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Publications

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 specific inhibitor of serine-threonine kinase cyclin dependent kinase-like 5 (CDKL5) demonstrates role in hippocampal CA1 physiology.

Castano A. et al, (2023), eLife, 12

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

Chen Z. et al, (2022), Cell Death & Differentiation, 29, 1955 - 1969

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

Ventura F. et al, (2021), Biomedicines, 9, 213 - 213

ALK2 Receptor Kinase Association with FKBP12.6 Is Structurally Conserved with the ALK2-FKBP12 Complex

Williams E. et al, (2021), Biomedicines, 9, 129 - 129

DFG-1 Residue Controls Inhibitor Binding Mode and Affinity, Providing a Basis for Rational Design of Kinase Inhibitor Selectivity

Schröder M. et al, (2020), Journal of Medicinal Chemistry, 63, 10224 - 10234

Leveraging an Open Science Drug Discovery Model to Develop CNS Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma

Smil D. et al, (2020), Journal of Medicinal Chemistry

Sequence and structural variations determining the recruitment of WNK kinases to the KLHL3 E3 ligase

Chen Z. et al, (2020)

Receptor-interacting protein kinase 2 (RIPK2) and nucleotide-binding oligomerization domain (NOD) cell signaling inhibitors based on a 3,5-diphenyl-2-aminopyridine scaffold.

Suebsuwong C. et al, (2020), European journal of medicinal chemistry, 200

Targeting ALK2: An Open Science Approach to Developing Therapeutics for the Treatment of Diffuse Intrinsic Pontine Glioma.

Ensan D. et al, (2020), Journal of medicinal chemistry, 63, 4978 - 4996

A Highly Selective Chemical Probe for Activin Receptor-like Kinases ALK4 and ALK5

Hanke T. et al, (2020), ACS Chemical Biology

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