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A high affinity pan-PI3K binding module supports selective targeted protein degradation of PI3Kα
Werner Theodor Jauslin, Matthias Schild, Thorsten Schaefer, Chiara Borsari, Clara Orbegozo, Lukas Bissegger, Saule Zhanybekova, Danilo Ritz, Alexander Schmidt, Matthias Wymann & Dennis Gillingham
Chem. Sci. 2024, 15, 683–691. doi:10.1039/D3SC04629J
Recording Binding Information Directly into DNA-Encoded Libraries Using Terminal Deoxynucleotidyl Transferase
Lukas A. Schneider, Basilius Sauter, Koder Dagher & Dennis Gillingham
J. Am. Chem. Soc. 2023, 145, 38, 20874–20882. doi:10.1021/jacs.3c05961
- The work of this paper was presented at the 11th International Symposium on DNA-encoded Chemical Libraries.
- Dr. Lukas Schneider won the poster-prize at the symposium for this work
Design principles for cyclin K molecular glue degraders
Zuzanna Kozicka, Dakota J. Suchyta, Vivian Focht, Georg Kempf, Georg Petzold, Marius Jentzsch, Charles Zou, Cristina Di Genua, Katherine A. Donovan, Seemon Coomar, Marko Cigler, Cristina Mayor-Ruiz, Jonathan L. Schmid-Burgk, Daniel Häussinger, Georg E. Winter, Eric S. Fischer, Mikołaj Słabicki, Dennis Gillingham, Benjamin L. Ebert & Nicolas H. Thomä
Nat. Chem. Biol. 2023. doi:10.1038/s41589-023-01409-z
- Some of the work in this paper was done by Dakota J. Suchyate, a Post-Doc from Nicolas Thomä, in our chemical laboratories.
Overlaid transcriptome and proteome analyses identify mitotic kinesins as important targets of arylsulfonamide-mediated RBM39 degradation
Seemon Coomar, Pedro Mota, Alexander Penson, Juerg Schwaller, Omar Abdel-Wahab & Dennis Gillingham
Mol. Cancer Res. 2023, 21, 8, 768–778. doi:10.1158/1541-7786.MCR-22-0541
- A fluorescent cell image from this work made it to the title page of the issue
- The paper was highlighted in the issue as a selected article.
Repurposing the Damage Repair Protein Methyl Guanine Methyl Transferase as a Ligand Inducible Fusion Degron
Gosia M. Murawska#, Caspar Vogel#, Max Jan, Xinyan Lu, Matthias Schild, Mikolaj Slabicki, Charles Zou, Saule Zhanybekova, Manisha Manojkumar, Georg Petzold, Peter Kaiser, Nicolas Thomä, Benjamin Ebert & Dennis Gillingham
ACS Chem. Biol. 2022, 17, 1, 24–31. doi:10.1021/acschembio.1c00771
- # These authors contributed equally
An assessment of the mutational load caused by various reactions used in DNA encoded libraries
Basilius Sauter, Lukas Schneider, Cedric Stress & Dennis Gillingham
Bioorg. Med. Chem. 2021, 52, 116508. doi:10.1016/j.bmc.2021.116508
- This article is part of the DNA-encoded library special issue edited by Andreas Brunschweiger.
