The Wnt pathway: from signaling mechanisms to synthetic modulators

EY Rim, H Clevers, R Nusse - Annual review of biochemistry, 2022 - annualreviews.org
The Wnt pathway is central to a host of developmental and disease-related processes. The
remarkable conservation of this intercellular signaling cascade throughout metazoan …

G protein-coupled receptors: structure-and function-based drug discovery

D Yang, Q Zhou, V Labroska, S Qin… - Signal transduction and …, 2021 - nature.com
As one of the most successful therapeutic target families, G protein-coupled receptors
(GPCRs) have experienced a transformation from random ligand screening to knowledge …

GPCR activation mechanisms across classes and macro/microscales

AS Hauser, AJ Kooistra, C Munk… - Nature structural & …, 2021 - nature.com
Two-thirds of human hormones and one-third of clinical drugs activate~ 350 G-protein-
coupled receptors (GPCR) belonging to four classes: A, B1, C and F. Whereas a model of …

Structural basis of GABA reuptake inhibition

Z Motiwala, NG Aduri, H Shaye, GW Han, JH Lam… - Nature, 2022 - nature.com
Abstract γ-Aminobutyric acid (GABA) transporter 1 (GAT1) regulates neuronal excitation of
the central nervous system by clearing the synaptic cleft of the inhibitory neurotransmitter …

A method for structure determination of GPCRs in various states

Q Guo, B He, Y Zhong, H Jiao, Y Ren, Q Wang… - Nature Chemical …, 2024 - nature.com
G-protein-coupled receptors (GPCRs) are a class of integral membrane proteins that detect
environmental cues and trigger cellular responses. Deciphering the functional states of …

Structure determination of inactive-state GPCRs with a universal nanobody

MJ Robertson, MM Papasergi-Scott, F He… - Nature Structural & …, 2022 - nature.com
Cryogenic electron microscopy (cryo-EM) has widened the field of structure-based drug
discovery by allowing for routine determination of membrane protein structures previously …

Cryo-EM structure determination of small proteins by nanobody-binding scaffolds (Legobodies)

X Wu, TA Rapoport - Proceedings of the National Academy of Sciences, 2021 - pnas.org
We describe a general method that allows structure determination of small proteins by single-
particle cryo-electron microscopy (cryo-EM). The method is based on the availability of a …

[HTML][HTML] New insights into GPCR coupling and dimerisation from cryo-EM structures

A Gusach, J García-Nafría, CG Tate - Current Opinion in Structural Biology, 2023 - Elsevier
Over the past three years (2020–2022) more structures of GPCRs have been determined
than in the previous twenty years (2000–2019), primarily of GPCR complexes that are large …

Structure, function and drug discovery of GPCR signaling

L Cheng, F **a, Z Li, C Shen, Z Yang, H Hou… - Molecular …, 2023 - Springer
G protein-coupled receptors (GPCRs) are versatile and vital proteins involved in a wide
array of physiological processes and responses, such as sensory perception (eg, vision …

Understanding the molecular mechanisms of odorant binding and activation of the human OR52 family

C Choi, J Bae, S Kim, S Lee, H Kang, J Kim… - Nature …, 2023 - nature.com
Structural and mechanistic studies on human odorant receptors (ORs), key in olfactory
signaling, are challenging because of their low surface expression in heterologous cells …