New Ligands and Inhibitors

• 5118 · PDF 通过计算机模拟发现靶向AR N端结构域的强效小分子抑制剂用于治疗去势抵抗性前列腺癌 In silico discovery of potent small molecule inhibitors targeting the AR N-terminal domain for treating castration-resistant prostate cancer Patrick Kunz, Thomas Alanine, Babette Schade, Ben Cossins, Sandro Bottaro, Daniele Peterle, Flavia Giamogante, Elia Gamba, Sasha Soldati, Nathalie Wyss, Lixin Yang, Michele Invernizzi, Michael Habeck, Rudy Rubini, Melissa Kachura, Dmitry Dmitry Ryzhenkov, Matteo Cerrina, Fabio Airoldi, Valentina Ceserani, Alice Santopolo, Heidi Derks, Stefano Ruschetta, Andrew Allen, David Lowe, Carlo Fisicaro, Ken Carson, Patrik Foerch, Kevin Sprott, Kamil Tamiola
• 5119 · PDF P015,一种高选择性PARP7&12双重抑制剂 P015, a highly selective PARP7&12 dual inhibitor Jinwen Huang, Hao Huang, Steve Shen
• 5120 · PDF 新型泛KRAS on/off抑制剂BH-501242的设计与发现,靶向KRAS switch II口袋 Design and discovery of BH-501242, a novel pan-KRAS on/off inhibitor targeting KRAS switch II pocket Eugene Rui, Nancy Ling, Wei Deng, Ping Jiang, Zhenping Wang, Yue Hu, Joshua Choi, Danan Li, Evan Rogers, Anindya Sarkar, Levan Darjania, Geoffrey Oxnard, Jean Cui
• 5121 · PDF 靶向外周alpha 2A肾上腺素受体作为一种整合癌症治疗与支持性护理的双重获益策略 Targeting peripheral alpha 2A -adrenoceptors as a dual-benefit approach for integrated cancer therapy and supportive care Zhiqiang Cheng, Yang Xu, Larry Zhu
• 5122 5122 调控m6A-RNA修饰作为癌症的新型疗法 Regulating m6A-RNA modification as new therapies for cancer Tariq Rana
• 5123 · PDF C018,一种强效选择性CDK4&9双重抑制剂 C018, a potent and selective CDK4&9 dual inhibitor Jinwen Huang, Zhongyuan Li, Steve Shen
• 5124 · PDF 一种新型PCNA相互作用小分子骨架的鉴定与结构表征 Identification and structural characterization of a novel PCNA-interacting small molecule scaffold Jennifer Jossart, Ning Ma, Pouya Haratipour, Caroline Li, Long Gu, Terrence O'Brien, Nagarajan Vaidehi, Linda H. Malkas, Robert Hickey, Jeff J. Perry
• 5125 · PDF 发现一种新型选择性脑渗透CDK4抑制剂用于靶向癌症治疗 Discovery of a novel, selective brain penetrant CDK4 inhibitor for targeted cancer therapy Boris Rogovoy, Dmitrii Shkil, Ruben Karapetian, Elena Bulanova, Alexei Rjakhovskiy, Sergey Shevyakov, Tudor Oprea, Amy Burd, Iain Dukes, Nikolay Savchuk
• 5127 · PDF 基于结构指导发现用于靶向癌症治疗的强效选择性DGKalpha抑制剂 Structure-guided discovery of potent and selective DGKalpha inhibitors for targeted cancer therapy Farag E. S. Mosa, Khaled Barakat
• 5128 · PDF 利用整合生成式化学与机制性PK模拟的AI驱动平台加速发现新型RORgammaT调节剂 Accelerated discovery of novel RORgammaT modulators using an AI-driven platform integrating generative chemistry and mechanistic PK simulation Jeremy Jones, Rafal Bachorz, Michael Lawless, Joanna Pastwinska, Anna Salkowska, Marcin Ratajewski
• 5129 · PDF 用于治疗乳腺癌的新型PI3K-CDK4/6双重抑制剂PC-13的发现与开发 Discovery and development of a novel PI3K-CDK4/6 dual inhibitor PC-13 for the treatment of breast cancer Xinyun Zhang, Jiaqi Hu, Xiaoxue Li, Qian Wang, Yanan Zhao, Qiang Xia, Jinhua Wang, Heng Xu, Tj (Tiejun) Bing
• 5130 5130 具有降解PI3Kalpha H1047R蛋白能力的泛突变选择性PI3Kalpha抑制剂的鉴定与表征 Identification and characterization of pan-mutant selective PI3Kalpha inhibitors with the capability of PI3Kalpha H1047R protein degradation Chengshan Niu*, #, Shengli Dong*, #, Shaoqing Chen*, Kaige Ji, Zhengfei Guo, Maolin Zheng, Mingtao Chen, Yuanjie Li, Meihua Li, Hongqiang Li, Yu Yu, Xinlong Yang, Zhiyong He, Apeng Liang, Zhou Yin, Wei Wu, Jun Li*, Yusheng Wu
• 5131 · PDF HDM2021——一种强效选择性CBL-B抑制剂，在抗肿瘤治疗中表现出强劲的免疫调节疗效 HDM2021, a potent and selective CBL-B inhibitor exhibits robust immunomodulatory efficacy for anti-tumor therapy Shulun Chen, Mengting Zhao, Zhimin Zhang, Jingwen E, Xi Yang, Xinyu Dai, Zhenna Xia, Xin Xu, Dongzhou Liu
