, Pikl Š, Zaburannyi N, Remškar M, Petkovic H, Müller R (2020)

Microb. Cell Fact. 19 (1)DOI: 10.1186/s12934-020-01495-x

François Diederich – In Memoriam**

Fraser Hof, Hirsch A (2020)

ChemMedChemDOI: 10.1002/cmdc.202000920

Frontispiece: Protein‐Templated Hit Identification through an Ugi Four‐Component Reaction

Federica Mancini, M. Yagiz Unver, Walid A. M. Elgaher, Varsha R. Jumde, Alaa Alhayek, Peer Lukat, Jennifer Herrmann, Martin D. Witte, Matthias Köck, Wulf Blankenfeldt, Rolf Müller, Hirsch A (2020)

Chemistry – A European Journal 26 (64)DOI: 10.1002/chem.202086462

Corallopyronin A for short-course anti-wolbachial, macrofilaricidal treatment of filarial infections

Schiefer A, Hübner M, Krome A, Lämmer C, Ehrens A, Aden T, Koschel M, Neufeld H, Chaverra-Muñoz L, Jansen R, …, Pfarr K, Hoerauf A (2020)

PLoS Negl. Trop. Dis. 14 (12)DOI: 10.1371/journal.pntd.0008930

Leben und Überleben im Boden: Myxococcus xanthus ist Mikrobe des Jahres 2020

Volz C, Krug D, Müller R (2020)

Biol. Unserer Zeit 50 (6): 424-432DOI: 10.1002/biuz.202010721

The antibiotic sorangicin A inhibits promoter DNA unwinding in a Mycobacterium tuberculosis rifampicin-resistant RNA polymerase

Lilic M, Chen J, Boyaci H, Braffman N, Hubin E, Herrmann J, Müller R, Mooney R, Landick R, Darst S, Campbell E (2020)

Proc. Natl. Acad. Sci. U.S.A.DOI: 10.1073/pnas.2013706117

Metabolic Profiling to Determine Bactericidal or Bacteriostatic Effects of New Natural Products using Isothermal Microcalorimetry

Cirnski K, Coetzee J, Herrmann J, Müller R (2020)

J. Vis. Exp. (164)DOI: 10.3791/61703

Protein-observed 19F NMR of LecA from Pseudomonas aeruginosa

Shanina E, Siebs E, Zhang H, Silva D, Joachim I, Titz A, Rademacher C (2020)

GlycobiologyDOI: 10.1093/glycob/cwaa057

Directing Drugs to Bugs: Antibiotic-Carbohydrate Conjugates Targeting Biofilm-Associated Lectins of Pseudomonas aeruginosa

Meiers J, Zahorska E, Röhrig T, Hauck D, Wagner S, Titz A (2020)

Journal of medicinal chemistry 63 (20): 11707-11724DOI: 10.1021/acs.jmedchem.0c00856

An extended catalogue of tandem alternative splice sites in human tissue transcriptomes

Mironov A, Denisov S, Gress A, Kalinina O, Pervouchine D (2020)

BookDOI: 10.1101/2020.09.11.292722

The bottromycin epimerase BotH defines a group of atypical α/β-hydrolase-fold enzymes

Sikandar A, Franz L, Adam S, Santos-Aberturas J, Horbal L, Luzhetskyy A, Truman A, Kalinina O, Koehnke J (2020)

Nat Chem Biol 16 (9): 1013-1018DOI: 10.1038/s41589-020-0569-y

DIGGER: exploring the functional role of alternative splicing in protein interactions

Louadi Z, Yuan K, Gress A, Tsoy O, Kalinina O, Baumbach J, Kacprowski T, List M (2020)

Nucleic Acids ResDOI: 10.1093/nar/gkaa768

Frequent subgraph mining for biologically meaningful structural motifs

Keller S, Miettinen P, Kalinina O (2020)

