Apirat Chaikuad

Scopus Author ID ORCID

Publication Activity (10 Years)

Years Active: 2017-2024
Publications (10 Years): 52

Top Topics

Acute Myeloid Leukemia

Amyotrophic Lateral Sclerosis

Top Venues

Journal of medicinal chemistry

Molecules (Basel, Switzerland)

International journal of molecular sciences

ACS chemical biology

This page only lists publications with an associated author ORCID identifier.

Publications

Max Lewandowski, Melania Carmina, Loris Knümann, Minh Sai, Sabine Willems, Till Kasch, Julius Pollinger, Stefan Knapp, Julian A Marschner, Apirat Chaikuad, Daniel Merk
Structure-Guided Design of a Highly Potent Partial RXR Agonist with Superior Physicochemical Properties. Journal of medicinal chemistry 67 (3) (2024)
Max Lewandowski, Melania Carmina, Loris Knümann, Minh Sai, Sabine Willems, Till Kasch, Julius Pollinger, Stefan Knapp, Julian A Marschner, Apirat Chaikuad, Daniel Merk
Structure-Guided Design of a Highly Potent Partial RXR Agonist with Superior Physicochemical Properties. Journal of medicinal chemistry (2024)
Max Lewandowski, Melania Carmina, Loris Knümann, Minh Sai, Sabine Willems, Till Kasch, Julius Pollinger, Stefan Knapp, Julian A Marschner, Apirat Chaikuad, Daniel Merk
Structure-Guided Design of a Highly Potent Partial RXR Agonist with Superior Physicochemical Properties. Journal of medicinal chemistry 67 (3) (2024)
Leonore Novak, Maria Petrosino, Alessandra Pasquo, Apirat Chaikuad, Roberta Chiaraluce, Stefan Knapp, Valerio Consalvi
Mutation in the Common Docking Domain Affects MAP Kinase ERK2 Catalysis and Stability. Cancers 15 (11) (2023)
Xiaomin Ni, Andreas C Joerger, Apirat Chaikuad, Stefan Knapp
Structural insights into a regulatory mechanism of FIR RRM1-FUSE interaction. Open biology 13 (5) (2023)
Frances M Bashore, Ariana B Marquez, Apirat Chaikuad, Stefanie Howell, Andrea S Dunn, Alvaro A Beltran, Jeffery L Smith, David Harold Drewry, Adriana S Beltran, Alison D Axtman
Modulation of tau tubulin kinases (TTBK1 and TTBK2) impacts ciliogenesis. Scientific reports 13 (1) (2023)
Silvia Arifi, Julian A Marschner, Julius Pollinger, Laura Isigkeit, Pascal Heitel, Astrid Kaiser, Lennart Obeser, Georg Höfner, Ewgenij Proschak, Stefan Knapp, Apirat Chaikuad, Jan Heering, Daniel Merk
Targeting the Alternative Vitamin E Metabolite Binding Site Enables Noncanonical PPARγ Modulation. Journal of the American Chemical Society (2023)
Jun Yong Choi, Yoshihiko Noguchi, James M Alburger, Simon Bayle, Eugene Chung, Wayne Grant, Apirat Chaikuad, Stefan Knapp, Derek R Duckett, William R Roush
Structure-Based Development of Isoform-Selective Inhibitors of Casein Kinase 1ε vs Casein Kinase 1δ. Journal of medicinal chemistry (2023)
Amelie Tjaden, Apirat Chaikuad, Eric Kowarz, Rolf Marschalek, Stefan Knapp, Martin Schröder, Susanne Müller
Image-Based Annotation of Chemogenomic Libraries for Phenotypic Screening. Molecules (Basel, Switzerland) 27 (4) (2022)