• 5132 · PDF 一种强效、口服生物利用度高、高选择性的小分子非共价KRAS[G12D]抑制剂的发现与临床前评估 Discovery and preclinical evaluation of a potent, orally bioavailable, highly selective, small molecule non-covalent KRAS[G12D] inhibitor Alexei Pushechnikov, Volodymyr Kysil, Ruben Karapetian, Stepan Mochalov, Aleksei Riakhovskii, Elena Bulanova, Nikolay Savchuk, Iain Dukes
• 5133 · PDF 用于癌症治疗的ACC1选择性抑制剂的设计、合成与药理学评价 Design, synthesis and pharmacological evaluation of ACC1 selective inhibitors for cancer treatment Ryo Mizojiri, Moriteru Asano, Daisuke Tomita, Hiroshi Banno, Noriyuki Nii, Masako Sasaki, Hiroyuki Sumi, Yoshihiko Satoh, Yukiko Yamamoto, Takeo Moriya, Yoshinori Satomi, Hironobu Maezaki
• 5135 · PDF 在EGFR突变型肺癌中靶向EGFR半胱氨酸775 Targeting EGFR cysteine 775 in EGFR mutant lung cancer Jie Jiang, Zhengnian Li, Yaning Wang, Stephen J. Collins, Felix H. Gottlieb, Prafulla C. Gokhale, Michael J. Eck, Pasi A. Jänne, Jianwei Che, Nathanael S. Gray, Tinghu Zhang
• 5136 · PDF 多靶点MNK抑制剂作为AML的抗癌药物 Multi-targeted MNK inhibitors as anticancer agents for AML Sophie Derusha, Erika Lisabeth, Sonali Kurup
• 5137 · PDF KBD880是一种用于治疗HCC的强效且选择性的GPC3多肽结合剂 KBD880 is a potent and selective GPC3 peptide binder for treatment of HCC Hongzhu Chu, Yang Chen, Yonggang Wei, Fei Ye, Jing Zhang, Zhiyong Li, Xiaoke Liu, Jiannan Cui
• 5138 · PDF 一种口服生物利用度良好的大环肽KRAS抑制剂的化学优化,该抑制剂通过识别单个氨基酸差异实现KRAS选择性 Chemical optimization of an orally bioavailable macrocyclic peptide KRAS inhibitors that achieve KRAS selectivity by recognizing a single amino acid difference Mirai Kage, Hatsuo Kawada, Koji Takano, Atsushi Matsuo, Yoshihisa Murata, Satoshi Hashimoto, Minoru Tamiya, Tomoya Kotake, Shino Kuramoto, Takashi Yamano, Machiko Irie, Kazuhiro Ohara, Yuuji Sakurai, Kenichi Nomura, Yuya Morita, Ryuji Hayashi, Yuma Wakamiya, Kana Takei, Hiroshi Tanaka, Yoshikazu Nishimura, Hitoshi Iikura, Takuya Shiraishi, Mikimasa Tanada
• 5140 · PDF 开发亲水性且代谢稳定的杂环AOH1996类似物用于儿科AML口服液体制剂 Development of hydrophilic and metabolically stable heterocyclic AOH1996 analogues for pediatric AML oral liquid formulations Pouya Haratipour, Melissa Valerio, Michaela R. Jacobs, Maryam Zangi, Long Gu, Caroline Li, Robert Lingeman, Jennifer Jossart, Jefferson J. Perry, Le Xuan Truong Nguyen, Linda H. Malkas, Robert J. Hickey
• 5141 · PDF ZMS-4084,一种强效且选择性的WRN抑制剂,在MSI-H肿瘤模型中诱导显著的肿瘤消退和持续的完全缓解 ZMS-4084, a potent and selective WRN inhibitor induces significant tumor regression and sustained complete responses in MSI-H tumor models Weikun Wang, Guimei Yang, Liting Xue, Yao Guo, Wenjing Li, Renhong Tang, Zhengtao Li
• 5142 · PDF PRMT5抑制剂SCR-6920下调HIF-1alpha并与贝伐珠单抗表现出协同抗肿瘤活性 PRMT5 inhibitor SCR-6920 downregulates HIF-1alpha and exhibits synergistic antitumor activity with Bevacizumab Guimei Yang, Huixia Dou, Liting Xue, Yao Guo, Wenjing Li, Zhen Li, Zhengtao Li, Renheng Tang
• 5145 · PDF 一种新型高效的多重RAS抑制剂ZMS-2195在临床前模型中有效阻断MAPK通路激活并诱导强劲的抗肿瘤生长效应 A novel highly potent multiple-RAS inhibitor ZMS-2195 efficiently blocks MAPK pathway activation and induces robust anti-tumor growth effects in preclinical models Zhengtao Li, Guimei Yang, Huixia Dou, Wei Zhu, Xiang Chen, Yao Guo, Wenjing Li, Liting Xue, Renhong Tang
• 5146 · PDF 发现一种新型ALK抑制剂ZM-8195,靶向ALK复合突变并具有优越的TRK选择性 Discovery of a novel ALK inhibitor ZM-8195 that targets ALK compound mutations with superior TRK selectivity Zhen Li, Yajing Liu, Mengying Li, Jing Dai, Xuefeng Wang, Yuan Cheng, Xue An, Jing Chen, Jianan Wang, Yuandong Zheng, Wenjing Li, Liting Xue, Zhengtao Li, Renghong Tang
• 5147 · PDF 一项针对cyclin A/B抑制剂ZMS-7506的新型研究显示其在体外和体内均具有强大的抗肿瘤疗效 A novel investigation of the cyclin A/B inhibitor ZMS-7506 demonstrates robust anti-tumor efficacy both in vitro and in vivo Guimei Yang, Ruina Wang, Weikun Wang, Liting Xue, Xiaokang Qin, Renhong Tang, Zhengtao Li

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