Design and synthesis of fluorescent and biotin tagged probes for the study of molecular actions of FAF1 inhibitor

Sung-eun Yoo; Changsun Yu; SeoHee Jung; Eunhee Kim; Nam Sook Kang

doi:10.1016/j.bmcl.2016.01.045

Design and synthesis of fluorescent and biotin tagged probes for the study of molecular actions of FAF1 inhibitor

Bioorg Med Chem Lett. 2016 Feb 15;26(4):1169-72. doi: 10.1016/j.bmcl.2016.01.045. Epub 2016 Jan 18.

Authors

Sung-eun Yoo¹, Changsun Yu², SeoHee Jung¹, Eunhee Kim², Nam Sook Kang¹

Affiliations

¹ Graduate School of New Drug Discovery and Development, Chungnam National University, Daehakno 99, Yuseong-gu, Daejeon 305-764, Republic of Korea.
² Department of Bioscience and Biotechnology, Chungnam National University, Daehakno 99, Yuseong-gu, Daejeon 305-764, Republic of Korea.

PMID: 26810261
DOI: 10.1016/j.bmcl.2016.01.045

Abstract

To study the molecular action of ischemic Fas-mediated cell death inhibitor, we prepared fluorescent-tagged and biotin-tagged probes of the potent inhibitor, KR-33494, of ischemic cell death. We used the molecular modeling technique to find the proper position for attaching those probes with minimum interference in the binding process of probes with Fas-mediated cell death target, FAF1.

Keywords: Biotin tagged probe; FAF1; Fas-mediated cell death pathways; Fluorescence tagged probe; KR-33493.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Adaptor Proteins, Signal Transducing / antagonists & inhibitors*
Adaptor Proteins, Signal Transducing / metabolism
Apoptosis / drug effects
Apoptosis Regulatory Proteins
Binding Sites
Biotin / chemistry*
Cell Line, Tumor
Cell Survival / drug effects
Drug Design*
Fluorescent Dyes / chemistry*
Humans
Hydrogen Peroxide / toxicity
Molecular Docking Simulation
Protein Binding
Protein Structure, Tertiary

Substances

Adaptor Proteins, Signal Transducing
Apoptosis Regulatory Proteins
FAF1 protein, human
Fluorescent Dyes
Biotin
Hydrogen Peroxide