Apirat Chaikuad, Rezart Zhubi, Claudia Tredup, Stefan Knapp
Comparative structural analyses of the NHL domains from the human E3 ligase TRIM-NHL family. IUCrJ 9 (Pt 6) (2022)
Gustave Adouvi, Laura Isigkeit, Úrsula López-García, Apirat Chaikuad, Julian A Marschner, Manfred Schubert-Zsilavecz, Daniel Merk
Rational Design of a New RXR Agonist Scaffold Enabling Single-Subtype Preference for RXRα, RXRβ, and RXRγ. Journal of medicinal chemistry 66 (1) (2022)
Giuseppe Faudone, Rezart Zhubi, Fatih Celik, Stefan Knapp, Apirat Chaikuad, Jan Heering, Daniel Merk
Design of a Potent TLX Agonist by Rational Fragment Fusion. Journal of medicinal chemistry 65 (3) (2022)
Ricardo A M Serafim, André da Silva Santiago, Martin P Schwalm, Zexi Hu, Caio V Dos Reis, Jessica E Takarada, Priscila Mezzomo, Katlin B Massirer, Mark Kudolo, Stefan Gerstenecker, Apirat Chaikuad, Lars Zender, Stefan Knapp, Stefan A Laufer, Rafael Miguez Couñago, Alexander Titz
Development of the First Covalent Monopolar Spindle Kinase 1 (MPS1/TTK) Inhibitor. Journal of medicinal chemistry 65 (4) (2022)
Vanesa Nozal, Loreto Martínez-González, Marta Gomez-Almeria, Claudia Gonzalo-Consuegra, Paula Santana, Apirat Chaikuad, Eva Pérez-Cuevas, Stefan Knapp, Daniel Lietha, David Ramírez, Sabrina Petralla, Barbara Monti, Carmen Gil, Angeles Martín-Requero, Valle Palomo, Eva de Lago, Ana Martinez
TDP-43 Modulation by Tau-Tubulin Kinase 1 Inhibitors: A New Avenue for Future Amyotrophic Lateral Sclerosis Therapy. Journal of medicinal chemistry 65 (2) (2022)
Gustave Adouvi, Laura Isigkeit, Úrsula López-García, Apirat Chaikuad, Julian A Marschner, Manfred Schubert-Zsilavecz, Daniel Merk
Rational Design of a New RXR Agonist Scaffold Enabling Single-Subtype Preference for RXRα, RXRβ, and RXRγ. Journal of medicinal chemistry 66 (1) (2022)
Jan Heering, Nathalie Jores, Whitney Kilu, Espen Schallmayer, Evelyn Peelen, Andreas Muehler, Hella Kohlhof, Daniel Vitt, Verena Linhard, Santosh L Gande, Apirat Chaikuad, Sridhar Sreeramulu, Harald Schwalbe, Daniel Merk
Mechanistic Impact of Different Ligand Scaffolds on FXR Modulation Suggests Avenues to Selective Modulators. ACS chemical biology 17 (11) (2022)
Gustave Adouvi, Laura Isigkeit, Úrsula López-García, Apirat Chaikuad, Julian A Marschner, Manfred Schubert-Zsilavecz, Daniel Merk
Rational Design of a New RXR Agonist Scaffold Enabling Single-Subtype Preference for RXRα, RXRβ, and RXRγ. Journal of medicinal chemistry (2022)
Laura Isigkeit, Apirat Chaikuad, Daniel Merk
A Consensus Compound/Bioactivity Dataset for Data-Driven Drug Design and Chemogenomics. Molecules (Basel, Switzerland) 27 (8) (2022)
Gustave Adouvi, Laura Isigkeit, Úrsula López-García, Apirat Chaikuad, Julian A Marschner, Manfred Schubert-Zsilavecz, Daniel Merk
Rational Design of a New RXR Agonist Scaffold Enabling Single-Subtype Preference for RXRα, RXRβ, and RXRγ. Journal of medicinal chemistry 66 (1) (2022)
