Structural mimicry of UM171 and neomorphic cancer mutants co-opts E3 ligase KBTBD4 for HDAC1/2 recruitment.
Chen Z. et al, (2025), Nature communications, 16
Toward target 2035: EUbOPEN - a public–private partnership to enable & unlock biology in the open
Tredup C. et al, (2025), RSC Medicinal Chemistry
Covalent Inhibitors of KEAP1 with Exquisite Selectivity.
Fejes I. et al, (2024), Journal of medicinal chemistry
Structure-Guided Conformational Restriction Leading to High-Affinity, Selective, and Cell-Active Tetrahydroisoquinoline-Based Noncovalent Keap1-Nrf2 Inhibitors.
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A BTB extension and ion-binding domain contribute to the pentameric structure and TFAP2A binding of KCTD1.
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Discovery of Two Highly Selective Structurally Orthogonal Chemical Probes for Activin Receptor-like Kinases 1 and 2.
Němec V. et al, (2024), Journal of medicinal chemistry
Discovery of Conformationally Constrained ALK2 Inhibitors.
González-Álvarez H. et al, (2024), Journal of medicinal chemistry
Still in Search for an EAAT Activator: GT949 Does Not Activate EAAT2, nor EAAT3 in Impedance and Radioligand Uptake Assays.
van Veggel L. et al, (2024), ACS chemical neuroscience
Discovery and Characterization of a Chemical Probe for Cyclin-Dependent Kinase-Like 2
Bashore FM. et al, (2024), ACS Medicinal Chemistry Letters
Structural and biochemical characterization establishes a detailed understanding of KEAP1-CUL3 complex assembly
Adamson RJ. et al, (2023), Free Radical Biology and Medicine
Discovery of a Potent and Selective CDKL5/GSK3 Chemical Probe That Is Neuroprotective.
Ong HW. et al, (2023), ACS Chem Neurosci
Target 2035 – an update on private sector contributions
Ackloo S. et al, (2023), RSC Medicinal Chemistry, 14, 1002 - 1011
Disease-associated KBTBD4 mutations in medulloblastoma elicit neomorphic ubiquitylation activity to promote CoREST degradation
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Protocol paper: a multi-center, double-blinded, randomized, 6-month, placebo-controlled study followed by 12-month open label extension to evaluate the safety and efficacy of Saracatinib in Fibrodysplasia Ossificans Progressiva (STOPFOP).
Smilde BJ. et al, (2022), BMC musculoskeletal disorders, 23
Sequence and structural variations determining the recruitment of WNK kinases to the KLHL3 E3 ligase.
Chen Z. et al, (2022), The Biochemical journal
Ubiquitin ligases: guardians of mammalian development
Cruz Walma DA. et al, (2022), Nature Reviews Molecular Cell Biology
Target 2035-update on the quest for a probe for every protein
Mueller S. et al, (2021), RSC MEDICINAL CHEMISTRY
Development of a Selective Dual Discoidin Domain Receptor (DDR)/p38 Kinase Chemical Probe.
Röhm S. et al, (2021), Journal of medicinal chemistry, 64, 13451 - 13474
Challenges and Opportunities for Drug Repositioning in Fibrodysplasia Ossificans Progressiva
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