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 ...
“lid” conformation that stacks on top of the ligand-binding pocket of FPR2 (Fig.1b). However, the structure does not rule out the possibility that the conformation of the receptor N terminus was affected by the N-terminal bRIL fusion protein, which is involved in mediating crystal packing...
cyclase (GC) domain that is linked to Ca2+level elevation [56]. The portions of LRR-RLKs that contain LRRs serve as the ligand-binding domains of these proteins [61]. For example, the LRR regions of FLS2 bind flg22 in the extracellular portion of this receptor [62]. LRR domains in ...
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 ...
Ligand-based peptide design and combinatorial peptide libraries to target G protein-coupled receptors. Curr. Pharm. Des. 16, 3071–3088 (2010). Article CAS PubMed PubMed Central Google Scholar Cragg, G. M. & Newman, D. J. Natural products: a continuing source of novel drug leads. ...
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...
Binding cleft formed via residues in both the CC′ and FG loops (33,36); 2OYP, 6DHB CEACAM Heterophilic interactions of Ceacam1 and Tim-3 along their FG-CC′ interface (37); 4QXW Metal ion-dependent ligand-binding site in FG loop (33,34,38); 2OYP, 3BIB, HMBG1 A-box domain of...
KIR Polymorphisms Modulate Peptide-Dependent Binding to an MHC Class I Ligand with a Bw6 Motif Molecular interactions between killer immunoglobulin-like receptors (KIRs) and their MHC class I ligands play a central role in the regulation of natural k... AD Colantonio,BN Bimber,WJ Neidermyer,....
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...