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

Discovery of Palazestrant (OP-1250), a Potent and Orally Bioavailable Complete Estrogen Receptor Antagonist (CERAN) and Selective Estrogen Receptor Degrader (SERD).

发现帕拉塞斯特兰(OP-1250),一种强效且口服生物利用度高的完全雌激素受体拮抗剂(CERAN)和选择性雌激素受体降解剂(SERD)

Ng Raymond A, Barratt Susanna, Parisian Alison, Palanisamy Gopinath S, Phukan Samiron, Sun Richard, Robello Brandon, Peña Guadalupe, Sapugay Judevin, Yeghikyan David, Wang Chenbo, Satish Kher Samir, Thangathirupathy Srinivasan, Millikin Robert, Yu Guijun, Watanabe Teruki, Zhou Fei, Rich Brian, Duncan Alexis, Andersen Samuel E, Chawla Reena, Zak David R, Heerding Dirk A, Hearn Brian R, Greene Geoffrey, Harmon Cyrus L, Hodges-Gallagher Leslie, Kushner Peter J, Fanning Sean W, Myles David C

Structural characterization of dicyanopyridine containing DNMT1-selective, non-nucleoside inhibitors

含二氰基吡啶的DNMT1选择性非核苷类抑制剂的结构表征

Horton, John R; Pathuri, Sarath; Wong, Kristen; Ren, Ren; Rueda, Lourdes; Fosbenner, David T; Heerding, Dirk A; McCabe, Michael T; Pappalardi, Melissa B; Zhang, Xing; King, Bryan W; Cheng, Xiaodong

Generation and Validation of Intracellular Ubiquitin Variant Inhibitors for USP7 and USP10

胞内 USP7 和 USP10 泛素变体抑制剂的生成和验证

Wei Zhang, Maria A Sartori, Taras Makhnevych, Kelly E Federowicz, Xiaohui Dong, Li Liu, Satra Nim, Aiping Dong, Jingsong Yang, Yanjun Li, Dania Haddad, Andreas Ernst, Dirk Heerding, Yufeng Tong, Jason Moffat, Sachdev S Sidhu

Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor

发现新型 AKT 抑制剂与 MEK 抑制剂联合使用可增强抗肿瘤作用

Melissa Dumble, Ming-Chih Crouthamel, Shu-Yun Zhang, Michael Schaber, Dana Levy, Kimberly Robell, Qi Liu, David J Figueroa, Elisabeth A Minthorn, Mark A Seefeld, Meagan B Rouse, Sridhar K Rabindran, Dirk A Heerding, Rakesh Kumar

Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development

GSK2656157 的发现:一种经过优化的 PERK 抑制剂,已选定用于临床前开发

Axten, Jeffrey M; Romeril, Stuart P; Shu, Arthur; Ralph, Jeffrey; Medina, Jesús R; Feng, Yanhong; Li, William Hoi Hong; Grant, Seth W; Heerding, Dirk A; Minthorn, Elisabeth; Mencken, Thomas; Gaul, Nathan; Goetz, Aaron; Stanley, Thomas; Hassell, Annie M; Gampe, Robert T; Atkins, Charity; Kumar, Rakesh

Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK)

发现 7-甲基-5-(1-{[3-(三氟甲基)苯基]乙酰基}-2,3-二氢-1H-吲哚-5-基)-7H-吡咯并[2,3-d]嘧啶-4-胺 (GSK2606414),一种强效且选择性的蛋白激酶 R (PKR) 样内质网激酶 (PERK) 抑制剂

Jeffrey M Axten, Jesús R Medina, Yanhong Feng, Arthur Shu, Stuart P Romeril, Seth W Grant, William Hoi Hong Li, Dirk A Heerding, Elisabeth Minthorn, Thomas Mencken, Charity Atkins, Qi Liu, Sridhar Rabindran, Rakesh Kumar, Xuan Hong, Aaron Goetz, Thomas Stanley, J David Taylor, Scott D Sigethy, Ginge

Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery

氨基吲唑类PDK1抑制剂:基于片段的药物发现案例研究

Medina, Jesús R; Blackledge, Charles W; Heerding, Dirk A; Campobasso, Nino; Ward, Paris; Briand, Jacques; Wright, Lois; Axten, Jeffrey M

Characterization of an Akt kinase inhibitor with potent pharmacodynamic and antitumor activity

具有强效药效学和抗肿瘤活性的 Akt 激酶抑制剂的表征

Nelson Rhodes, Dirk A Heerding, Derek R Duckett, Derek J Eberwein, Victoria B Knick, Timothy J Lansing, Randy T McConnell, Tona M Gilmer, Shu-Yun Zhang, Kimberly Robell, Jason A Kahana, Robert S Geske, Elena V Kleymenova, Anthony E Choudhry, Zhihong Lai, Jack D Leber, Elisabeth A Minthorn, Susan L S

Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase

4-(2-(4-氨基-1,2,5-恶二唑-3-基)-1-乙基-7-{[(3S)-3-哌啶基甲基]氧基}-1H-咪唑并[4,5-c]吡啶-4-基)-2-甲基-3-丁炔-2-醇 (GSK690693) 的鉴定,AKT 激酶的新型抑制剂

Dirk A Heerding, Nelson Rhodes, Jack D Leber, Tammy J Clark, Richard M Keenan, Louis V Lafrance, Mei Li, Igor G Safonov, Dennis T Takata, Joseph W Venslavsky, Dennis S Yamashita, Anthony E Choudhry, Robert A Copeland, Zhihong Lai, Michael D Schaber, Peter J Tummino, Susan L Strum, Edgar R Wood, Dere

Contribution of plasminogen activators and their inhibitors to the survival prognosis of patients with Dukes' stage B and C colorectal cancer

纤溶酶原激活剂及其抑制剂对 Dukes B 期和 C 期结直肠癌患者生存预后的影响

Ganesh, S; Sier, C F; Heerding, M M; van Krieken, J H; Griffioen, G; Welvaart, K; van de Velde, C J; Verheijen, J H; Lamers, C B; Verspaget, H W