However, the ligand-binding modes of FPR2 remain elusive, thereby limiting the development of potential drugs. Here we report the crystal structure of FPR2 bound to the potent peptide agonist WKYMVm at 2.8 resolution. The structure adopts an active conformation and exhibits a deep ligand-binding ...
(35–45%)13,14,15,16,17. This mutation may introduce extra hydrophobic interactions with its neighboring residues on the external surface of the receptor, aiming for better protein stability. Functional assays indicate that the above modifications have little effect on ligand binding and receptor ...
The ligand is considered to quickly activate upon exposure to various external stimuli. Lens epithelial cells also up-regulate ligands and receptors (Saika et al., 2000a). The potential mechanisms of TGFβ activation include the roles of thrombospondin-1, integrinαvβ5, matrix metaloproteinase-...
(and flg22) is the ligand for FLAGELLIN-SENSING 2 (FLS2), a receptor in plant cell membranes. FLS2 is similar in structure to, for example, the Pep receptors (PEPRs), which bind the endogenous plant elicitor peptides (Peps) [10]. Plants also employ endogenous signaling compounds called...
These receptors represent useful molecular targets for the detection and treatment of cancer since they are located on the plasma membrane and upon binding of a radiopeptide the receptor–ligand complex is internalized, allowing sufficiently long retention of radioactivity in tumor cells for efficient ...
Still WC (1996) Discovery of sequence-specific peptide binding by synthetic receptors using encoded combinatorial libraries. Acc Chem Res 29: 155–163... WC Still - 《Cheminform》 被引量: 633发表: 1996年 ChemInform Abstract: Prediction of Ligand-Receptor Binding Thermodynamics by Free Energy Force...
The prolactin-releasing peptide receptor and its bioactive RF-amide peptide (PrRP20) have been investigated to explore the ligand binding mode of peptide G-protein-coupled receptors (GPCRs). By receptor mutagenesis, we identified the conserved aspartate in the upper transmembrane helix 6 (Asp(6.59...
ICAM-1 is a key adhesion molecule on epithelial cells that acts as a ligand to the integrins receptors on polymorphonuclear leukocytes, mediating their recruitment and migration into tissues. ICAM-1 is typically expressed at low levels; however, its expression is up-regulated during sepsis and infl...
immune cells, and so forth, by interacting with specific receptors located on the plasma membrane of target cells. Most of them transmit their signal via guanosine triphosphate (GTP)-binding protein-receptor coupling and thereby trigger changes of membrane-bound enzymes and second messenger levels(3...
Table 2. Heart of the binding interface of various checkpoint protein–protein interactions ReceptorInteracting domainLigandInteracting domain; PDB code CTLA-4 FG loop B7-1 GFCC′ strands surface (25); 1I8L FG loop and CC′ strands B7-2 GFCC′C″ strands and the CC′, C″D, and FG loop...