PO.ET09.07 · 实验与分子治疗
Novel Antitumor Agents 2
- 4558 4558 首次公开一种高效、高选择性的口服 KRAS G12V 抑制剂 PSTA-6208 First disclosure of a highly potent and selective oral KRAS G12V inhibitor PSTA-6208 Wenxi Li, Lihong Hu, zhenzhen Zhu, Yingchun Liu, Tao Yu, Qianwei Jiang, Chi-Chung Chan, Jian Li, Shuhui Chen
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4559 · PDF PLM-103:一种双机制 YES1/YAP 通路抑制剂,展现广谱抗肿瘤疗效及免疫肿瘤学协同作用 PLM-103: A dual-mechanism YES1/YAP pathway inhibitor exhibiting broad antitumor efficacy and immuno-oncology synergy Soo Jin Kim, Kyoung Mee Kim, Jaehyeon Kim, Soo Yeon Jang, Yong-Chul Kim
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4560 · PDF CTPS1 作为乳腺癌和卵巢癌的代谢脆弱性及新型治疗靶点 CTPS1 as a metabolic vulnerability and novel therapeutic target in breast and ovarian cancer Xiyin Wang, Michael Emch, Lauren Voll, Rebecca Epp, Esther Rodman, Noa Odell, Hannah Smith, Nicole Pearson, Xiaonan Hou, Matthew Goetz, Scott Kaufmann, S. John Weroha, Phillip Beer, John Hawse
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4561 · PDF 使用 ISM3830 抑制 Cbl-b 可恢复固有免疫和适应性免疫,并在体外和体内对实体瘤展现抗肿瘤活性 Cbl-b inhibition with ISM3830 restores innate and adaptive immunity and demonstrates antitumor activity against solid tumors in vitro and in vivo Zhongying Cao, Fanye Meng, Jinxin Liu, Zhilin Ning, Jiaojiao Yu, David Gennert, Suguna Rachakonda, Man Zhang, Xin Cai, Xiao Ding, Alex Zhavoronkov
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4562 · PDF ISM6210,一种用于治疗 HR+/HER2- 乳腺癌的强效、选择性 CDK4 抑制剂 ISM6210, a potent and selective CDK4 inhibitor for the treatment of HR+/HER2- breast cancer Yilin Yang, Zhongying Cao, Zhisen Zhang, Fanye Meng, Jinxin Liu, Jiamin Zheng, Zuoxiao Shi, Ling Wang, David Gennert, Suguna Rachakonda, Xiao Ding, Xin Cai, Man Zhang, Feng Ren, Alex Zhavoronkov
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4563 · PDF 小分子抑制失调的 STAT3-促炎轴并在胰腺癌和乳腺癌中诱导抗肿瘤应答 Small molecules inhibited dysregulated STAT3-proinflammatory axis and induced antitumor responses in pancreatic and breast cancer Rasaq Akinsola, Monday Ogaba Ogese, Lihong Huo, Yue Chen, Francisco Lopez-Tapia, Richard T. Waldron, Aurelia Lugea, Stephen J. Pandol, James Turkson
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4564 · PDF PARP7 抑制驱动强效抗肿瘤活性的双重机制 Dual mechanisms of PARP7 inhibition driving potent antitumor activity Iksoo Jang, Dajeong Kim, Daehyeon Seong, Jeong Yoon Shin, Kyu Hwan Kim, SeungHyun Song, Joon Yonug Hwang, Hong Sik Han, Kyung Seok Lee, Jongho Cho, Ki Moon Ryu, Mi-Kyung Kim
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4565 · PDF GFH276 单药治疗及联合治疗用于 RAS 突变肿瘤的临床前评估 Preclinical evaluation of GFH276 monotherapy and combination therapy for RAS-mutant tumors Feng Yan, Jichen Zhao, Jingyang Zhang, Siyuan Le, Fusheng Zhou, Jiong Lan, Qiang Lu
