Scientific advancements and News

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Publications

24. Lerma Romero JA, Meyners C, Christmann A, Reinbold LM, Charalampidou A, Hausch F, Kolmar H. Binding pocket stabilization by high-throughput screening of yeast display libraries. Front Mol Biosci. 2022;9. doi: 10.3389/fmolb.2022.1023131.
23. Upadhyay N, Tilekar K, Safuan S, Kumar AP, Schweipert M, Meyer-Almes FJ, Ramaa CS.
Development and investigation of thiazolidinedione and pyrazoline compounds as antiangiogenic weapons targeting VEGFR-2.
Future Med Chem. 2021 Nov;13(22):1963-1986. doi: 10.4155/fmc-2021-0139. Epub 2021 Sep 28. PMID: 34581188.
22. Upadhyay N, Tilekar K, Safuan S, Kumar AP, Schweipert M, Meyer-Almes FJ,
Ramaa CS.
Double-edged Swords: Diaryl pyrazoline thiazolidinediones synchronously targeting cancer epigenetics and angiogenesis.
Bioorg Chem. 2021 Nov;116:105350. doi: 10.1016/j.bioorg.2021.105350. Epub 2021 Sep 11. PMID: 34547645.
21. Schweipert M, Jänsch N, Upadhyay N, Tilekar K, Wozny E, Basheer S, Wurster E,
Müller M, C S R, Meyer-Almes FJ.
Mechanistic Insights into Binding of Ligands with Thiazolidinedione Warhead to Human Histone Deacetylase 4.
Pharmaceuticals (Basel). 2021 Oct 11;14(10):1032. doi: 10.3390/ph14101032. PMID: 34681256; PMCID: PMC8537711.
20. Thomas Nehls, Tim Heymann, Christian Meyners, Felix Hausch and Frederik Lermyte
Fenton-Chemistry-Based Oxidative Modification of Proteins Reflects Their Conformation
Int. J. Mol. Sci. 2021, 22(18), 9927; DOI: https://doi.org/10.3390/ijms22189927
19. Frühauf A, Meyer-Almes FJ.
Non-Hydroxamate Zinc-Binding Groups as Warheads for Histone Deacetylases.
Molecules. 2021 Aug 25;26(17):5151. doi: 10.3390/molecules26175151. PMID: 34500583; PMCID: PMC8434074.
18. Upadhyay N, Tilekar K, Safuan S, Kumar AP, Schweipert M, Meyer-Almes FJ, C S
R.
Multi-target weapons: diaryl-pyrazoline thiazolidinediones simultaneously targeting VEGFR-2 and HDAC cancer hallmarks.
RSC Med Chem. 2021 Jul 27;12(9):1540-1554. doi: 10.1039/d1md00125f. PMID: 34671737; PMCID: PMC8459325.
17. K. Tilekar, J. D. Hess, N. Upadhyay, M. Schweipert, F. Flath, D. A. Gutierrez, et al.
HDAC4 Inhibitors with Cyclic Linker and Non-hydroxamate Zinc Binding Group: Design, Synthesis, HDAC Screening and in vitro Cytotoxicity evaluation.
ChemistrySelect 2021 Vol. 6 Issue 26 Pages 6748-6763.
doi: 10.1002/slct.202102061
16. Cinzia Imberti, Frederik Lermyte, Emily P. Friar, Peter B. O'Connor and Peter J. Sadler
Facile protein conjugation of platinum for light-activated cytotoxic payload release
DOI: 10.1039/D1CC02722K (Communication) Chem. Commun., 2021, 57, 7645-7648.
15. Tilekar K, Hess JD, Upadhyay N, Bianco AL, Schweipert M, Laghezza A, Loiodice
F, Meyer-Almes FJ, Aguilera RJ, Lavecchia A, C S R.
Thiazolidinedione “Magic Bullets” Simultaneously Targeting PPARγ and HDACs: Design, Synthesis, and Investigations of their In Vitro and In Vivo Antitumor Effects.
J Med Chem. 2021 May 27;64(10):6949-6971.
doi: 10.1021/acs.jmedchem.1c00491. Epub 2021 May 18. PMID: 34006099.
14. Frederik Lermyte, Alina Theisen, Peter B. O'Connor.
Solution Condition-Dependent Formation of Gas-Phase Protomers of Alpha-Synuclein in Electrospray Ionization
Journal of the American Society for Mass Spectrometry, 2021, 32, 364. doi.org/10.1021/jasms.0c00373.
13. Mowei Zhou, Carter Lantz, Kyle A. Brown, Ying Ge, Ljiljana Paša-Tolić, Joseph A. Loo, Frederik Lermyte.
Higher-order structural characterisation of native proteins and complexes by top-down mass spectrometry
Chemical Science, 2020, 11, 12918. DOI: 10.1039/D0SC04392C.
12. Elizabeth J. Anthony, Elizabeth M. Bolitho, Hannah E. Bridgewater, Oliver W. L. Carter, Jane M. Donnelly, Cinzia Imberti, Edward C. Lant, Frederik Lermyte, Russell J. Needham, Marta Palau, Peter J. Sadler, Huayun Shi, Fang-Xin Wang, Wen-Ying Zhang, Zijin Zhang.
