一二三四区视频,亚洲少妇熟女色,日本久热无码视频网,欧美国产日韩大尺度,亚洲a视频,久久少妇一区二区,日韩999无码视频,刺激久久久久久久,啊啊啊啊不要啊在线

ChemicalBook >> journal list >> SLAS Discovery >>article
SLAS Discovery

SLAS Discovery

IF: 2.7
Download PDF

Medium-Throughput Detection of Hsp90/Cdc37 Protein-Protein Interaction Inhibitors Using a Split Renilla Luciferase-Based Assay

Published:1 February 2020 DOI: 10.1177/2472555219884033
Farid Ahmad Siddiqui , Hanna Parkkola , Ganesh babu Manoharan , Daniel Abankwa

Abstract

The protein-folding chaperone Hsp90 enables the maturation and stability of various oncogenic signaling proteins and is thus pursued as a cancer drug target. Folding in particular of protein kinases is assisted by the co-chaperone Cdc37. Several inhibitors against the Hsp90 ATP-binding site have been developed. However, they displayed significant toxicity in clinical trials. By contrast, the natural product conglobatin A has an exceptionally low toxicity in mice. It targets the protein–protein interface (PPI) of Hsp90 and Cdc37, suggesting that interface inhibitors have an interesting drug development potential.

In order to identify inhibitors of the Hsp90/Cdc37 PPI, we have established a mammalian cell lysate-based, medium-throughput amenable split Renilla luciferase assay. This assay employs N-terminal and C-terminal fragments of Renilla luciferase fused to full-length human Hsp90 and Cdc37, respectively. We expect that our assay will allow for the identification of novel Hsp90/Cdc37 interaction inhibitors. Such tool compounds will help to evaluate whether the toxicity profile of Hsp90/Cdc37 PPI inhibitors is in general more favorable than that of ATP-competitive Hsp90 inhibitors. Further development of such tool compounds may lead to new classes of Hsp90 inhibitors with applications in cancer and other diseases.

Substances (6)

Materials Related products
Procduct Name CAS Molecular Formula Supplier Price
Geldanamycin 30562-34-6 C29H40N2O9 374 suppliers $14.00-$3791.00
Geldanamycin 30562-34-6 C29H40N2O9 374 suppliers $14.00-$3791.00
Geldanamycin 30562-34-6 C29H40N2O9 374 suppliers $14.00-$3791.00
Geldanamycin 30562-34-6 C29H40N2O9 374 suppliers $14.00-$3791.00

Similar articles

IF:6.8

Structure-Based Discovery of M-89 as a Highly Potent Inhibitor of the Menin-Mixed Lineage Leukemia (Menin-MLL) Protein–Protein Interaction

Journal of Medicinal Chemistry Angelo Aguilar, Ke Zheng,etc Published: 22 June 2019
IF:2.5

Development of an Indirect ELISA Based on the VP1 Protein for Detection of Antibodies against Water Buffalo Hunnivirus

Biochemical and biophysical research communications Qianyuan Liu, Xiaoying Feng,etc Published: 23 November 2024
壤塘县| 柯坪县| 汶川县| 望谟县| 冕宁县| 广昌县| 黄龙县| 都昌县| 壶关县| 武胜县| 海伦市| 长岛县| 揭西县| 余庆县| 独山县| 兴宁市| 临泽县| 高雄市| 屯门区| 克拉玛依市| 锦州市| 乐东| 甘孜| 新龙县| 湘阴县| 天等县| 桦甸市| 彰化市| 阳山县| 和林格尔县| 伊金霍洛旗| 阿克陶县| 吐鲁番市| 峡江县| 体育| 松滋市| 新巴尔虎右旗| 长寿区| 天水市| 台前县| 阳山县|