Markus Hartmann, Jessica Huber, Jan S Kramer, Jan Heering, Larissa Pietsch, Holger Stark, Dalibor Odadzic, Iris Bischoff, Robert Fürst, Martin Schröder, Masato Akutsu, Apirat Chaikuad, Volker Dötsch, Stefan Knapp, Ricardo M Biondi, Vladimir V Rogov, Ewgenij Proschak
Demonstrating Ligandability of the LC3A and LC3B Adapter Interface. Journal of medicinal chemistry 64 (7) (2021)
Felix F Lillich, Sabine Willems, Xiaomin Ni, Whitney Kilu, Carmen Borkowsky, Mirko Brodsky, Jan S Kramer, Steffen Brunst, Victor Hernandez-Olmos, Jan Heering, Simone Schierle, Roxane-I Kestner, Franziska M Mayser, Moritz Helmstädter, Tamara Göbel, Lilia Weizel, Dmitry Namgaladze, Astrid Kaiser, Dieter Steinhilber, Waltraud Pfeilschifter, Astrid S Kahnt, Anna Proschak, Apirat Chaikuad, Stefan Knapp, Daniel Merk, Ewgenij Proschak
Structure-Based Design of Dual Partial Peroxisome Proliferator-Activated Receptor γ Agonists/Soluble Epoxide Hydrolase Inhibitors. Journal of medicinal chemistry 64 (23) (2021)
Mehmet Karatas, Apirat Chaikuad, Bianca Berger, Michael H G Kubbutat, Frank Totzke, Stefan Knapp, Conrad Kunick
7-(2-Anilinopyrimidin-4-yl)-1-benzazepin-2-ones Designed by a "Cut and Glue" Strategy Are Dual Aurora A/VEGF-R Kinase Inhibitors. Molecules (Basel, Switzerland) 26 (6) (2021)
Nicole Bata, Apirat Chaikuad, Nicole A Bakas, Allison S Limpert, Lester J Lambert, Douglas J Sheffler, Lena Marie Berger, Guoxiong Liu, Cunxiang Yuan, Li Wang, Yi Peng, Jing Dong, Maria Celeridad, Fabiana Layng, Stefan Knapp, Nicholas D P Cosford
Inhibitors of the Hippo Pathway Kinases STK3/MST2 and STK4/MST1 Have Utility for the Treatment of Acute Myeloid Leukemia. Journal of medicinal chemistry (2021)
Giuseppe Faudone, Whitney Kilu, Xiaomin Ni, Apirat Chaikuad, Sridhar Sreeramulu, Pascal Heitel, Harald Schwalbe, Stefan Knapp, Manfred Schubert-Zsilavecz, Jan Heering, Daniel Merk
The Transcriptional Repressor Orphan Nuclear Receptor TLX Is Responsive to Xanthines. ACS pharmacology & translational science 4 (6) (2021)
Nadine Russ, Martin Schröder, Benedict-Tilman Berger, Sebastian Mandel, Yagmur Aydogan, Sandy Mauer, Christian Pohl, David Harold Drewry, Apirat Chaikuad, Susanne Müller, Stefan Knapp
Design and Development of a Chemical Probe for Pseudokinase Ca2+/calmodulin-Dependent Ser/Thr Kinase. Journal of medicinal chemistry 64 (19) (2021)
Simone Schierle, Apirat Chaikuad, Felix F Lillich, Xiaomin Ni, Stefano Woltersdorf, Espen Schallmayer, Beatrice Renelt, Riccardo Ronchetti, Stefan Knapp, Ewgenij Proschak, Daniel Merk
Oxaprozin Analogues as Selective RXR Agonists with Superior Properties and Pharmacokinetics. Journal of medicinal chemistry 64 (8) (2021)
Olivier Etebe Nonga, Darja Lavogina, Erki Enkvist, Katrin Kestav, Apirat Chaikuad, Sarah E Dixon-Clarke, Alex N Bullock, Sergei Kopanchuk, Taavi Ivan, Ramesh Ekambaram, Kaido Viht, Stefan Knapp, Asko Uri
Crystal Structure-Guided Design of Bisubstrate Inhibitors and Photoluminescent Probes for Protein Kinases of the PIM Family. Molecules (Basel, Switzerland) 26 (14) (2021)
