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Publications

Discovery of Conformationally Constrained ALK2 Inhibitors.

González-Álvarez H. et al, (2024), J Med Chem

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 Chem Neurosci

Author Correction: CIS is a potent checkpoint in NK cell-mediated tumor immunity.

Delconte RB. et al, (2023), Nat Immunol

Target 2035 - an update on private sector contributions.

Ackloo S. et al, (2023), RSC Med Chem, 14, 1002 - 1011

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), bioRxiv

Structural and biochemical characterization establishes a detailed understanding of KEAP1-CUL3 complex assembly

Adamson RJ. et al, (2023)

A Potent and Selective CDKL5/GSK3 Chemical Probe is Neuroprotective.

Ong HW. et al, (2023), bioRxiv

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

Chen Z. et al, (2022), Biochem J

Target 2035 - update on the quest for a probe for every protein.

Müller S. et al, (2022), RSC Med Chem, 13, 13 - 21

Ubiquitin ligases: guardians of mammalian development.

Cruz Walma DA. et al, (2022), Nat Rev Mol Cell Biol

Development of a Selective Dual Discoidin Domain Receptor (DDR)/p38 Kinase Chemical Probe.

Röhm S. et al, (2021), J Med Chem, 64, 13451 - 13474

PRMT5 inhibition reduces viability and stemness of pediatric high grade glioma.

Brown EJ. et al, (2021), CANCER RESEARCH, 81

Saracatinib is an efficacious clinical candidate for fibrodysplasia ossificans progressiva.

Williams E. et al, (2021), JCI Insight, 6

Challenges and Opportunities for Drug Repositioning in Fibrodysplasia Ossificans Progressiva.

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

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

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

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

Schröder M. et al, (2020), J Med Chem, 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), J Med Chem, 63, 10061 - 10085

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), Eur J Med Chem, 200

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

Chen Z. et al, (2020)

Identification of a PGXPP degron motif in dishevelled and structural basis for its binding to the E3 ligase KLHL12.

Chen Z. et al, (2020), Open Biol, 10

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