Analytical chemistry 2011-08-15

Log-scale dose response of inhibitors on a chip.

Jae Young Yun, Sachin Jambovane, Se-Kwon Kim, Sung-Hak Cho, Evert C Duin, Jong Wook Hong

Index: Anal. Chem. 83(16) , 6148-53, (2011)

Full Text: HTML

Abstract

We demonstrate the accommodation of log-scale concentration gradients of inhibitors on a single microfluidic chip with a semidirect dilution capability of reagents for the determination of the half-inhibitory concentration or IC(50). The chip provides a unique tool for hosting a wide-range of concentration gradient for studies that require an equal distribution of measuring points on a logarithmic scale. Using Matrix metalloproteinase IX and three of its inhibitors, marimastat, batimastat, and CP471474, we evaluated the IC(50) of each inhibitor with a single experiment. The present work could be applied to the systematic study of biochemical binding and inhibition processes particularly in the field of mechanistic enzymology and the pharmaceutical industry.


Related Compounds

Related Articles:

The sorting protein PACS-2 promotes ErbB signalling by regulating recycling of the metalloproteinase ADAM17.

2015-01-01

[Nat. Commun. 6 , 7518, (2015)]

Inside-out Regulation of Ectodomain Cleavage of Cluster-of-Differentiation-44 (CD44) and of Neuregulin-1 Requires Substrate Dimerization.

2015-07-10

[J. Biol. Chem. 290 , 17041-54, (2015)]

Prevention of abdominal aortic aneurysm progression by targeted inhibition of matrix metalloproteinase activity with batimastat-loaded nanoparticles.

2015-11-06

[Circ. Res. 117 , e80-9, (2015)]

Activation of the P2X7 receptor induces the rapid shedding of CD23 from human and murine B cells.

2015-01-01

[Immunol. Cell Biol. 93(1) , 77-85, (2015)]

Simulated physiological stretch-induced proliferation of human bladder smooth muscle cells is regulated by MMPs.

2014-12-15

[Arch. Biochem. Biophys. 564 , 197-202, (2014)]

More Articles...