日期:
2020 年 — 2026 年
2020
2021
2022
2023
2024
2025
2026
影响因子:

Editor's Note: Small-Molecule Inhibition of the Acyl-Lysine Reader ENL as a Strategy against Acute Myeloid Leukemia

编者按:小分子抑制酰基赖氨酸阅读器ENL作为对抗急性髓系白血病的策略

Liu, Yiman; Li, Qinglan; Alikarami, Fatemeh; Barrett, Declan R; Mahdavi, Leila; Li, Hangpeng; Tang, Sylvia; Khan, Tanweer A; Michino, Mayako; Hill, Connor; Song, Lele; Yang, Lu; Li, Yuanyuan; Pokharel, Sheela Pangeni; Stamford, Andrew W; Liverton, Nigel; Renzetti, Louis M; Taylor, Simon; Watt, Gillian F; Ladduwahetty, Tammy; Kargman, Stacia; Meinke, Peter T; Foley, Michael A; Shi, Junwei; Li, Haitao; Carroll, Martin; Chen, Chun-Wei; Gardini, Alessandro; Maillard, Ivan; Huggins, David J; Bernt, Kathrin M; Wan, Liling

A Chemical Strategy toward Novel Brain-Penetrant EZH2 Inhibitors

一种开发新型脑穿透性EZH2抑制剂的化学策略

Liang, Rui; Tomita, Daisuke; Sasaki, Yusuke; Ginn, John; Michino, Mayako; Huggins, David J; Baxt, Leigh; Kargman, Stacia; Shahid, Maaz; Aso, Kazuyoshi; Duggan, Mark; Stamford, Andrew W; DeStanchina, Elisa; Liverton, Nigel; Meinke, Peter T; Foley, Michael A; Phillips, Richard E

Discovery of TDI-10229: A Potent and Orally Bioavailable Inhibitor of Soluble Adenylyl Cyclase (sAC, ADCY10)

TDI-10229 的发现:一种强效且口服生物利用度高的可溶性腺苷酸环化酶 (sAC, ADCY10) 抑制剂

Fushimi, Makoto; Buck, Hannes; Balbach, Melanie; Gorovyy, Anna; Ferreira, Jacob; Rossetti, Thomas; Kaur, Navpreet; Levin, Lonny R; Buck, Jochen; Quast, Jonathan; van den Heuvel, Joop; Steegborn, Clemens; Finkin-Groner, Efrat; Kargman, Stacia; Michino, Mayako; Foley, Michael A; Miller, Michael; Liverton, Nigel J; Huggins, David J; Meinke, Peter T

Novel Pure αVβ3 Integrin Antagonists That Do Not Induce Receptor Extension, Prime the Receptor, or Enhance Angiogenesis at Low Concentrations.

新型纯αVβ3整合素拮抗剂,低浓度下不诱导受体延伸、启动受体或增强血管生成

Li Jihong, Fukase Yoshiyuki, Shang Yi, Zou Wei, Muñoz-Félix José M, Buitrago Lorena, van Agthoven Johannes, Zhang Yixiao, Hara Ryoma, Tanaka Yuta, Okamoto Rei, Yasui Takeshi, Nakahata Takashi, Imaeda Toshihiro, Aso Kazuyoshi, Zhou Yuchen, Locuson Charles, Nesic Dragana, Duggan Mark, Takagi Junichi, Vaughan Roger D, Walz Thomas, Hodivala-Dilke Kairbaan, Teitelbaum Steven L, Arnaout M Amin, Filizola Marta, Foley Michael A, Coller Barry S

Antimalarial proteasome inhibitor reveals collateral sensitivity from intersubunit interactions and fitness cost of resistance

抗疟蛋白酶体抑制剂揭示了亚基间相互作用引起的协同敏感性以及耐药性的适应性代价。

Kirkman, Laura A; Zhan, Wenhu; Visone, Joseph; Dziedziech, Alexis; Singh, Pradeep K; Fan, Hao; Tong, Xinran; Bruzual, Igor; Hara, Ryoma; Kawasaki, Masanori; Imaeda, Toshihiro; Okamoto, Rei; Sato, Kenjiro; Michino, Mayako; Alvaro, Elena Fernandez; Guiang, Liselle F; Sanz, Laura; Mota, Daniel J; Govindasamy, Kavitha; Wang, Rong; Ling, Yan; Tumwebaze, Patrick K; Sukenick, George; Shi, Lei; Vendome, Jeremie; Bhanot, Purnima; Rosenthal, Philip J; Aso, Kazuyoshi; Foley, Michael A; Cooper, Roland A; Kafsack, Bjorn; Doggett, J Stone; Nathan, Carl F; Lin, Gang