Xiaomin Ni, Allyn T Londregan, Dafydd R Owen, Stefan Knapp, Apirat Chaikuad
Structure and Inhibitor Binding Characterization of Oncogenic MLLT1 Mutants. ACS chemical biology 16 (4) (2021)
Martin Reynders, Apirat Chaikuad, Benedict-Tilmann Berger, Katharina Bauer, Pierre Koch, Stefan A Laufer, Stefan Knapp, Dirk H Trauner
Controlling the Covalent Reactivity of a Kinase Inhibitor with Light. Angewandte Chemie (International ed. in English) 60 (37) (2021)
Markus Hartmann, Sofia-Iris Bibli, Daniel Tews, Xiaomin Ni, Theresa Kircher, Jan S Kramer, Whitney Kilu, Jan Heering, Victor Hernandez-Olmos, Lilia Weizel, Gerhard K E Scriba, Sulaiman Krait, Stefan Knapp, Apirat Chaikuad, Daniel Merk, Ingrid Fleming, Pamela Fischer-Posovszky, Ewgenij Proschak
Combined Cardioprotective and Adipocyte Browning Effects Promoted by the Eutomer of Dual sEH/PPARγ Modulator. Journal of medicinal chemistry 64 (5) (2021)
Stefan Gerstenecker, Lisa Haarer, Martin Schröder, Mark Kudolo, Martin Peter Schwalm, Valentin Wydra, Ricardo A M Serafim, Apirat Chaikuad, Stefan Knapp, Stefan A Laufer, Alexander Titz
Discovery of a Potent and Highly Isoform-Selective Inhibitor of the Neglected Ribosomal Protein S6 Kinase Beta 2 (S6K2). Cancers 13 (20) (2021)
Giuseppe Faudone, Iris Bischoff-Kont, Lea Rachor, Sabine Willems, Rezart Zhubi, Astrid Kaiser, Apirat Chaikuad, Stefan Knapp, Robert Fürst, Jan Heering, Daniel Merk
Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells. Journal of medicinal chemistry 64 (12) (2021)
Leonie Gellrich, Pascal Heitel, Jan Heering, Whitney Kilu, Julius Pollinger, Tamara Goebel, Astrid Kahnt, Silvia Arifi, Werner Pogoda, Alexander Paulke, Dieter Steinhilber, Ewgenij Proschak, Mario Wurglics, Manfred Schubert-Zsilavecz, Apirat Chaikuad, Stefan Knapp, Iris Bischoff, Robert Fürst, Daniel Merk
l-Thyroxin and the Nonclassical Thyroid Hormone TETRAC Are Potent Activators of PPARγ. Journal of medicinal chemistry 63 (13) (2020)
Thomas Hanke, Sun-Yee Cheung, Whitney Kilu, Jan Heering, Xiaomin Ni, Viktoria Planz, Simone Schierle, Giuseppe Faudone, Marius Friedrich, Marek Wanior, Oliver Werz, Maike Windbergs, Ewgenij Proschak, Manfred Schubert-Zsilavecz, Apirat Chaikuad, Stefan Knapp, Daniel Merk
A Selective Modulator of Peroxisome Proliferator-Activated Receptor γ with an Unprecedented Binding Mode. Journal of medicinal chemistry 63 (9) (2020)
Alfredo Picado, Apirat Chaikuad, Carrow I Wells, Safal Shrestha, William J Zuercher, Julie E Pickett, Frank E Kwarcinski, Parvathi Sinha, Chandi S de Silva, Reena Zutshi, Shubin Liu, Natarajan Kannan, Stefan Knapp, David Harold Drewry, Timothy M Willson
A Chemical Probe for Dark Kinase STK17B Derives Its Potency and High Selectivity through a Unique P-Loop Conformation. Journal of medicinal chemistry 63 (23) (2020)
