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Researcher in Laboratory © HIPS

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)

DOI: 10.26434/chemrxiv-2024-3mtxb

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