Challenge
Our client requested characterization of the oncology clinical candidate MRTX1719’s interaction with two forms of Protein Arginine Methyl Transferase 5 (PRMT5), bound to either SAM (PRMT5•SAM) or MTA (PRMT5•MTA).
SPR (Surface Plasmon Resonance) direct measurement was not feasible due to the slow dissociation rate (koff) of MRTX1719 from both PRMT5 complexes. The dissociation rate was too slow, causing minimal dissociation during single-cycle kinetics, which prevented accurate koff determination.
Achievements
To overcome this problem an adapted SPR chaser assay was implemented. This strategy indirectly measured the dissociation rate constant (koff) and allowed for the determination of the affinity of MRTX1719 for both complexes.
Tackling the Hard-to-Drug Frontier: The Power of Complementary Screening Modalities
Developing small-molecule drugs for hard-to-drug targets remains one of the toughest challenges in modern drug discovery. Targets like cytokines, transcription factors, and scaffolding proteins often lack well-defined…
Meet the ZoBio SPR Team: Advancing Drug Discovery Around the Clock
Drug discovery doesn’t sleep, and neither does our SPR (Surface Plasmon Resonance) team. While the Assay Group takes a well-deserved weekend break and goes for dinner tonight, our relentless SPR team is tirelessly screening compounds, revealing critical insights that help drive discovery forward.
Meet the Team:
Each of our SPR machines brings unique strengths to the lab, earning their names and personalities for how they support our research. These workhorses are the true heroes of our lab, capturing precise data…
32nd Protein Structure Determination in Industry meeting
In person Starting from Sunday, November 10th, the ZoBio team participated in the 32nd Protein Structure Determination in Industry meeting, which was held at the Novotel Paris Centre Tour Eiffel in Paris, France. This year’s meeting was organized jointly by SERVIER and Synchrotron SOLEIL, with support from Hg3 Conferences. The scientific talks focused on the…