Novel Antitumor Agents 2

• 4558 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
• 4559 · PDF 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
• 4560 · PDF 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
• 4561 · PDF 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
• 4562 · PDF 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
• 4563 · PDF 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
• 4564 · PDF 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
• 4565 · PDF 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
• 4566 · PDF 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
• 4567 · PDF 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
• 4568 · PDF 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
• 4569 · PDF 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
• 4570 · PDF 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
• 4571 · PDF 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
• 4572 · PDF 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
• 4573 · PDF 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 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
• 4575 · PDF 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
• 4576 · PDF 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
• 4577 · PDF 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
• 4578 · PDF 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
• 4579 · PDF 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
• 4580 · PDF 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
• 4581 · PDF Small molecule restoring mutant p53R273H DNA binding and activity Anne Kingsland, Kyle P. Kisor, Emil Alexov, Diane L. Barber
• 4582 · PDF Targeting MEIS2 in platinum resistant ovarian cancer Yinu Wang, Natalia Obrochta, Jennifer Heo, Junzui Li, Natalia Maria Masnica, Daniela E. Matei
• 4583 · PDF 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
• 4584 · PDF 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
• 4585 · PDF 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
• 4586 · PDF 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
• 4587 · PDF 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

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