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Identification of the gene that codes for the σ2 receptor
Significance Of the many receptors that were pharmacologically described during the 20th century, almost all were cloned by the end of the 1990s. A key exception is the σ2 receptor, a potentialExpand
Thermodynamic and structural effects of conformational constraints in protein-ligand interactions. Entropic paradoxy associated with ligand preorganization.
Succinate- and cyclopropane-derived phosphotyrosine (pY) replacements were incorporated into a series of Grb2 SH2 binding ligands wherein the pY+1 residue was varied to determine explicitly howExpand
Phosphatidylcholine-Preferring Phospholipase C from B. cereus. Function, Structure, and Mechanism
The PLC class of enzymes has been studied extensively over the past 15–20 years because of their involvement in signaling pathways in which extracellular messages are delivered to the cell to induceExpand
Structural and energetic aspects of Grb2-SH2 domain-swapping.
The SH2 domain of growth factor receptor-bound protein 2 (Grb2) has been the focus of numerous studies, primarily because of the important roles it plays in signal transduction. More recently, it hasExpand
Applications of multicomponent reactions to the synthesis of diverse heterocyclic scaffolds.
The sequencing of multicomponent reactions (MCRs) and subsequent cyclization reactions is a powerful stratagem for the rapid synthesis of diverse heterocyclic scaffolds. The optimal MCR isExpand
Applications of multicomponent reactions for the synthesis of diverse heterocyclic scaffolds.
A four-component coupling process involving sequential reactions of aldehydes, primary amines, acid chlorides, and nucleophiles has been developed to prepare multifunctional substrates that may beExpand
Sigma 2 Receptor/Tmem97 Agonists Produce Long Lasting Antineuropathic Pain Effects in Mice.
Neuropathic pain is an important medical problem with few effective treatments. The sigma 1 receptor (σ1R) is known to be a potential target for neuropathic pain therapeutics, and antagonists forExpand
Probing the effect of conformational constraint on phosphorylated ligand binding to an SH2 domain using polarizable force field simulations.
Preorganizing a ligand in the conformation it adopts upon binding to a protein has long been considered to be an effective way to improve affinity by making the binding entropy more favorable.Expand