Pharmacotrafficking Assays

Identify Pharmacochaperones that Rescue Disease Relevant Mutant Membrane Proteins

Small molecule pharmacochaperones function as protein chaperones to rescue and guide misfolded proteins from the endoplasmic reticulum (ER) to their intended cellular location. Mutated misfolded GPCRs, ion channels, or transporters trapped in the ER are unable to move to the plasma membrane and can lead to diseases such as cystic fibrosis, obesity, diabetes, cardiac arrhythmias, and more.

Pharmacochaperones act as therapeutic agents to stabilize and correct the misfolded protein and allow for the proteins’ proper trafficking from the ER to the plasma membrane to prevent the disease.

Utilize Eurofins DiscoverX® PathHunter® cell-based pharmacotrafficking assays to identify, characterize, and optimize pharmacochaperones. These homogeneous cell-based assays are easy-to-use, quantitative, and provide a superior alternative to imaging or antibody-based methods.

Product Highlights
  • Extensive Portfolio – Cell lines, custom assays, and toolbox products applicable for disease relevant mutant GPCRs, ion channels, and transporters
  • Small Molecule Discovery – Assays to identify small molecule pharmacological chaperones that rescue or correct several disease relevant mutant membrane proteins
  • Scalable – Homogenous quantitative, easy-to-use assays amenable for low, medium, and high throughput screening (HTS) programs
  • Superior Readout — Antibody- and image-free assays with a sensitive chemiluminescent read-out

Consider Eurofins DiscoverX’s custom development capabilities for custom cell lines, assays, & enzyme development.

SHOP PRODUCTSGPCR SOLUTIONSION CHANNEL SOLUTIONSDOWNLOAD EBOOK

Products

Target Class Target Protein Description Disease Relevance Readout
GPCR ADRB2(W158A) Adrenergic receptor beta 2 Endosome – EA
GPCR AVPR2(S167T) Vasopressin receptor 2 Nephrogenic diabetes insipidus Endosome – EA
Ion Channel CFTR-ΔF508 Cystic fibrosis transmembrane conductance regulator Cystic fibrosis Membrane – EA
Ion Channel KCNH2(G601S) Potassium voltage-gated channel, subfamily H (eag-related), member 2 Long QT syndrome (Cardiac arrhythmias) Membrane – EA
GPCR MC4R(T162I) Melanocortin 4 receptor ObesityEndosome – EA
GPCR mRHO(P23H) Rhodopsin Retinitis pigmentosa Endosome & Membrane – EA
GPCR SMO(W535L) Smoothened frizzled family receptor Basal skin cell carcinomas Membrane – EA

Parental Cell Lines – Engineered cells to generate your own pharmacotrafficking assays and investigate trafficking of your target protein to the plasma membrane, nucleus, or endosome