There are two ways to study receptor responsiveness in cultured cell lines: use a cell line...

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Biology

There are two ways to study receptor responsiveness in culturedcell lines: use a cell line that naturally expresses the receptorof interest; and transfect a cell line with a gene for the receptoryou are interested in in order to ensure large numbers of thisreceptor. Taking into consideration what you know about Gprotein-coupled receptors and about measurement in pharmacology,briefly discuss what the possible advantage(s) and disadvantage(s)might be of each of these approaches.

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ANswer One of the greatest technical and theoretical challenges to elucidating and exploiting structurefunction relationships in these systems is the emerging concept of GPCR conformational flexibility and its causeeffect relationship for receptorreceptor and receptoreffector interactions Such conformational changes can be subtle and triggered by relatively small binding energy effects leading to full or partial efficacy in the activation or inactivation of the receptor system at large GPCR structurefunction A principal hallmarks of GPCR structure include a serpentine transmembrane topology compsed of seven helical hydrophobic stretches interspersed by intraand extracellular loops of indeterminate structure This results in the presentation of an extracellular amino and cytoplasmic carboxyl terminus The N terminus and extracellular loops can be glycosylated to varying degrees and extracellular loops 1 and 2 are connected via a disulfide linkage required for stability and function of the receptor The Cterminal tail is anchored to the intracellular face of the lipid bilayer via palmitoylation to produce a short intracellular loop which typically forms See Answer

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