BookDOI: 10.1101/2020.05.14.095695

Drug Administration Routes Impact the Metabolism of a Synthetic Cannabinoid in the Zebrafish Larvae Model

Park Y, Meyer M, Müller R, Herrmann J (2020)

Molecules 25 (19)DOI: 10.3390/molecules25194474

2-Hydroxysorangiadenosine: Structure and Biosynthesis of a Myxobacterial Sesquiterpene-Nucleoside

Okoth D, Hug J, Garcia R, Spröer C, Overmann J, Müller R (2020)

Molecules (Basel, Switzerland) 25 (11)DOI: 10.3390/molecules25112676

Biosynthesis of Cittilins, Unusual Ribosomally Synthesized and Post-translationally Modified Peptides from Myxococcus xanthus

Hug J, Dastbaz J, Adam S, Revermann O, Koehnke J, Krug D, Müller R (2020)

ACS chemical biology 15 (8): 2221-2231DOI: 10.1021/acschembio.0c00430

7-Hydroxycoumarins are Affinity-based Fluorescent Probes for Competitive Binding Studies of Macrophage Migration Inhibitory Factor

Xiao Z, Chen D, Song S, van der Vlag R, van der Wouden P, van Merkerk R, Cool R, Hirsch A, Melgert B, Quax W, Poelarends G, Dekker F (2020)

Journal of medicinal chemistryDOI: 10.1021/acs.jmedchem.0c01160

Polymer-Cargo-Complexes compremising cross-linked copolymers and cargo molecules

Lee S, Loretz B, Lehr C, Hirsch A (2020)


N-Aryl Mercaptopropionamides as inhibitors of Metallo-ß-Lactamases

Yahiaoui, S., Kaya, C., Kany, A. M., Haupenthal, J., Wichelhaus, T., …, Hirsch, Anna K. H. (2020)

Patent (EP20164855.7)

Advancing human in vitro pulmonary disease models in preclinical research: opportunities for lung-on-chips

Artzy-Schnirman A, Lehr C, Sznitman J (2020)

Expert Opinion on Drug Delivery 17 (5): 621-625DOI: 10.1080/17425247.2020.1738380

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

Itaconic Acid Increases the Efficacy of Tobramycin against Pseudomonas aeruginosa Biofilms

Ho D, Rossi C, Loretz B, Murgia X, Lehr C (2020)

Pharmaceutics 12 (8)DOI: 10.3390/pharmaceutics12080691

Safety assessment of excipients (SAFE) for orally inhaled drug products

Metz J, Scharnowske L, Hans F, Schnur S, Knoth K, Zimmer H, Limberger M, Groß H, Lehr C, Hittinger M (2020)

ALTEX 37 (2): 275-286DOI: 10.14573/altex.1910231

P. aeruginosa Infected 3D Co-Culture of Bronchial Epithelial Cells and Macrophages at Air-Liquid Interface for Preclinical Evaluation of Anti-Infectives

Montefusco-Pereira C, Horstmann J, Ebensen T, Beisswenger C, Bals R, Guzmán C, Schneider-Daum N, Carvalho-Wodarz C, Lehr C (2020)

Journal of visualized experiments : JoVE (160)DOI: 10.3791/61069

Nanoparticle Targeting to Scalp Hair Follicles: New Perspectives for a Topical Therapy for Alopecia Areata

Christmann R, Thomas C, Jager N, Raber A, Loretz B, Schaefer U, Tschernig T, Vogt T, Lehr C (2020)

The Journal of investigative dermatology 140 (1): 243-246DOI: 10.1016/j.jid.2019.05.028

Design and in vitro characterization of multistage silicon-PLGA budesonide particles for inflammatory bowel disease

Leonard F, Srinivasan S, Liu X, Collnot E, Ferrari M, Lehr C, Godin B (2020)

European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V 151: 61-72DOI: 10.1016/j.ejpb.2020.03.020

pH-Dependent morphology and optical properties of lysine-derived molecular biodynamers