Jakob Gebel, Marcel Tuppi, Apirat Chaikuad, Katharina Hötte, Martin Schröder, Laura Schulz, Frank Löhr, Niklas Gutfreund, Franziska Finke, Erik Henrich, Julija Mezhyrova, Ralf Lehnert, Francesco Pampaloni, Gerhard Hummer, Ernst H K Stelzer, Stefan Knapp, Volker Dötsch
p63 uses a switch-like mechanism to set the threshold for induction of apoptosis. Nature chemical biology 16 (10) (2020)
Martin Schröder, Panagis Filippakopoulos, Martin P Schwalm, Carla A Ferrer, David Harold Drewry, Stefan Knapp, Apirat Chaikuad
Crystal Structure and Inhibitor Identifications Reveal Targeting Opportunity for the Atypical MAPK Kinase ERK3. International journal of molecular sciences 21 (21) (2020)
Anne Wurzlbauer, Katharina Rüben, Ece Gürdal, Apirat Chaikuad, Stefan Knapp, Wolfgang Sippl, Walter Becker, Franz Bracher
How to Separate Kinase Inhibition from Undesired Monoamine Oxidase A Inhibition-The Development of the DYRK1A Inhibitor AnnH75 from the Alkaloid Harmine. Molecules (Basel, Switzerland) 25 (24) (2020)
Natali Abeywickrama-Samarakoon, Jean-Claude Cortay, Camille Sureau, Susanne Müller, Dulce Alfaiate, Francesca Guerrieri, Apirat Chaikuad, Martin Schröder, Philippe Merle, Massimo Levrero, Paul Dény
Hepatitis Delta Virus histone mimicry drives the recruitment of chromatin remodelers for viral RNA replication. Nature communications 11 (1) (2020)
Apirat Chaikuad, Julius Pollinger, Michael Rühl, Xiaomin Ni, Whitney Kilu, Jan Heering, Daniel Merk
Comprehensive Set of Tertiary Complex Structures and Palmitic Acid Binding Provide Molecular Insights into Ligand Design for RXR Isoforms. International journal of molecular sciences 21 (22) (2020)
Huiyu Ren, Nicole A Bakas, Mitchell Vamos, Apirat Chaikuad, Allison S Limpert, Carina D Wimer, Sonja N Brun, Lester J Lambert, Lutz Tautz, Maria Celeridad, Douglas J Sheffler, Stefan Knapp, Reuben J Shaw, Nicholas D P Cosford
Design, Synthesis, and Characterization of an Orally Active Dual-Specific ULK1/2 Autophagy Inhibitor that Synergizes with the PARP Inhibitor Olaparib for the Treatment of Triple-Negative Breast Cancer. Journal of medicinal chemistry 63 (23) (2020)
Isabelle Meijer, Sabine Willems, Xiaomin Ni, Jan Heering, Apirat Chaikuad, Daniel Merk
Chemical Starting Matter for HNF4α Ligand Discovery and Chemogenomics. International journal of molecular sciences 21 (21) (2020)
Martin Schröder, Alex N Bullock, Oleg Fedorov, Franz Bracher, Apirat Chaikuad, Stefan Knapp
DFG-1 Residue Controls Inhibitor Binding Mode and Affinity, Providing a Basis for Rational Design of Kinase Inhibitor Selectivity. Journal of medicinal chemistry 63 (18) (2020)
Michael Forster, Xiaojun Julia Liang, Martin Schröder, Stefan Gerstenecker, Apirat Chaikuad, Stefan Knapp, Stefan A Laufer, Alexander Titz
Discovery of a Novel Class of Covalent Dual Inhibitors Targeting the Protein Kinases BMX and BTK. International journal of molecular sciences 21 (23) (2020)
Christian Lechner, Maren Flaßhoff, Hannes Falke, Lutz Preu, Nadége Loaëc, Laurent Meijer, Stefan Knapp, Apirat Chaikuad, Conrad Kunick