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4566 · PDF CKD-9001的发现与表征:一种新型PARP1选择性抑制剂及DNA捕获剂,在HRD癌症中具有更强疗效和更优的毒性特征 Discovery and characterization of CKD-9001, a novel PARP1-selective inhibitor and DNA trapper with enhanced efficacy and an improved toxicity profile in HRD cancers Yuji Kim, Moosung Ko, Gun-Woo Park, Yoo-Kyung Song, Hye-Jin Hong, Keesoo Nam, Junho Cho, Younghue Han, Jaeyoung Lee, Dahae Lee, Jiyeon Back, Seong-Ho Hong, Ju Young Song, Jinsol Park, Hyunmo Yang, Nina Ha, Se-Mi Kim, In-Chang Hwang, Changsik Lee, Sung Jun Kang
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4567 · PDF 一种新型PARP7抑制剂通过免疫激活和肿瘤内在生长抑制表现出双重抗肿瘤活性 A novel PARP7 inhibitor exhibits dual antitumor activity through immune activation and tumor-intrinsic growth inhibition Dajeong Kim, Iksoo Jang, Daehyeon Seong, Jeongyoon Shin, Kyu Hwan Kim, SeungHyun Song, Joon Yonug Hwang, Hong Sik Han, Kyung Seok Lee, Boram Lee, Soo-Jung Choi, Song-Yi Lee, Dae Young Lee, Jinhoon Jeong, Hojeong Hong, Haneol Kim, Jongho Cho, Ki Moon Ryu, Mi-Kyung Kim
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4568 · PDF 抑制烟酰胺磷酸核糖转移酶(NAMPT)损害细胞活力、影响能量代谢、诱导DNA损伤,并在神经母细胞瘤临床前模型中驱动肿瘤消退 Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) impairs cellular viability, affects energy metabolism, induces DNA damage, and drives tumor regression in preclinical models of neuroblastoma Amy Yu, Sophia Varriano, Victor J. Collins, Ariana E. Nelson, Abantika Chakraborty, Unsun Lee, Amy James, Kristine Isanogle, Nimit Patel, Joong Kim, Ming Sun, Ye Yang, Ying Wu, Krithika Bhuvaneshwar, Bhushan L. Thakur, Arnulfo Mendoza, Sameer H. Issaq, Mirit I. Aladjem, John F. Shern, Parthav Jailwala, Joseph D. Kalen, Simone Difilippantonio, Craig J. Thomas, Daniel R. Crooks, Rosa Nguyen, Carol J. Thiele, Christine M. Heske
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4569 · PDF D3S-003:一种口服生物利用度良好的强效选择性双状态抑制剂,同时靶向GDP结合型和GTP结合型KRAS G12D D3S-003, an orally bioavailable potent and selective dual-state inhibitor targeting both GDP- and GTP-bound KRAS G12D Jing Zhang, Tienan Wang, Robert A. Mook Jr., Haibo Xie, Shaonan Wang, Zhiqiang Zheng, Xin Xiong, Hui Wang, Zhi Jian Chen
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4570 · PDF HEC228032:一种口服生物利用度良好的分子胶泛RAS(ON)抑制剂,具有高强度的抗肿瘤疗效 HEC228032, an orally bioavailable molecular glue pan-RAS (ON) inhibitor with highly potent anti-tumor efficacy Haiwang Liu, Lingling Chen, Yangyang Meng, Hong Huang, Ming Li, Ning Kang, Yahui Feng, Ziting Liu, Jing Li, Kai Lin, Yingjun Zhang
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4571 · PDF RGT-490的发现与表征:一种突变选择性PI3Kalpha抑制剂 Discovery and characterization of RGT-490, a mutant selective PI3Kalpha inhibitor Jing Han, Kailiang Wang, Feng Zhao, Xinjuan Wang, Xiaoming Ren, Xiuliang Huang, Xiumei Chen, Teng Feng, Xin Hua, Zhuanzhuan Zhang, Lili Yao, Jing Lin, Wenge Zhong, Julie Xie
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4572 · PDF SY-14556的发现:一种高效选择性的p53 Y220C突变体小分子再激活剂,具有差异化的临床前特征 Discovery of SY-14556, a highly potent and selective small molecule reactivator of p53 Y220C mutant with differentiated preclinical profile Hongjuan Li, Zhenbang Lou, Xiaopeng Li, Chang Lu, Shikang Cheng, Bo Li, Xianxing Shang, Xiaofeng Zhai, Yan Zhu, Hong Luo, Yinghui Sun
