ACS central science · 2018

Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.

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Kearney Sara E, Zahoránszky-Kőhalmi Gergely, Brimacombe Kyle R, Henderson Mark J, Lynch Caitlin, Zhao Tongan, Wan Kanny K, Itkin Zina, Dillon Christopher, Shen Min, Cheff Dorian M, Lee Tobie D, Bougie Danielle, Cheng Ken, Coussens Nathan P, Dorjsuren Dorjbal, Eastman Richard T, Huang Ruili, Iannotti Michael J, Karavadhi Surendra, Klumpp-Thomas Carleen, Roth Jacob S, Sakamuru Srilatha, Sun Wei, Titus Steven A, Yasgar Adam, Zhang Ya-Qin, Zhao Jinghua, Andrade Rodrigo B, Brown M Kevin, Burns Noah Z, Cha Jin K, Mevers Emily E, Clardy Jon, Clement Jason A, Crooks Peter A, Cuny Gregory D, Ganor Jake, Moreno Jesus, Morrill Lucas A, Picazo Elias, Susick Robert B, Garg Neil K, Goess Brian C, Grossman Robert B, Hughes Chambers C, Johnston Jeffrey N, Joullie Madeleine M, Kinghorn A Douglas, Kingston David G I, Krische Michael J, Kwon Ohyun, Maimone Thomas J, Majumdar Susruta, Maloney Katherine N, Mohamed Enas, Murphy Brian T, Nagorny Pavel, Olson David E, Overman Larry E, Brown Lauren E, Snyder John K, Porco John A, Rivas Fatima, Ross Samir A, Sarpong Richmond, Sharma Indrajeet, Shaw Jared T, Xu Zhengren, Shen Ben, Shi Wei, Stephenson Corey R J, Verano Alyssa L, Tan Derek S, Tang Yi, Taylor Richard E, Thomson Regan J, Vosburg David A, Wu Jimmy, Wuest William M, Zakarian Armen, Zhang Yufeng, Ren Tianjing, Zuo Zhong, Inglese James, Michael Sam, Simeonov Anton, Zheng Wei, Shinn Paul, Jadhav Ajit, Boxer Matthew B, Hall Matthew D, Xia Menghang, Guha Rajarshi, Rohde Jason M

Аннотация

Natural products and their derivatives continue to be wellsprings of nascent therapeutic potential. However, many laboratories have limited resources for biological evaluation, leaving their previously isolated or synthesized compounds largely or completely untested. To address this issue, the Canvass library of natural products was assembled, in collaboration with academic and industry researchers, for quantitative high-throughput screening (qHTS) across a diverse set of cell-based and biochemical assays. Characterization of the library in terms of physicochemical properties, structural diversity, and similarity to compounds in publicly available libraries indicates that the Canvass library contains many structural elements in common with approved drugs. The assay data generated were analyzed using a variety of quality control metrics, and the resultant assay profiles were explored using statistical methods, such as clustering and compound promiscuity analyses. Individual compounds were then sorted by structural class and activity profiles. Differential behavior based on these classifications, as well as noteworthy activities, are outlined herein. One such highlight is the activity of (-)-2(S)-cathafoline, which was found to stabilize calcium levels in the endoplasmic reticulum. The workflow described here illustrates a pilot effort to broadly survey the biological potential of natural products by utilizing the power of automation and high-throughput screening.

Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.

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Аннотация