Understanding structure activity relationship (SAR) becomes more and more valuable in drug discovery research. The United States and the European Union are currently promoting the use of SAR for screening large numbers of chemicals that have already entered commerce, as well as for development and registration of novel compounds. Creative Biolabs has developed a Peparray™ high throughput screening (HTS) peptide array platform. Based on this advanced platform, our scientists are able to perform rapid and effective SAR analysis between peptides and their corresponding partners. We are proud to offer this platform for SAR analysis service, tailored to your specific needs.
Since similar compounds may have similar physical and biological properties. The biological effects of a new chemical compound can often be predicted from its molecular structure using data about other similar compounds. The relationship between the structure of a molecule and its biological activity is referred to as SAR. The analysis of SAR enables the determination of the chemical group responsible for enducing a target biological effect in the organism. That is why SAR is so valuable in drug discovery research. This allows modification of a bioactive compound by changing its chemical structure, and the bioactive compound could be peptides. Medicinal chemists use the techniques of chemical synthesis to insert new chemical groups into the biomedical compound and test the modifications for their biological effects. However, these chemical methods are time consuming and low throughput. The SAR tools and models, which are used to evaluate the relationship between specific chemical compound structures and their biological activities, are continuously being established. A high throughput method to screen optimized compounds is required urgently.
Peptide arrays are widely used in specific detection of individual proteins in complex mixtures, identification of binding sites between proteins, determination the contribution of individual amino acid residues to the binding and high throughput measurements of enzymatic activities. Peptide arrays can also be used for high throughput SAR analysis. There are many studies of SAR analysis based on peptide array, including the shortened and modiﬁed peptides for effective HIV-1 Rev-integrase interaction, optimized Api137 for an increased antimicrobial activity against Pseudomonas aeruginosa, etc.
Fig.1 Antimicrobial activities of monosubstituted Api137 peptides determined in 12.5% MHB against P. aeruginosa DSM1117 (Bluhm et al. 2015).
Creative Biolabs has developed a cutting-edge Peparray™ HTS peptide array platform for all peptides related interaction projects. Based on this advanced platform, scientists of Creative Biolabs are proficient in SAR analysis. We’ll first design a peptide array with modified peptides, which could include an alanine scan, truncations and systematic replacements of each residue. Then, we can synthesize hundreds of monosubstituted analogs, screen them, and combine the best substitutions yielding double and triple substituted analogs. Next, HTS screening will be applied to investigate SAR and determine which residues are crucial for the activities.
Key advantages including but not limited to:
HTS peptide arrays are excellent tools to perform detailed SAR binding studies. They are applied to discover and develop new optimized shorter peptides with better pharmacological properties. Creative Biolabs is happy to share extensive expertise in HTS peptide array to facilitate our customers’ research and project development. We can offer high-quality customized services in SAR analysis to meet every customer’s specific requirements.
For more detailed information, please feel free to contact us or directly send us an inquiry.