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4573 · PDF JMKX007129是一种靶向N端结构域的新一代雄激素受体抑制剂,用于治疗转移性去势抵抗性前列腺癌 JMKX007129 is a next generation of androgen receptor inhibitor targeting N-terminal domain for the treatment of metastatic castration-resistant prostate cancers Shengjian Huang, Gang Deng, Liyan Yue, Xiaodong Zhang, Aishen Gong, Xiumei Li, Nan Liu, Shurong Yang, Amin Wang, Jiayu Zhao, Jianbiao Peng
- 4574 4574 针对HR功能正常肿瘤的高效RAD51抑制剂,具备同类首创潜力 Highly potent inhibitors of RAD51, with first-in-class potential, targeting HR-proficient cancers Alessandro Galbiati, Daniela Asa, Pietro Picconi, Annamaria Marra, Claudia Stellato, Patrizia Banfi, Liviana Cozzi, Fabio Gasparri, Frank Narjes, Claudia Perrera, Alessia Montagnoli
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4575 · PDF 新型B7-H4靶向抗体-药物偶联物Mocertatug Rezetecan(GSK5733584)的非临床表征 Non-clinical characterization of Mocertatug Rezetecan (GSK5733584), a novel B7-H4-directed antibody-drug conjugate Jeremy Waight, Yuanfeng Zhou, Danni Sun, Lu Zhang, Jon Chung, Michael Adam, Wenjin Zhou, Pengchao Qiu, Jifa Fan, Anna Strobl, Jaegil Kim, Aishwarya Bhaskar, Srujana Neelam, Geeta Sharma, Shannon McKearnan, Huifeng Niu, Takahiro Sato, Derek Poore, Alexander Cocks, Prajna Behera, Chris Hopson, Ken Hance, Richard Davidson
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4576 · PDF 2X-121/stenoparib——一种在晚期卵巢癌2期临床试验中的新型PARP和tankyrase双重抑制剂——在临床相关药物浓度下阻断WNT信号通路并抑制人结直肠癌细胞系的生长 2X-121/ stenoparib - a novel, dual inhibitor of PARP and tankyrase in phase 2 clinical trials in advanced ovarian cancer- blocks the WNT signaling pathway and inhibits growth of human colorectal cancer cell lines at clinically relevant drug concentrations Louis F. Stancato, Sydney Leohr, Mustapha Moussaif, Mogens Winkel Madsen, Steen Knudsen, Annette Nielsen, Mette Jacobsen, Peter Gimsing, Thomas Jensen, Jeremy R. Graff
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4577 · PDF 用HBS-101靶向midkine驱动的致癌信号:一种针对肺癌的新型治疗策略 Targeting midkine-driven oncogenic signaling with HBS-101: A novel therapeutic strategy for lung cancer Roberto Borea, Francesco Drago, Malaak Sammour, Nigita Giovanni, Serena Li Zhao, Blake R. Peterson, Hareesh B. Nair, Christian Rolfo, Eswar Shankar
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4578 · PDF 发现同类最佳的小分子p53 Y220C重激活剂:突破效力天花板 Discovery of a Best-in-Class small molecule p53 Y220C reactivator: Breaking through the potency ceiling Ruben Boon, Jo Alen, Nihed Draoui, Koen Vandyck, Elke Behaeghel, Godelieve Lammens, Sandrine Vendeville, Lijs Beke, Pieter Peeters, Stéphane De Cesco, Bart Stoops, Pierre Raboisson, Francois Gonzalvez, Carla De Legher
