X‐ray crystal structuresG proteinヽoupled receptors (GPCRs) are the largest family of membrane proteins. GPCRs are involved in a wide variety of cellular functions, serving as key players in cellular signaling.
Hoffmann 1✉ G protein-coupled receptors (GPCRs) activate G proteins and undergo a complex regulation by interaction with GPCR kinases (GRKs) and the formation of receptor–arrestin complexes. However, the impact of individual GRKs on arrestin binding is not clear. We report the creation of ...
While G-protein coupled receptors (GPCRs) represent a highly druggable target (20 % of all drugs approved since 1983), the ‘golden age of GPCR structural biology’ starting in the early 2000s further drove the elucidation of their three-dimensional (3D) structures [8]. Consequently, specific...
Drug discovery, however, is a time-consuming, pricey, and dangerous endeavor. Artificial intelligence (AI) has become a potent instrument that has transformed several industries, including healthcare, in recent years. This summary gives a general overview of how AI is expediting the creation of ...
EXPERT OPINION ON DRUG DISCOVERY 2024, VOL. 19, NO. 8, 887–915 https://doi.org/10.1080/17460441.2024.2367023 PERSPECTIVE Phage display technology and its impact in the discovery of novel protein-based drugs Catherine J. Hutchingsa and Aaron K. Satob aIndependent Consultant, UK; bTwist ...
G protein-coupled receptors (GPCRs) activate G proteins and undergo a complex regulation by interaction with GPCR kinases (GRKs) and the formation of receptor–arrestin complexes. However, the impact of individual GRKs on arrestin binding is not clear. W
(serine 473 and threonine 308). PI3Ks are activated by growth factors through GPCR or RTK receptors. The PI3K activation results in the conversion of PtdIns(4,5)P2 (PIP2) to PtdIns(3,4,5)P3 (PIP3), a process that is reversed by the phosphatase PTEN. Then PIP3 interacts with the ...
nearly half of the pharmacologic gene targets fall into just six gene families: G-protein-coupled receptors (GPCRs), serine/threonine and tyrosine protein kinases, zinc metallopeptidases, serine proteases, nuclear hormone receptors and phosphodiesterases41. Moreover, many large gene families are locali...
Thus, modulation of this large signaling family has potential for chronic disease treatment. There are representative experimentally determined structures within each of the three receptor families. We are designing selective agonists, antagonists and allosteric modulators of purinergic GPCRs. Examples of ...
The proposed method was validated using human leukotriene B4 receptor BLT1 as a sample GPCR. The obtained accurate information on structures of GPCRs is expected to accelerate the research activity by being used in the computer-assisted drug design.Yoko Ishino...