WNT stimulation induces dynamic conformational changes in the Frizzled-Dishevelled interaction
CF Bowin, P Kozielewicz, L Grätz, M Kowalski-Jahn… - Science …, 2023 - science.org
Frizzleds (FZDs) are G protein–coupled receptors (GPCRs) that bind to WNT family ligands.
FZDs signal through multiple effector proteins, including Dishevelled (DVL), which acts as a …
FZDs signal through multiple effector proteins, including Dishevelled (DVL), which acts as a …
[HTML][HTML] A conserved molecular switch in Class F receptors regulates receptor activation and pathway selection
…, M Kowalski-Jahn, J Petersen, CF Bowin… - Nature …, 2019 - nature.com
Class F receptors are considered valuable therapeutic targets due to their role in human
disease, but structural changes accompanying receptor activation remain unexplored. …
disease, but structural changes accompanying receptor activation remain unexplored. …
[HTML][HTML] Structural insight into small molecule action on Frizzleds
WNT-Frizzled (FZD) signaling plays a critical role in embryonic development, stem cell
regulation and tissue homeostasis. FZDs are linked to severe human pathology and are seen as …
regulation and tissue homeostasis. FZDs are linked to severe human pathology and are seen as …
[HTML][HTML] Cryo-EM structure of constitutively active human Frizzled 7 in complex with heterotrimeric Gs
…, GW Han, M Kowalski-Jahn, P Kozielewicz, CF Bowin… - Cell research, 2021 - nature.com
Dear Editor, The ten mammalian Frizzleds (FZD1–10) belong to the class F of G protein-coupled
receptors (GPCRs) and mediate WNT signaling through interaction with transducer …
receptors (GPCRs) and mediate WNT signaling through interaction with transducer …
Quantitative profiling of WNT-3A binding to all human frizzled paralogues in HEK293 cells by NanoBiT/BRET assessments
…, R Shekhani, S Moser, CF Bowin… - ACS Pharmacology & …, 2021 - ACS Publications
The WNT signaling system governs critical processes during embryonic development and
tissue homeostasis, and its dysfunction can lead to cancer. Details concerning selectivity and …
tissue homeostasis, and its dysfunction can lead to cancer. Details concerning selectivity and …
[HTML][HTML] Residue 6.43 defines receptor function in class F GPCRs
The class Frizzled of G protein-coupled receptors (GPCRs), consisting of ten Frizzled (FZD 1-10
) subtypes and Smoothened (SMO), remains one of the most enigmatic GPCR families. …
) subtypes and Smoothened (SMO), remains one of the most enigmatic GPCR families. …
[HTML][HTML] WNT-3A–induced β-catenin signaling does not require signaling through heterotrimeric G proteins
CF Bowin, A Inoue, G Schulte - Journal of biological chemistry, 2019 - ASBMB
The network of Wingless/Int-1 (WNT)-induced signaling pathways includes β-catenin–dependent
and –independent pathways. β-Catenin regulates T cell factor/lymphoid enhancer–…
and –independent pathways. β-Catenin regulates T cell factor/lymphoid enhancer–…
A NanoBRET-based binding assay for smoothened allows real-time analysis of ligand binding and distinction of two binding sites for BODIPY-cyclopamine
Smoothened (SMO) is a GPCR that mediates hedgehog signaling. Hedgehog binds the
transmembrane protein Patched, which in turn regulates SMO activation. Overactive SMO …
transmembrane protein Patched, which in turn regulates SMO activation. Overactive SMO …
SAG1. 3-derived Frizzled-targeting negative allosteric modulators
Exaggerated Wingless/Int1 (WNT)/Frizzled (FZD) signaling contributes to pathologies
including fibrosis and different forms of cancers. Thus, targeting FZDs as WNT receptors for …
including fibrosis and different forms of cancers. Thus, targeting FZDs as WNT receptors for …
WNT stimulation induced conformational dynamics in the Frizzled-Dishevelled interaction
CF Bowin, P Kozielewicz, L Grätz, M Kowalski-Jahn… - bioRxiv, 2022 - biorxiv.org
Frizzleds (FZD 1-10 ) are G protein-coupled receptors containing an extracellular cysteine-rich-domain
(CRD) that presents the orthosteric binding site of the 19 mammalian WNTs, the …
(CRD) that presents the orthosteric binding site of the 19 mammalian WNTs, the …