Membrane Proteins Applications


Because mutations and misfolding of membrane proteins have been associated with many known diseases such heart disease, cystic fibrosis, depression, obesity, cancer and many others, membrane proteins have been widely used in drug discovery in the field of medicine. Currently approximately 60% of available drugs target membrane proteins of which G protein-coupled receptors (GPCRs) and ion channels constitute the largest groups, followed by transporters and kinases. Analysis of drug targets approved by the US Food and Drug Administration (FDA) in 2016 found that GPCR and ion channels accounted for 33% and 18% of small molecule therapeutics, respectively. In this context, drugs based on GPCRs have been developed for diseases such as asthma, hypertension, rhinitis, schizophrenia, pain, migraine and prostate cancer.

Representative examples of therapeutically-relevant membrane protein structures.Fig. 1. Representative examples of therapeutically-relevant membrane protein structures.

Applications in Practice

Membrane proteins as targets have been widely in drug discovery, and the Table 1 illustrates some specific examples [1].

Table.1 Examples of recent drug discovery using membrane proteins.

TargetTarget typeDisease indication(s)Therapeutic typeDiscovery platform
NTS1GPCR: neurotensin receptorInflammation, cancer, addictionSmall moleculeHTS fluorescence polarization assay
CCR5GPCR: chemokine receptorHIVmAbDNA immunization (chicken) boosted w/purified protein
CB1GPCR: cannabinoid receptorVariousmAbImmunization (mouse hybridoma) plus phage display
CCR1GPCR: chemokine receptorAutoimmune diseasesmAbNaïve library (yeast-based) screened with cells; purified protein was used for affinity maturation
AT1RGPCR: angiotensin II receptorHypertension, kidney diseasemAbSynthetic library (yeast-based) screened with purified protein
ASIC1aAcid-sensing ion channelStrokemAbscFv phage library
P2X4Ligand-gated ion channelNeuropathic painmAbNaïve scFv phage library
P2X3Ligand-gated ion channelNeuropathic painmAbImmunization (mouse hybridoma)
TRPM8Ion channelNeuropathic painSmall moleculeSBDD/molecular modeling using cryo-EM structures
ENT1SLC transporterIschemia, pancreatic cancermAbSynthetic library (ribosome display) screened with purified protein
ASCT2SLC transporterTumorsSmall moleculeSBDD/virtual screening using a homology model based on EAAT1 structure
APJGPCR: apelin receptorChronic heart failuremAbimmunization (camel) with SBDD
Orexin receptorsGPCRInsomniaSmall moleculeSBDD
MC4RGPCRObesitySmall moleculeSBDD
CGRP receptorGPCRMigraineSmall moleculeSBDD
TREK-1Ion channelDepressionSmall moleculeSBDD using molecular dynamics to model an intermediate conformational state based on TREK-2 structures
GLUT5SLC transporterCancersSmall moleculeSBDD (virtual screening) plus liposome assay
GlyT1SLC transporterNervous system disordersmAbSynthetic library (ribosome display) screened w/purified protein
Various K+ channelsIon channelVariousSmall moleculeHTS of compound library
TrpV5Ion channelkidney diseasesSmall moleculeStructure-based virtual screening
Kv1.3Voltage-gated ion channelAutoimmune diseasesmAbImmunization (chicken) with proteoliposomes; screening of B cells with magnetic beads
GCGRGPCR: glucagon receptorMetabolic disordersmAbDNA immunization (llamas), phage selections with VLPs
CXCR4GPCR: chemokine receptorCancer, fibrosismAbPhage library of single-domain antibodies
P2X3ligand-gated ion channelNeuropathic painmAbImmunization (chicken)
GLUT4SLC transporterType 2 diabetesmAbImmunization (chicken)
DRD1GPCR: dopamine receptorCerebral meningiomamAbImmunization (mouse)
Claudin-5Structural (tight junctions)Neurodegenerative disordersmAbImmunization (mouse)

Alfa Chemistry can produce high-quality native membrane protein targets and our technology maintains the structural and functional integrity of membrane protein targets, facilitating accurate discovery of drug. Meanwhile, we provide a wide range of membrane protein services such as membrane proteins solubilization and stabilization, membrane proteins purification, membrane proteins characterization, membrane proteins structural determination and so on, which will provide you with strong technical support for drug discovery. Our high-quality native, pure, stable membrane proteins are the preferred target for drug discovery scientists. Please feel free to contact us for more details.


  1. Gulezian E., et al. Membrane protein production and formulation for drug discovery[J]. Trends in Pharmacological Sciences, 2021, 42(8): 657-674.

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