Trends in kinase drug discovery: targets, indications and inhibitor design
The FDA approval of imatinib in 2001 was a breakthrough in molecularly targeted cancer
therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology …
therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology …
[HTML][HTML] 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 …
GPCRdb in 2021: integrating GPCR sequence, structure and function
AJ Kooistra, S Mordalski… - Nucleic Acids …, 2021 - academic.oup.com
G protein-coupled receptors (GPCRs) form both the largest family of membrane proteins and
drug targets, mediating the action of one-third of medicines. The GPCR database, GPCRdb …
drug targets, mediating the action of one-third of medicines. The GPCR database, GPCRdb …
GPCRdb in 2023: state-specific structure models using AlphaFold2 and new ligand resources
G Pándy-Szekeres, J Caroli, A Mamyrbekov… - Nucleic acids …, 2023 - academic.oup.com
G protein-coupled receptors (GPCRs) are physiologically abundant signaling hubs routing
hundreds of extracellular signal substances and drugs into intracellular pathways. The …
hundreds of extracellular signal substances and drugs into intracellular pathways. The …
Sequencing of 640,000 exomes identifies GPR75 variants associated with protection from obesity
INTRODUCTION Obesity accounts for a substantial and growing burden of disease globally.
Body adiposity is highly heritable, and human genetic studies can lead to biological and …
Body adiposity is highly heritable, and human genetic studies can lead to biological and …
[HTML][HTML] Trends in antidiabetic drug discovery: FDA approved drugs, new drugs in clinical trials and global sales
AD Dahlén, G Dashi, I Maslov, MM Attwood… - Frontiers in …, 2022 - frontiersin.org
Type 2 diabetes mellitus (T2DM) continues to be a substantial medical problem due to its
increasing global prevalence and because chronic hyperglycemic states are closely linked …
increasing global prevalence and because chronic hyperglycemic states are closely linked …
An atlas of the protein-coding genes in the human, pig, and mouse brain
INTRODUCTION The brain is the most complex organ of the mammalian body, boasting a
diverse physiology combined with intricate cellular organization. In an effort to expand our …
diverse physiology combined with intricate cellular organization. In an effort to expand our …
[HTML][HTML] Receptor-associated independent cAMP nanodomains mediate spatiotemporal specificity of GPCR signaling
SE Anton, C Kayser, I Maiellaro, K Nemec, J Möller… - Cell, 2022 - cell.com
G protein-coupled receptors (GPCRs) relay extracellular stimuli into specific cellular
functions. Cells express many different GPCRs, but all these GPCRs signal to only a few …
functions. Cells express many different GPCRs, but all these GPCRs signal to only a few …
[HTML][HTML] 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 …
[HTML][HTML] Common activation mechanism of class A GPCRs
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …
physiology. Understanding receptor activation mechanism is critical for discovering novel …