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 …
Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials
Undruggable proteins are a class of proteins that are often characterized by large, complex
structures or functions that are difficult to interfere with using conventional drug design …
structures or functions that are difficult to interfere with using conventional drug design …
GPCR activation mechanisms across classes and macro/microscales
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 …
coupled receptors (GPCR) belonging to four classes: A, B1, C and F. Whereas a model of …
The good, the bad, and the opportunities of the complement system in neurodegenerative disease
ND Schartz, AJ Tenner - Journal of Neuroinflammation, 2020 - Springer
The complement cascade is a critical effector mechanism of the innate immune system that
contributes to the rapid clearance of pathogens and dead or dying cells, as well as …
contributes to the rapid clearance of pathogens and dead or dying cells, as well as …
Clinical promise of next-generation complement therapeutics
The complement system plays a key role in pathogen immunosurveillance and tissue
homeostasis. However, subversion of its tight regulatory control can fuel a vicious cycle of …
homeostasis. However, subversion of its tight regulatory control can fuel a vicious cycle of …
Therapeutic targeting of the complement system: from rare diseases to pandemics
P Garred, AJ Tenner, TE Mollnes - Pharmacological reviews, 2021 - ASPET
The complement system was discovered at the end of the 19th century as a heat-labile
plasma component that “complemented” the antibodies in killing microbes, hence the name …
plasma component that “complemented” the antibodies in killing microbes, hence the name …
Advances in therapeutic peptides targeting G protein-coupled receptors
AP Davenport, CCG Scully, C de Graaf… - Nature Reviews Drug …, 2020 - nature.com
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 …
[HTML][HTML] Systemic delivery of peptides by the oral route: Formulation and medicinal chemistry approaches
In its 33 years, ADDR has published regularly on the po5tential of oral delivery of biologics
especially peptides and proteins. In the intervening period, analysis of the preclinical and …
especially peptides and proteins. In the intervening period, analysis of the preclinical and …
Structure of an allosteric modulator bound to the CB1 cannabinoid receptor
The CB1 receptor mediates the central nervous system response to cannabinoids, and is a
drug target for pain, anxiety and seizures. CB1 also responds to allosteric modulators, which …
drug target for pain, anxiety and seizures. CB1 also responds to allosteric modulators, which …
Molecular recognition of formylpeptides and diverse agonists by the formylpeptide receptors FPR1 and FPR2
The formylpeptide receptors (FPRs) mediate pattern recognition of formylated peptides
derived from invading pathogens or mitochondria from dead host cells. They can also sense …
derived from invading pathogens or mitochondria from dead host cells. They can also sense …