Building Boron Heterocycles into DNA-Encoded Libraries
Pinwen Cai, Lukas A. Schneider, Cedric Stress & Dennis Gillingham
Org. Lett. 2021, 23, 22, 8772–8776. doi:10.1021/acs.orglett.1c03262
The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K
Mikołaj Słabicki, Zuzanna Kozicka, Georg Petzold, Yen-Der Li, Manisha Manojkumar, Richard D. Bunker, Katherine A. Donovan, Quinlan L. Sievers, Jonas Koeppel, Dakota Suchyta, Adam S. Sperling, Emma C. Fink, Jessica A. Gasser, Li R. Wang, Steven M. Corsello, Rob S. Sellar, Max Jan, Dennis Gillingham, Claudia Scholl, Stefan Fröhling, Todd R. Golub, Eric S. Fischer, Nicolas H. Thomä & Benjamin L. Ebert
Nature 2020, 585, 293–297. doi:10.1038/s41586-020-2374-x
Quantum-chemistry-aided identification, synthesis and experimentalvalidation of model systems for conformationally controlled reactionstudies: Separation of the conformers of 2,3-dibromobuta-1,3-dienein the gas phase
Ardita Kilaj, Hong Gao, Diana Tahchieva, Raghunathan Ramakrishnan, Daniel Bachmann, Dennis Gillingham, O. Anatole von Lilienfeld, Jochen Küppere and Stefan Willitsch
Phys. Chem. Chem. Phys. 2020, 22, 13431–13439. doi:10.1039/D0CP01396J
A DNA‐encoded chemical library incorporating elements of natural macrocycles
Cedric J. Stress, Basilius Sauter, Lukas Schneider, Timothy Sharpe and Dennis G. Gillingham
Angew. Chem. Int. Ed. 2019, 58, 28, 9570─9574. doi:10.1002/anie.201902513
- This article was highlighted in ChemView on the 11. June 2019
- An press release describing the research topic in layman's terms is available in English and in German
- A German version of this article is available with the doi:10.1002/ange.201902513
- This article was published first as a draft in ChemRXiv: Cedric J. Stress, Basilius Sauter, Lukas Schneider, Timothy Sharpe and Dennis G. Gillingham, «A DNA-Encoded Macrocycle Library that Resembles Natural Macrocycles», ChemRxiv 2019. doi:10.26434/chemrxiv.7679984
Nanopore sequencing accurately identifies the mutagenic DNA lesion O⁶‐carboxymethyl guanine and reveals its behavior in replication
Yu Wang, Kiran Patil, Shuanghong Yan, Weiming Guo, Yuqin Wang, Panke Zhang, Hong-Yuan Chen, Dennis G. Gillingham and Shuo Huang
Angew. Chem. Int. Ed. 2019, 58, 25, 8432─8436. doi:10.1002/anie.201902521
Exploring DCAF15 for reprogrammable targeted protein degradation
Seemon Coomar and Dennis G. Gillingham
bioRxiv 2019, 542506, preprint. doi:10.1101/542506
High Sensitivity of Human Translesion DNA Synthesis Polymerase κ to Variation in O⁶-carboxymethylguanine Structures
Michael H. Räz, Emma Sandell, Kiran Patil, Dennis G. Gillingham and Shana J. Sturla
ACS Chem. Biol. 2019, 14, 2, 214─222. doi:10.1021/acschembio.8b00802
Synthesis of Various Water Soluble and Stable Copper Complexes Bearing N‐Heterocyclic Carbene Ligands and Their Activity in DNA Alkylation
Stefanie Geigle, Dnyaneshwar Rasale and Dennis G. Gillingham
Helvetica Chimica Acta 2019, 102, e1800183. doi:10.1002/hlca.201800183
Direct and Selective Modification of RNA – An Open Challenge in Nucleic Acid Chemistry
Dennis G. Gillingham and Dnyaneshwar Rasale
Chimia 2018, 72, 11, 777─781. doi:10.2533/chimia.2018.777
A new water soluble copper N-heterocyclic carbene complex delivers mild O⁶G-selective RNA alkylation
Dnyaneshwar Rasale, Kiran Patil, Basilius Sauter, Stefanie Geigle, Saule Zhanybekova and Dennis G. Gillingham
Chemical Communications 2018, 54, 9174─9177. doi:10.1039/C8CC04476G
Profiling the nucleobase and structure selectivity of anticancer drugs and other DNA alkylating agents by RNA sequencing
Basilius Sauter and Dennis G. Gillingham
ChemBioChem 2018, 19, 1638─1642. doi:10.1002/cbic.201800235
An Artificial Metalloenzyme for Carbene Transfer Based on a Biotinylated Dirhodium Anchored within Streptavidin
Jingming Zhao, Daniel Bachmann, Markus Lenz, Dennis G. Gillingham and Thomas R. Ward
Catalysis Science & Technology 2018, 8, 2294─2298. doi:10.1039/C8CY00646F
Genomic studies reveal new aspects of the biology of DNA damaging agents
Dennis G. Gillingham and Basilius Sauter
ChemBioChem 2017, 18, 2368─2375. doi:10.1002/cbic.201700520
Copper carbenes alkylate guanine chemoselectively through a substrate directed reaction
Stefanie Geigle, Laura A. Wyss, Shana J. Sturla and Dennis G. Gillingham
Chemical Science 2017, 8, 499─506. doi:10.1039/c6sc03502g
The role of boronic acids in accelerating condensation reactions of α-effect amines with carbonyls
Dennis G. Gillingham
Organic & Biomolecular Chemistry 2016, 14, 7606─7609. doi:10.1039/C6OB01193D
The pKa of Brønsted acids controls their reactivity with diazo compounds
Na Fei, Basilius Sauter and Dennis G. Gillingham
Chemical Communications 2016, 52, 47, 7501─7504. doi:10.1039/c6cc03561b
Comparison of boron-assisted oxime and hydrazone formations leads to the discovery of a fluorogenic variant.