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4579 · PDF 一种新型双曲线型NAMPT抑制剂联合pan-RAS靶向疗法在胰腺导管腺癌中的临床前评估 Preclinical evaluation of a novel hyperbolic NAMPT inhibitor in combination with pan-RAS targeted therapies in pancreatic ductal adenocarcinoma Husain Yar Khan, Mohammed Najeeb Al Hallak, Sahar F. Bannoura, Md. Hafiz Uddin, Bin Bao, Mohamad Walid Sukkari, Adeeb Aboukameel, Khalil Choucair, Hugo Jimenez, Grayson Barker, Callum McGrath, Ganji Purnachandra Nagaraju, Rafic Beydoun, Yang Shi, Philip A. Philip, Azeddine Atfi, Bassel El-Rayes, Ramzi M. Mohammad, Min Wu, Michael Schelle, Boris C. Pasche, Asfar S. Azmi
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4580 · PDF 新型PCNA抑制剂AOH1996在胰腺导管腺癌中与KRAS靶向疗法协同作用 Novel PCNA inhibitor AOH1996 synergizes with KRAS-targeted therapies in pancreatic ductal adenocarcinoma Sahar F. Bannoura, Husain Y. Khan, Md Hafiz Uddin, Amro Aboukameel, Yin Wan, Bin Bao, Adeeb Aboukameel, Rafic Beydoun, Pouya Haratipour, Long Gu, Muhammad Wasif Saif, Robert J. Hickey, Linda H. Malkas, Yang Shi, Mohammed Najeeb Al Hallak, Ramzi M. Mohammad, Boris C. Pasche, Asfar S. Azmi
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4581 · PDF 恢复突变型p53R273H DNA结合与活性的小分子 Small molecule restoring mutant p53R273H DNA binding and activity Anne Kingsland, Kyle P. Kisor, Emil Alexov, Diane L. Barber
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4582 · PDF 靶向MEIS2治疗铂耐药卵巢癌 Targeting MEIS2 in platinum resistant ovarian cancer Yinu Wang, Natalia Obrochta, Jennifer Heo, Junzui Li, Natalia Maria Masnica, Daniela E. Matei
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4583 · PDF 多靶点激酶抑制剂olverembatinib(HQP1351)在子宫内膜癌(EC)临床前模型中有效并与化疗产生协同作用 Multitarget kinase inhibitor olverembatinib (HQP1351) is efficacious and synergizes with chemotherapy in preclinical models of endometrial carcinoma (EC) Yan Xiong, Zhiyan Liang, Huidan Yu, Bingxing Wu, Guoqin Zhai, Zhou Yu, Dajun Yang, Yifan Zhai
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4584 · PDF 麦角甾醇过氧化物对三阴性乳腺癌细胞蛋白质稳态破坏的影响 Effects of ergosterol peroxide on proteostasis disruption in triple negative breast cancer cells Michelle Martínez-Montemayor, Aliyah Bocachica-Adorno, Adriana Aponte-Ramos, Taotao Ling, Fatima Rivas
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4585 · PDF 一种新型硫杂蒽酮激活p47phox以利用急性髓系白血病中的氧化还原脆弱性 A novel thioxanthenone activates p47phox to exploit redox vulnerabilities in acute myeloid leukemia Madison Gamble, Claudia M. Espitia, Sruthi Sureshkumar, Natalie Hakim, Kevin R. Kelly, Wei Wang, Steffan T. Nawrocki, Jennifer S. Carew
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4586 · PDF 用CB-5339抑制p97/VCP在肾细胞癌中诱导REDD1依赖性抗肿瘤活性 p97/VCP inhibition with CB-5339 induces REDD1-dependent antitumor activity in renal cell carcinoma Sruthi Sureshkumar, Claudia M. Espitia, Maria Janina Carrera Espinoza, Madison Gamble, Natalie Hakim, Kevin Kelly, Jennifer S. Carew, Steffan T. Nawrocki
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4587 · PDF 用GL-320抑制USP10增强NSCLC中化疗-免疫治疗疗效并克服耐药 USP10 inhibition with GL-320 enhances chemo-immunotherapy efficacy and overcomes resistance in NSCLC Sadaf Dorandish, Komal Bhayekar, Prahlad Parajuli, Amirreza Samarbakhsh, Babita Kushwaha, Yubin Ge, Navnath Gavande