Metallodrugs are unique: opportunities and challenges of discovery and development
Chemical Science, 2020, 11, 12888. DOI: 10.1039/d0sc04082g.
11. Joshua B Sheetz, Sebastian Mathea, Hanna Karvonen, Ketan Malhotra, Deep Chatterjee, Wilhelmiina Niininen, Robert Perttilä, Franziska Preuss, Krishna Suresh, Steven E Stayrook, Yuko Tsutsui, Ravi Radhakrishnan, Daniela Ungureanu, Stefan Knapp, Mark A Lemmon.
Structural Insights into Pseudokinase Domains of Receptor Tyrosine Kinases
Mol Cell. 2020 Aug 6;79(3):390-405.e7. doi: 10.1016/j.molcel.2020.06.018. Epub 2020 Jul 2.
10. Martin Schröder, Li Tan, Jinhua Wang, Yanke Liang, Nathanael S Gray, Stefan Knapp, Apirat Chaikuad.
Catalytic Domain Plasticity of MKK7 Reveals Structural Mechanisms of Allosteric Activation and Diverse Targeting Opportunities
Cell Chem Biol. 2020 Oct 15;27(10):1285-1295.e4.
doi: 10.1016/j.chembiol.2020.07.014. Epub 2020 Aug 11.
9. Franziska Preuss, Deep Chatterjee, Sebastian Mathea, Safal Shrestha, Jonathan St-Germain, Manipa Saha, Natarajan Kannan, Brian Raught, Robert Rottapel, Stefan Knapp.
Nucleotide Binding, Evolutionary Insights, and Interaction Partners of the Pseudokinase Unc-51-like Kinase 4
Structure. 2020 Nov 3;28(11):1184-1196.e6. doi: 10.1016/j.str.2020.07.016. Epub 2020 Aug 18.
8. Steffen C Hinz, Adrian Elter, Julius Grzeschik, Jan Habermann, Bastian Becker, Harald Kolmar.
Simplifying the Detection of Surface Presentation Levels in Yeast Surface Display by Intracellular tGFP Expression
Methods Mol Biol. 2020;2070:211-222. doi: 10.1007/978-1-4939-9853-1_12.
7. Steffen C Hinz, Adrian Elter, Oliver Rammo, Achim Schwämmle, Ataurehman Ali, Stefan Zielonka, Thomas Herget, Harald Kolmar.
A Generic Procedure for the Isolation of pH- and Magnesium-Responsive Chicken scFvs for Downstream Purification of Human Antibodies
Front Bioeng Biotechnol. 2020 Jun 23;8:688. doi: 10.3389/fbioe.2020.00688. eCollection 2020.
6. Xixi Feng, Claudia Sippel, Fabian H Knaup, Andreas Bracher 3, Stefania Staibano, Maria F Romano, Felix Hausch.
A Novel Decalin-Based Bicyclic Scaffold for FKBP51-Selective Ligands
J Med Chem. 2020 Jan 9;63(1):231-240. doi: 10.1021/acs.jmedchem.9b01157. Epub 2019 Dec 18.
5. Deniston, Salogiannis, Mathea, Snead, Lahiri, Matyszewski, Donosa, Watanabe, Böhning, Shiau, Knapp, Villa, Reck-Peterson, Leschziner.
Structure of LRRK2 in Parkinson's disease and model for microtubule interaction
Nature. 2020 Aug 19. doi: 10.1038/s41586-020-2673-2. Online ahead of print.
4. Matthias Bischoff, Peter Mayer, Christian Meyners, Felix Hausch.
Enantioselective Synthesis of a Tricyclic, sp 3 -Rich Diazatetradecanedione: an Amino Acid-Based Natural Product-Like Scaffold
Chemistry. 2020 Apr 9;26(21):4677-4681. doi: 10.1002/chem.201905144. Epub 2020 Feb 19.
3. Jan P Bogen, Julius Grzeschik, Simon Krah, Stefan Zielonka, Harald Kolmar.
Rapid Generation of Chicken Immune Libraries for Yeast Surface Display
Methods Mol Biol . 2020;2070:289-302. doi: 10.1007/978-1-4939-9853-1_16.
2. Devaraj Basavarajappa, Stella Uebbing, Marius Kreiss, Ana Lukic, Beatrix Suess, Dieter Steinhilber, Bengt Samuelsson, Olof Rådmark.
Dicer up-regulation by inhibition of specific proteolysis in differentiating monocytic cells
Proc Natl Acad Sci U S A . 2020 Apr 14;117(15):8573-8583.
doi: 10.1073/pnas.1916249117. Epub 2020 Mar 27.
1. Stephanie Ballweg, Erdinc Sezgin, Milka Doktorova, Roberto Covino, John Reinhard, Dorith Wunnicke, Inga Hänelt, Ilya Levental, Gerhard Hummer, Robert Ernst.
Regulation of lipid saturation without sensing membrane fluidity
Nat Commun. 2020 Feb 6;11(1):756. doi: 10.1038/s41467-020-14528-1.

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February 28, 2024

New Publication in ACS Central Science