Lee S, Kaya C, Jang H, Koch M, Loretz B, Buhler E, Lehr C, Hirsch A (2020)

Mater. Chem. Front. 4 (3): 905-909DOI: 10.1039/C9QM00651F

Inhalationstoxizität von Nanopartikeln // The role of alveolar macrophages in biokinetics and biological effects of inhaled nanoparticles

Koltermann-Jülly J (2020)

BookDOI: 10.22028/D291-31034

3D air-liquid interface culture of Cystic Fibrosis bronchial epithelia, macrophages and P. aeruginosa to assess host-pathogen interaction and drug efficacy

Montefusco C, Montefusco-Pereira C (2020)

BookDOI: 10.22028/D291-31815

Rapid Discovery of Aspartyl Protease Inhibitors Using an Anchoring Approach

Markella Konstantinidou, Francesca Magari, Fandi Sutanto, Jörg Haupenthal, Varsha R. Jumde, M. Yagiz Ünver, Andreas Heine, Carlos Jamie Camacho, Hirsch A, Gerhard Klebe, Alexander Dömling (2020)

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

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

Optimized Inhibitors of MDM2 via an Attempted Protein‐Templated Reductive Amination

Vlag R, Yagiz Unver M, Felicetti T, Twarda-Clapa A, Kassim F, Ermis C, Neochoritis C, Musielak B, Labuzek B, Dömling A, Holak T, Hirsch A (2020)

ChemMedChem 15 (4): 370-375DOI: 10.1002/cmdc.201900574

Discovery of Antibacterial Agents Inhibiting the Energy-Coupling Factor (ECF) Transporters by Structure-Based Virtual Screening

Diamanti E, Setyawati I, Bousis S, mojas l, Swier l, Haupenthal J, Gibson P, Volz C, stanek w, Jaeger m, …, slotboom d, Hirsch A (2020)

BookDOI: 10.26434/chemrxiv.11728710.v1

Validating the 1,2-Difluoro Motif As a Hybrid Bioisostere of CF3 and Et Using Matrix Metalloproteinases As Structural Probes

Erdeljac N, Thiehoff C, Jumde R, Daniliuc C, Höppner S, Faust A, Hirsch A, Gilmour R (2020)

Journal of medicinal chemistry 63 (11): 6225-6237DOI: 10.1021/acs.jmedchem.0c00648

BOPC1 Enantiomers Preparation and HuR Interaction Study. From Molecular Modeling to a Curious DEEP-STD NMR Application

Della Volpe S, Listro R, Parafioriti M, Di Giacomo M, Rossi D, Ambrosio F, Costa G, Alcaro S, Ortuso F, Hirsch A, Vasile F, Collina S (2020)

ACS medicinal chemistry letters 11 (5): 883-888DOI: 10.1021/acsmedchemlett.9b00659

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

Flotillin-mediated membrane fluidity controls peptidoglycan synthesis and MreB movement

Zielinska A, Savietto A, Sousa Borges A, Martinez D, Berbon M, Roelofsen J, Hartman A, Boer R, van der Klei I, Hirsch A, …, Bramkamp M, Scheffers D (2020)

eLife 9DOI: 10.7554/eLife.57179

Potential Dental Biofilm Inhibitors: Dynamic Combinatorial Chemistry Affords Sugar-Based Molecules that Target Bacterial Glucosyltransferase

Hartman A, Jumde V, Elgaher W, Te Poele E, Dijkhuizen L, Hirsch A (2020)

ChemMedChemDOI: 10.1002/cmdc.202000222

A rapid synthesis of low-nanomolar divalent LecA inhibitors in four linear steps from d -galactose pentaacetate

Zahorska E, Kuhaudomlarp S, Minervini S, Yousaf S, Lepsik M, Kinsinger T, Hirsch A, Imberty A, Titz A (2020)

Chem. Commun. 56 (62): 8822-8825DOI: 10.1039/d0cc03490h

Resistance-associated substitutions in patients with chronic hepatitis C virus genotype 4 infection

