
Dr Alexander Kiefer
About
Having completed his PhD under the supervision of Prof. Uli Kazmaier at Saarland University, Alexander has honed skills in both classic total synthesis and medicinal chemistry-approaches to obtained cyclomarins with improved antimicrobial activities. During his short postdoctoral stay at Aalto University in Finland under the guidance of Prof. Dr. Jan Deska, he shifted from classical total synthesis to chemoenzymatic synthesis, focusing on the structurally unique angiopterlactone B. He successfully developed an efficient chemo-inspired biocatalytic total synthesis that integrated native enzymatic substrate conversion with artificial modules featuring abiotic transformations. After joining Prof. Dr. Anna Hirsch’s lab at the Helmholtz Institute for Pharmaceutical Research Saarland (HIPS) in mid-2019, he was involved in a variety of research projects centered on medicinal chemistry. With support of the DFG Walter Benjamin Program Fellowship, he transitioned to Prof. Dr. Ben Shen’s lab at Scripps Florida in early 2022, where he was a project leader, guiding an interdisciplinary team from three different labs. His research endeavors were centered on the development of anthraquinone-fused enediyne-based antibody-drug conjugates as promising anticancer agents. Upon returning to HIPS in mid-2024 on a DFG Walter Benjamin Return Fellowship, he was awarded the prestigious 21st Helmholtz Investigator Groups grant. This enabled him to establish his research group, focusing on natural product-inspired drug development at the interface of chemistry and biology.
2025
Unlocking the Antiviral Arsenal: Structure-Guided Optimization of Small-Molecule Inhibitors against RSV and hCoV-229E
Karhan C, Sake S, Gunesch A, Grethe C, Hellwinkel B, Köhler N, Kiefer A, Hapko U, Kany A, Pietschmann T, Hirsch A (2025)
European journal of medicinal chemistryDOI: 10.1016/j.ejmech.2025.117282
2024
The Natural Products Discovery Center: Release of the First 8490 Sequenced Strains for Exploring Actinobacteria Biosynthetic Diversity
Kalkreuter E, Kautsar S, Yang D, Bader C, Teijaro C, Fluegel L, Davis C, Simpson J, Lauterbach L, Steele A, …, Carvalho L, Shen B (2024)
bioRxivDOI: 10.1101/2023.12.14.571759
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 (2024)
2023
The many facets of sulfur incorporation in natural product biosynthesis
Steele A, Kiefer A, Shen B (2023)
Current opinion in chemical biology 76DOI: 10.1016/j.cbpa.2023.102366
Application of a Biocatalytic Strategy for the Preparation of Tiancimycin-Based Antibody-Drug Conjugates Revealing Key Insights into Structure-Activity Relationships
Steele A, Kiefer A, Hwang D, Yang D, Teijaro C, Adhikari A, Rader C, Shen B (2023)
Journal of medicinal chemistry 66 (2): 1562-1573DOI: 10.1021/acs.jmedchem.2c01771
An Artificial In Vitro Metabolism to Angiopterlactone B Inspired by Traditional Retrosynthesis
Kiefer A, Liu Y, Gummerer R, Jäger C, Deska J (2023)
Angewandte Chemie (International ed. in English) 62 (23)DOI: 10.1002/anie.202301178
pH-Responsive Dynaplexes as Potent Apoptosis Inductors by Intracellular Delivery of Survivin siRNA
Liu Y, Ashmawy S, Latta L, Weiss A, Kiefer A, Nasr S, Loretz B, Hirsch A, Lee S, Lehr C (2023)
Biomacromolecules 24 (8): 3742-3754DOI: 10.1021/acs.biomac.3c00424
Insights into the biosynthesis of icumazole, unveiling a distinctive family of crotonyl-CoA carboxylase/reductase
Xie F, Kiefer A, Hirsch A, Kalinina O, Fu C, Müller R (2023)
Cell Reports Physical Science 4 (5)DOI: 10.1016/j.xcrp.2023.101394
2022
Phage display-based discovery of cyclic peptides against the broad spectrum bacterial anti-virulence target CsrA
Jakob V, Zoller B, Rinkes J, Wu Y, Kiefer A, Hust M, Polten S, White A, Harvey P, Durek T, …, Kazmaier U, Empting M (2022)
European journal of medicinal chemistry 231DOI: 10.1016/j.ejmech.2022.114148
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
Sandacrabins - Structurally Unique Antiviral RNA Polymerase Inhibitors from a Rare Myxobacterium
Bader C, Panter F, Garcia R, Tchesnokov E, Haid S, Walt C, Spröer C, Kiefer A, Götte M, Overmann J, Pietschmann T, Müller R (2022)
Chem. Eur. J. 28 (10)DOI: 10.1002/chem.202104484
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)
2020
Flexible Fragment Growing Boosts Potency of Quorum-Sensing Inhibitors against Pseudomonas aeruginosa Virulence
Zender M, Witzgall F, Kiefer A, Kirsch B, Maurer C, Kany A, Xu N, Schmelz S, Börger C, Blankenfeldt W, Empting M (2020)
ChemMedChem 15 (2): 188-194DOI: 10.1002/cmdc.201900621
2019
Syntheses of Cyclomarins – Interesting Marine Natural Products with Distinct Mode of Action towards Malaria and Tuberculosis
Kiefer A, Kazmaier U (2019)
Synthesis 51 (01): 107-121DOI: 10.1055/s-0037-1610377
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
2018
Synthesis of modified β-methoxyphenylalanines via diazonium chemistry and their incorporation in desoxycyclomarin analogues
Kiefer A, Kazmaier U (2018)
Org. Biomol. Chem. 17 (1): 88-102DOI: 10.1039/C8OB02777C
2015
Palladium‐Catalyzed Allylic Alkylation Reactions of Glycolates as a Tool for the Synthesis of Functionalized α‐Hydroxy Esters
Kiefer A, Gawas D, Kazmaier U (2015)
Liebigs Ann. 2015 (26): 5810-5816DOI: 10.1002/ejoc.201500755