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 …
(GPCRs) have experienced a transformation from random ligand screening to knowledge …
Applications of nanobodies
S Muyldermans - Annual review of animal biosciences, 2021 - annualreviews.org
Unique, functional, homodimeric heavy chain–only antibodies, devoid of light chains, are
circulating in the blood of Camelidae. These antibodies recognize their cognate antigen via …
circulating in the blood of Camelidae. These antibodies recognize their cognate antigen via …
Drug-induced phospholipidosis confounds drug repurposing for SARS-CoV-2
TA Tummino, VV Rezelj, B Fischer, A Fischer… - Science, 2021 - science.org
Repurposing drugs as treatments for COVID-19, the disease caused by severe acute
respiratory syndrome coronavirus 2 (SARS-CoV-2), has drawn much attention. Beginning …
respiratory syndrome coronavirus 2 (SARS-CoV-2), has drawn much attention. Beginning …
Activation pathway of a G protein-coupled receptor uncovers conformational intermediates as targets for allosteric drug design
S Lu, X He, Z Yang, Z Chai, S Zhou, J Wang… - Nature …, 2021 - nature.com
G protein-coupled receptors (GPCRs) are the most common proteins targeted by approved
drugs. A complete mechanistic elucidation of large-scale conformational transitions …
drugs. A complete mechanistic elucidation of large-scale conformational transitions …
Conformational basis of G protein-coupled receptor signaling versatility
G protein-coupled receptors (GPCRs) are privileged structural scaffolds in biology that have
the versatility to regulate diverse physiological processes. Interestingly, many GPCR ligands …
the versatility to regulate diverse physiological processes. Interestingly, many GPCR ligands …
The angiotensin AT2 receptor: from a binding site to a novel therapeutic target
Discovered more than 30 years ago, the angiotensin AT 2 receptor (AT 2 R) has evolved
from a binding site with unknown function to a firmly established major effector within the …
from a binding site with unknown function to a firmly established major effector within the …
Advances in therapeutic peptides targeting G protein-coupled receptors
Dysregulation of peptide-activated pathways causes a range of diseases, fostering the
discovery and clinical development of peptide drugs. Many endogenous peptides activate G …
discovery and clinical development of peptide drugs. Many endogenous peptides activate G …
Molecular mechanism of biased signaling in a prototypical G-protein-coupled receptor
Over one-third of current drugs target G-protein-coupled receptors (GPCRs). Leveraging the
phenomenon of biased signaling, where different ligands that bind to the same GPCR …
phenomenon of biased signaling, where different ligands that bind to the same GPCR …
Heterotrimeric Gq proteins act as a switch for GRK5/6 selectivity underlying β-arrestin transducer bias
Signaling-biased ligands acting on G-protein-coupled receptors (GPCRs) differentially
activate heterotrimeric G proteins and β-arrestins. Although a wealth of structural knowledge …
activate heterotrimeric G proteins and β-arrestins. Although a wealth of structural knowledge …
Celastrol attenuates angiotensin II–induced cardiac remodeling by targeting STAT3
S Ye, W Luo, ZA Khan, G Wu, L Xuan, P Shan… - Circulation …, 2020 - Am Heart Assoc
Rationale: Excessive Ang II (angiotensin II) levels lead to a profibrotic and hypertrophic
milieu that produces deleterious remodeling and dysfunction in hypertension-associated …
milieu that produces deleterious remodeling and dysfunction in hypertension-associated …