Cedric J. Stress, Pascal Schmidt and Dennis G. Gillingham
Organic & Biomolecular Chemistry 2016, 14, 24, 5529─5533. doi:10.1039/C6OB00168H
Properties and reactivity of nucleic acids relevant to epigenomics, transcriptomics, and therapeutic
Dennis G. Gillingham, Stefanie Geigle and O. Anatole Lilienfeld
Chemical Society Reviews 2016, 45, 9, 2637─2655. doi:10.1039/c5cs00271k
Synthesis of New Alkylated Mononucleotide Analogues and Their Repair Proficiency by the Prokaryotic DNA Repair Protein AlkB
Kiril Tishinov and Dennis G. Gillingham
Synlett 2015, 26, 19, 2720─2723. doi:10.1055/s-0035-1560491
Modular Ligands for Dirhodium Complexes Facilitate Catalyst Customization
Daniel Bachmann, Pascal Schmidt, Stefanie Geigle, Antoinette Chougnet, Wolf-Dietrich Woggon and Dennis G. Gillingham
Advanced Synthesis & Catalysis 2015, 357, 9, 2033─2038. doi:10.1002/adsc.201500050
Catalysts for RNA and DNA modification
Dennis G. Gillingham and Ramla Shahid
Current Opinion in Chemical Biology 2015, 25, 110─114. doi:10.1016/j.cbpa.2014.12.025
Boronic acids facilitate rapid oxime condensations at neutral pH
Pascal Schmidt, Cedric J. Stress and Dennis G. Gillingham
Chemical Science 2015, 6, 6, 3329─3333. doi:10.1039/C5SC00921A
Dialdehydes Lead to Exceptionally Fast Bioconjugations at Neutral pH by Virtue of a Cyclic Intermediate
Pascal Schmidt, Linna Zhou, Kiril Tishinov, Kasper Zimmermann and Dennis G. Gillingham
Angewandte Chemie International Edition 2014, 53, 41, 10928─10931. doi:10.1002/anie.201406132
Catalytic carbene transfer allows the direct customization of cyclic purine dinucleotides
Na Fei, Seraina Bluemli, Benoit-Joseph Lavantie, Lorenzo D. Bizzini, Kasper Zimmermann, Urs Jenal and Dennis G. Gillingham
Chemical Communications 2014, 50, 62, 8499─8502. doi:10.1039/C4CC01919A
Stereoselective Heck Reactions with Vinyl Sulfoxides, Sulfides and Sulfones
Daniel Bachmann, Christopher C. Witter and Dennis G. Gillingham
Advanced Synthesis & Catalysis 2013, 355, 18, 3703─3707. doi:10.1002/adsc.201300678
Catalytic X-H insertion reactions based on carbenoids
Dennis G. Gillingham and Na Fei
Chemical Society Reviews 2013, 42, 12, 4918─4931. doi:10.1039/C3CS35496B
Synthesis of Nucleic Acid Polymers with Non-Canonical Nucleobases
Dennis G. Gillingham and Kiril Tishinov
Synlett 2013, 24, 8, 893─897. doi:10.1055/s-0032-1318493
Cu(I)-catalysed N-H insertion in water: a new tool for chemical biology
Kiril Tishinov, Na Fei and Dennis G. Gillingham
Chemical Science 2013, 4, 12, 4401─4406. doi:10.1039/C3SC51363G
Structure-Selective Catalytic Alkylation of DNA and RNA
Kiril Tishinov, Kristina Schmidt, Daniel Häusinger and Dennis G. Gillingham
Angewandte Chemie International Edition 2012, 51, 12000─12004. doi:10.1002/anie.201205201
A Report from the 47th EUCHEMS Conference on Stereochemistry: The Bürgenstock Conference
