Faculty Sponsor(s)
Andrew Baggett
Location
Jereld R. Nicholson Library: Grand Avenue
Subject Area
Chemistry
Description
The Actin-Related Protein (Arp) 2/3 Complex is an actin nucleating factor intrinsically involved in cellular regulation of actin networks during life-essential processes such as motility. Overexpression of the Arp2/3 complex has indicated as a factor allowing the proliferation of certain metastatic cancers. This work describes the synthesis and in vitro biochemical testing of several molecules predicted by computational docking to be inhibitors of Arp2/3 Complex, and therefore of potential interest in clinical applications. The molecules are designed based off of the structure of known Arp2/3 inhibitor CK-666, which was discovered via high-throughput screening. Details of the synthesis of the tryptamine derivatives are discussed, and the bulk actin polymerization assay used to determine potency of the new compounds is discussed.
Recommended Citation
Sripeng, Atchara; Wade, Natalie; Nolen, Brad J.; and Baggett, Andrew W., "Synthesis of Small Molecule Derivatives of CK-666 as Potential Inhibitors of the Arp2/3 Complex" (2019). Linfield University Student Symposium: A Celebration of Scholarship and Creative Achievement. Event. Submission 45.
https://digitalcommons.linfield.edu/symposium/2019/all/45
Synthesis of Small Molecule Derivatives of CK-666 as Potential Inhibitors of the Arp2/3 Complex
Jereld R. Nicholson Library: Grand Avenue
The Actin-Related Protein (Arp) 2/3 Complex is an actin nucleating factor intrinsically involved in cellular regulation of actin networks during life-essential processes such as motility. Overexpression of the Arp2/3 complex has indicated as a factor allowing the proliferation of certain metastatic cancers. This work describes the synthesis and in vitro biochemical testing of several molecules predicted by computational docking to be inhibitors of Arp2/3 Complex, and therefore of potential interest in clinical applications. The molecules are designed based off of the structure of known Arp2/3 inhibitor CK-666, which was discovered via high-throughput screening. Details of the synthesis of the tryptamine derivatives are discussed, and the bulk actin polymerization assay used to determine potency of the new compounds is discussed.