[b]-Annulated Halogen-Substituted Indoles as Potential DYRK1A Inhibitors. Molecules (Basel, Switzerland) 24 (22) (2019)
Apirat Chaikuad, Sebastian E Koschade, Alexandra Stolz, Katarina Zivkovic, Christian Pohl, Shabnam Shaid, Huiyu Ren, Lester J Lambert, Nicholas D P Cosford, Christian H Brandts, Stefan Knapp
Conservation of structure, function and inhibitor binding in UNC-51-like kinase 1 and 2 (ULK1/2). The Biochemical journal 476 (5) (2019)
Sandra Röhm, Benedict-Tilman Berger, Martin Schröder, Apirat Chaikuad, Rob Winkel, Koen F W Hekking, Jorg J C Benningshof, Gerhard Müller, Roberta Tesch, Mark Kudolo, Michael Forster, Stefan A Laufer, Stefan Knapp
Fast Iterative Synthetic Approach toward Identification of Novel Highly Selective p38 MAP Kinase Inhibitors. Journal of medicinal chemistry 62 (23) (2019)
Jan S Kramer, Stefano Woltersdorf, Thomas Duflot, Kerstin Hiesinger, Felix F Lillich, Felix Knöll, Sandra K Wittmann, Franca-M Klingler, Steffen Brunst, Apirat Chaikuad, Christophe Morisseau, Bruce D Hammock, Carola Buccellati, Angelo Sala, G Enrico Rovati, Matthieu Leuillier, Sylvain Fraineau, Julie Rondeaux, Victor Hernandez-Olmos, Jan Heering, Daniel Merk, Denys Pogoryelov, Dieter Steinhilber, Stefan Knapp, Jeremy Bellien, Ewgenij Proschak
Discovery of the First in Vivo Active Inhibitors of the Soluble Epoxide Hydrolase Phosphatase Domain. Journal of medicinal chemistry 62 (18) (2019)
Christina Heroven, Victoria Georgi, Gaurav K Ganotra, Paul Brennan, Finn Wolfreys, Rebecca C Wade, Amaury E Fernández-Montalván, Apirat Chaikuad, Stefan Knapp
Halogen-Aromatic π Interactions Modulate Inhibitor Residence Times. Angewandte Chemie (International ed. in English) 57 (24) (2018)
David Heidenreich, Moses Moustakim, Jurema Schmidt, Daniel Merk, Paul E Brennan, Oleg Fedorov, Apirat Chaikuad, Stefan Knapp
Structure-Based Approach toward Identification of Inhibitory Fragments for Eleven-Nineteen-Leukemia Protein (ENL). Journal of medicinal chemistry 61 (23) (2018)
Michael Forster, Apirat Chaikuad, Teodor Dimitrov, Eva Döring, Julia Holstein, Benedict-Tilman Berger, Alexander Titz, Kamran Ghoreschi, Susanne Müller, Stefan Knapp, Stefan A Laufer
Development, Optimization, and Structure-Activity Relationships of Covalent-Reversible JAK3 Inhibitors Based on a Tricyclic Imidazo[5,4- d]pyrrolo[2,3- b]pyridine Scaffold. Journal of medicinal chemistry 61 (12) (2018)
Amaury E Fernández-Montalván, Markus Berger, Benno Kuropka, Seong Joo Koo, Volker Badock, Joerg Weiske, Vera Puetter, Simon J Holton, Detlef Stöckigt, Antonius Ter Laak, Paolo A Centrella, Matthew A Clark, Christoph E Dumelin, Eric A Sigel, Holly H Soutter, Dawn M Troast, Ying Zhang, John W Cuozzo, Anthony D Keefe, Didier Roche, Vincent Rodeschini, Apirat Chaikuad, Laura Díaz-Sáez, James M Bennett, Oleg Fedorov, Kilian V M Huber, Jan Hübner, Hilmar Weinmann, Ingo V Hartung, Mátyás Gorjánácz
Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action. ACS chemical biology 12 (11) (2017)