Binding, gating, a nity and e cacy Page 1 SEMINAR Binding, gating, a nity and e cacy The nature
of the problem Some history The classical era The interaction between binding and conformation …

The past decade has witnessed a significant growth in the identification of allosteric
modulators of G protein–coupled receptors (GPCRs), ie, ligands that interact with binding …

We have replaced the C-terminal portion of the third intracellular loop of the beta 2-
adrenergic receptor (residues 266-272) with the homologous region of the alpha 1B …

The human β-adrenoceptor is a member of the seven-transmembrane family of receptors,
encoded by a gene on chromosome 5. β-Adrenoceptors have been classified into β1, β2 …

The β 1-adrenergic receptor (β 1 AR) is a key cell surface signaling protein expressed in the
heart and other organs that mediates the actions of catecholamines of the sympathetic …

Adrenoceptors are prototypic members of the superfamily of seven transmembrane domain,
G protein-coupled receptors. Study of the properties of several mutationally activated …

There are many examples of a single receptor coupling directly to more than one cellular
signal transduction pathway. Although traditional receptor theory allows for activation of …

Over the past few years, the concept that the activation of G protein-coupled receptors and
transmitter-gated ion channels depends on a conformational change has received …

Some G-protein-coupled receptors display 'constitutive activity', that is, spontaneous activity
in the absence of agonist,,,. This means that a proportion of the receptor population …

Environmental stimuli that are reliably associated with the effects of many abused drugs,
especially stimulants such as cocaine, can produce craving and relapse in abstinent human …