Post-translational Modification Specificity Testing

HuProt Can Play a Key Role in Drug Discovery

PTM specificity testing is crucial for validating binding to modified forms of proteins.

Post-translational modifications (PTMs) are chemical modifications that occur on proteins after they have been synthesized. PTMs regulate protein activity, localization, and interactions by altering protein structure, stability, and interactions with other molecules. For example, phosphorylation can regulate enzyme activity, while ubiquitination targets proteins for degradation. As PTMs play crucial roles in protein function, targeting PTMs has emerged as a promising strategy in drug discovery. PTM specificity testing is crucial for validating binding to modified forms of proteins.

In the featured publication below, multiplexed PTM reactions on HuProt™ microarrays were developed and applied to 102 TCGA ovarian tumor samples. Data integration and networks analysis led to the prediction that 19 tyrosine kinases were elevated and potentially responsible for the dysregulated pTyr signaling pathways in ovarian tumors. Elevated kinase activities of PTK2 and PTK2B were confirmed in several ovarian cancer cell lines.