Aminopyrimidine Class Aggregation Inhibitor Effectively Blocks Aβ-Fibrinogen Interaction and Aβ-Induced Contact System Activation

氨基嘧啶类聚集抑制剂有效阻断Aβ-纤维蛋白原相互作用和Aβ诱导的接触系统激活

Singh, Pradeep K; Kawasaki, Masanori; Berk-Rauch, Hanna E; Nishida, Goushi; Yamasaki, Takeshi; Foley, Michael A; Norris, Erin H; Strickland, Sidney; Aso, Kazuyoshi; Ahn, Hyung Jin

Mps1 Regulates Kinetochore-Microtubule Attachment Stability via the Ska Complex to Ensure Error-Free Chromosome Segregation

Mps1 通过 Ska 复合物调节动粒-微管附着稳定性,以确保无错染色体分离

John Maciejowski, Hauke Drechsler, Kathrin Grundner-Culemann, Edward R Ballister, Jose-Antonio Rodriguez-Rodriguez, Veronica Rodriguez-Bravo, Mathew J K Jones, Emily Foley, Michael A Lampson, Henrik Daub, Andrew D McAinsh, Prasad V Jallepalli

Diversity-oriented synthesis yields novel multistage antimalarial inhibitors.

多样性导向合成产生新型多阶段抗疟疾抑制剂

Kato Nobutaka, Comer Eamon, Sakata-Kato Tomoyo, Sharma Arvind, Sharma Manmohan, Maetani Micah, Bastien Jessica, Brancucci Nicolas M, Bittker Joshua A, Corey Victoria, Clarke David, Derbyshire Emily R, Dornan Gillian L, Duffy Sandra, Eckley Sean, Itoe Maurice A, Koolen Karin M J, Lewis Timothy A, Lui Ping S, Lukens Amanda K, Lund Emily, March Sandra, Meibalan Elamaran, Meier Bennett C, McPhail Jacob A, Mitasev Branko, Moss Eli L, Sayes Morgane, Van Gessel Yvonne, Wawer Mathias J, Yoshinaga Takashi, Zeeman Anne-Marie, Avery Vicky M, Bhatia Sangeeta N, Burke John E, Catteruccia Flaminia, Clardy Jon C, Clemons Paul A, Dechering Koen J, Duvall Jeremy R, Foley Michael A, Gusovsky Fabian, Kocken Clemens H M, Marti Matthias, Morningstar Marshall L, Munoz Benito, Neafsey Daniel E, Sharma Amit, Winzeler Elizabeth A, Wirth Dyann F, Scherer Christina A, Schreiber Stuart L

High-throughput identification of genotype-specific cancer vulnerabilities in mixtures of barcoded tumor cell lines.

利用条形码标记的肿瘤细胞系混合物进行高通量基因型特异性癌症脆弱性鉴定

Yu Channing, Mannan Aristotle M, Yvone Griselda Metta, Ross Kenneth N, Zhang Yan-Ling, Marton Melissa A, Taylor Bradley R, Crenshaw Andrew, Gould Joshua Z, Tamayo Pablo, Weir Barbara A, Tsherniak Aviad, Wong Bang, Garraway Levi A, Shamji Alykhan F, Palmer Michelle A, Foley Michael A, Winckler Wendy, Schreiber Stuart L, Kung Andrew L, Golub Todd R

Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes

利用小分子探针推进生物学理解和治疗药物发现

Schreiber, Stuart L; Kotz, Joanne D; Li, Min; Aubé, Jeffrey; Austin, Christopher P; Reed, John C; Rosen, Hugh; White, E Lucile; Sklar, Larry A; Lindsley, Craig W; Alexander, Benjamin R; Bittker, Joshua A; Clemons, Paul A; de Souza, Andrea; Foley, Michael A; Palmer, Michelle; Shamji, Alykhan F; Wawer, Mathias J; McManus, Owen; Wu, Meng; Zou, Beiyan; Yu, Haibo; Golden, Jennifer E; Schoenen, Frank J; Simeonov, Anton; Jadhav, Ajit; Jackson, Michael R; Pinkerton, Anthony B; Chung, Thomas D Y; Griffin, Patrick R; Cravatt, Benjamin F; Hodder, Peter S; Roush, William R; Roberts, Edward; Chung, Dong-Hoon; Jonsson, Colleen B; Noah, James W; Severson, William E; Ananthan, Subramaniam; Edwards, Bruce; Oprea, Tudor I; Conn, P Jeffrey; Hopkins, Corey R; Wood, Michael R; Stauffer, Shaun R; Emmitte, Kyle A