Protein Engineering of GPCR

Protein Engineering of GPCR

For Research Use Only. Not For Clinical Use.

Creative Biolabs has years of experience in providing professional services for protein engineering of GPCR to facilitate the cutting-edge programs of GPCR research and drug development.

Introduction of Protein Engineering

G protein-coupled receptors (GPCRs) are the most diverse group of membrane receptors in eukaryotes. They perform many of the essential functions required for life. GPCRs have many potential uses in biotechnological processes and are often the drug targets of multiple diseases. The knowledge gap in GPCR research is a major bottleneck in the development of future biotechnological and biomedical advances. Therefore, it is important and necessary to understand them and manipulate their functions. Protein engineering plays a central role to design and construct GPCRs with desired properties and functions.

Protein engineering is the process of developing useful or valuable unnatural proteins through rational protein design or directed evolution. Rational design is the most classical method used for proteins with well-known structure and mechanism. Directed evolution is a more practical approach for proteins with limited structure information and unclear mechanism. These two methods are not mutually exclusive. Protein engineering is a powerful tool to precisely characterize protein structure and tune GPCR function for a desired application. With the development of modern protein engineering techniques, there will be numerous ways to overcome these challenges in GPCR production and research.

Figure 1. Comparison of rational protein engineering (left) and directed protein evolution (right). (Kang M K & Tullman-Ercek D, 2018)Figure 1. Comparison of rational protein engineering (left) and directed protein evolution (right). (Kang M K & Tullman-Ercek D, 2018)

Our Services

We have long-term devoted to protein engineering of GPCRs and are capable to provide customized services for protein engineering based on both rational design and directed evolution. Our extensive experience and advanced platform will help our customers accelerate their project process.

Rational Design

Detailed knowledge of the protein structure and function is required in rational design. Site-specific mutagenesis, chemical modification and computational techniques are commonly used to make desired changes. Rational design provides an efficient and economical strategy to engineering GPCRs.

Directed Evolution

Directed evolution can mimic the process of natural selection to steer proteins toward a user-defined goal without knowing the structure and function of the protein in advance. It is an alternative method to rational design and has proved to be an effective strategy for altering or improving the activity of proteins for research, therapeutic and industrial applications.

Semi-Rational Approaches

Semi-rational approaches are the combination of rational design and directed evolution to address the limitations of both methods.

Creative Biolabs is always ready to provide the best services to each of our customers. If you are interested in our services or have any specific requirements, please feel free to contact us for more details.


  1. Kang M K & Tullman-Ercek D. Engineering expression and function of membrane proteins. Methods, 2018, 147: 66-72.
  2. Lluis M W, et al. Protein engineering methods applied to membrane protein targets. Protein engineering, design & selection, 2013, 26(2): 91-100.
  3. Lutz S. Beyond directed evolution—semi-rational protein engineering and design. Current opinion in biotechnology, 2010, 21(6): 734-743.