PMID: 11921439Mar 29, 2002Paper

Functional proteomics using chromophore-assisted laser inactivation

Proteomics
Susanne RubenwolfLeodevico L Ilag

Abstract

Proteins are the molecules that fulfil most cellular functions and represent over 90% of drug targets in the market. Chromophore-assisted laser inactivation (CALI) provides a timely and locally restricted protein inactivation and has proven to specifically destroy protein function using dye-coupled ligands and laser irradiation. CALI involves the generation of short-lived radicals thus limiting the radius of covalent modifications to spatially restricted sites on the target molecule. A transient functional inactivation occurs if the radicals modify amino acids of the target protein that are responsible for function. Here we show specific inactivation of several protein targets, that are members of relevant signal transduction pathways. For each of these targets, simple and high throughput screening-scaleable assays have been developed, making it possible to quantify the observed inactivation. Activities of target proteins have been addressed in cell-free as well as cell-based assays employing human primary and tumor-derived cell lines. In all cases, at least 50% inactivation was achieved. The data presented here demonstrate that CALI is a highly versatile tool for validating disease relevant targets at the protein level. This a...Continue Reading

Citations

Jan 28, 2003·Drug Discovery Today·Leodevico L IlagStefan W Henning
Mar 14, 2003·Nature·Sam Hanash
Dec 22, 2005·Nature Biotechnology·Maria E BulinaKonstantin A Lukyanov
Dec 1, 2003·Acta Neuropsychiatrica·Amy F EisenerMichele T Pato
Jul 23, 2003·Journal of Cellular Biochemistry·Qing-Yu He, Jen-Fu Chiu
Sep 1, 2007·Proteomics. Clinical Applications·José Bermúdez-Crespo, José Luis López
Oct 1, 2004·Drug Discovery Today. Technologies·Leodevico L Ilag
Oct 1, 2004·Drug Discovery Today. Technologies·K K Jain
Aug 22, 2012·Human Vaccines & Immunotherapeutics·Justyna BazanAndrzej Gamian
Jul 29, 2010·Physiological Reviews·Dmitriy M ChudakovKonstantin A Lukyanov

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