Dennis G. Gillingham, Alexandre Martinez and Zbigniew Pianowski
Chimia 2012, 66, 873─875. doi:10.2533/chimia.2012.873
A De novo chemoenzymatic synthesis of sialic acid
Pierre Stallforth, Stefan Matthies, Alexander Adibekian, Dennis G. Gillingham, Donald Hilvert and Peter Seeberger
Chemical Communications 2012, 48, 11987─11989. doi:10.1039/c2cc37305j
An artificial metalloenzyme for olefin metathesis
Clemens Mayer, Dennis G. Gillingham, Thomas R. Ward and Donald Hilvert
Chemical Communications 2011, 47, 12068─12070. doi:10.1039/C1CC15005G
A Chemoenzymatic Synthesis of Differentially Protected 3-Deoxysugars
Dennis G. Gillingham, Pierre Stallforth, Alexander Adibekian, Peter Seeberger and Donald Hilvert
Nature Chemistry 2010, 2, 102─105. doi:10.1038/nchem.504
- This article was also featured in the News and Views section: Benjamin G. Davis, «Enzyme catalysis: Sweet flexibility», Nature Chemistry 2010, 2, 85─86. doi:10.1038/nchem.529
The Putative Diels-Alderase Macrophomate Synthase is an Efficient Aldolase
Jörg M. Serafimov, Dennis G. Gillingham, Simon Kuster and Donald Hilvert
Journal of the American Chemical Society 2008, 130, 7798─7799. doi:10.1021/ja8017994
Highly Site- and Enantioselective Cu-Catalyzed Allylic Alkylation Reactions with Easily Accessible Vinylaluminum Reagents
Yunmi Lee, Katsuhiro Akiyama, Dennis G. Gillingham, M. Kevin Brown and Amir H. Hoveyda
Journal of the American Chemical Society 2008, 130, 446─447. doi:10.1021/ja0782192
Chiral N-Heterocyclic Carbenes in Natural Product Synthesis: Application of Ru-Catalyzed Asymmetric Ring-Opening/Cross-Metathesis and Cu-Catalyzed Allylic Alkylation to Total Synthesis of Baconipyrone C
Dennis G. Gillingham and Amir H. Hoveyda
Angewandte Chemie International Edition 2007, 46, 3860─3864. doi:10.1002/anie.200700501
Efficient Enantioselective Synthesis of Functionalized Tetrahydropyrans by Ru-Catalyzed Asymmetric Ring-Opening Metathesis/Cross-Metathesis (AROM/CM)
Dennis G. Gillingham, Osamu Kataoka, Steven B. Garber and Amir H. Hoveyda
Journal of the American Chemical Society 2004, 126, 12288─12290. doi:10.1021/ja0458672
Ru Complexes Bearing Bidentate Carbenes: From Innocent Curiosity to Uniquely Effective Catalysts for Olefin Metathesis
Amir H. Hoveyda, Dennis G. Gillingham, Joshua J. VanVeldhuizen, Osamu Kataoka, Steven B. Garber, Jason S. Kingsbury and Joseph P. Harrity
Organic & Biomolecular Chemistry 2004, 2, 8─23. doi:10.1039/b311496c
Chiral Ru-based Complexes for Asymmetric Olefin Metathesis: Enhancement of Catalyst Activity through Steric and Electronic Modifications
Joshua J. VanVeldhuizen, Dennis G. Gillingham, Stephen B. Garber, Osamu Kataoka and Amir H. Hoveyda
Journal of the American Chemical Society 2003, 125, 12502─12508. doi:10.1021/ja030222