Dietz J, Kalinina O, Vermehren J, Peiffer K, Matschenz K, Buggisch P, Niederau C, Schattenberg J, Müllhaupt B, Yerly S, …, Welsch C, Sarrazin C (2020)

J. Viral Hepat.DOI: 10.1111/jvh.13322.

Non-active site mutants of HIV-1 protease influence resistance and sensitisation towards protease inhibitors

Bastys T, Gapsys V, Walter H, Heger E, Doncheva N, Kaiser R, Groot B, Kalinina O (2020)

Retrovirology 17 (1)DOI: 10.1186/s12977-020-00520-6

A shift of dynamic equilibrium between the KIT active and inactive states causes drug resistance

Srikakulam S, Bastys T, Kalinina O (2020)

ProteinsDOI: 10.1002/prot.25963

Synthetic studies of cystobactamids as antibiotics and bacterial imaging carriers lead to compounds with high in vivo efficacy

Testolin G, Cirnski K, Rox K, Prochnow H, Fetz V, Grandclaudon C, Mollner T, Baiyoumy A, Ritter A, Leitner C, …, Müller R, Brönstrup M (2020)

Chemical Science 11 (5): 1316-1334DOI: 10.1039/C9SC04769G

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

New PqsR Inverse Agonists

Schütz, C., Emmpting, M., Ahmed, A., Hamed, M., Hartmann, R. W., …, Hirsch, Anna K. H. (2020)

Patent (EP 20150104.6-1110)

Coupling quaternary ammonium surfactants to the surface of liposomes improves both antibacterial efficacy and host cell biocompatibility

Montefusco-Pereira C, Formicola B, Goes A, Re F, Marrano C, Mantegazza F, Carvalho-Wodarz C, Fuhrmann G, Caneva E, Nicotra F, Lehr C, Russo L (2020)

European Journal of Pharmaceutics and Biopharmaceutics 149: 12-20DOI: 10.1016/j.ejpb.2020.01.013

Liver-derived extracellular vesicles: A cell by cell overview to isolation and characterization practices

Zivko C, Fuhrmann G, Luciani P (2020)

Biochimica et Biophysica Acta - General Subjects 1865 (4)DOI: 10.1016/j.bbagen.2020.129559

Diffusion and transport of extracellular vesicles

Fuhrmann G (2020)

Nature Nanotechnology 15 (3): 168-169DOI: 10.1038/s41565-020-0651-3

Expression, Purification, and Functional Characterization of Tectonin 2 from Laccaria bicolor: A Six-Bladed Beta-Propeller Lectin Specific for O-Methylated Glycans

Wohlschlager T, Titz A, Künzler M, Varrot A (2020)

Methods Mol Biol 2132: 669-682DOI: 10.1007/978-1-0716-0430-4_58

Bacteria as genetically programmable producers of bioactive natural products

Hug J, Krug D, Müller R (2020)

Nat. rev. chem. 4 (4): 172-193DOI: 10.1038/s41570-020-0176-1

Host Development for Heterologous Expression and Biosynthetic Studies of Myxobacterial Natural Products

Hug J, Müller R (2020)

In pressDOI: 10.1016/B978-0-12-409547-2.14818-8

Myxobakterielle Naturstofffabriken

Krug D, Garcia R, Müller R (2020)

Biospektrum 26 (1): 32-36DOI: 10.1007/s12268-020-1334-1

Hot EVs – how temperature affects extracellular vesicles

Schulz E, Karagianni A, Koch M, Fuhrmann G (2020)

European Journal of Pharmaceutics and Biopharmaceutics 146: 55-63DOI: 10.1016/j.ejpb.2019.11.010

In depth natural product discovery - Myxobacterial strains that provided multiple secondary metabolites

Bader C, Panter F, Müller R (2020)

Biotechnol Adv. 39DOI: 10.1016/j.biotechadv.2019.107480