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Journal Mol. Cancer Ther.

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Preclinical Development of MGC018, a Duocarmycin-based Antibody-drug Conjugate Targeting B7-H3 for Solid Cancer.

Juniper A Scribner, Jennifer G Brown, Thomas Son, Michael Chiechi, Pam Li, Sharad Sharma, Hua Li, Anushka De Costa, Ying Li, Yan Chen, Ann Easton, Nicholas C Yee-Toy, Francine Z Chen, Sergey Gorlatov, Bhaswati Barat, Ling Huang, Christina R Wolff, Jeff Hooley, Tim E Hotaling, Timur Gaynutdinov, Valentina Ciccarone, James Tamura, Scott Koenig, Paul A Moore, Ezio Bonvini, Deryk Loo,

B7-H3, also referred to as CD276, is a member of the B7 family of immune regulatory proteins. B7-H3 is overexpressed on many solid cancers, including prostate cancer, renal cell carcinoma, melanoma, squamous cell carcinoma of the head and neck, non-small cell lung cancer and breast cancer. Over-expression of B7-H3 is ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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CH7233163 overcomes osimertinib resistant EGFR-Del19/T790M/C797S mutation.

Kenji Kashima, Hiroki Kawauchi, Hiromi Tanimura, Yukako Tachibana, Takashi Chiba, Takuya Torizawa, Hiroshi Sakamoto,

Osimertinib is the only EGFR-tyrosine kinase inhibitor (TKI) capable of overcoming EGFR-T790M-mutated NSCLC, but osimertinib-resistant EGFR triple mutations (Del19/T790M/C797S or L858R/T790M/C797S) have been reported. Although allosteric EGFR TKIs (eg. EAI-045) which potentially overcome L858R/T790M/C797S have been identified, there are no effective inhibitors against Del19/T790M/C797S. In this study, we identified CH7233163 ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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Dual mechanisms of novel CD73-targeted antibody and antibody-drug conjugate in inhibiting lung tumor growth and promoting antitumor immune-effector function.

Rui Jin, Liang Liu, Yun Xing, Tao Meng, Lanping Ma, Jinpeng Pei, Ying Cong, Xuesai Zhang, Zhiqiang Ren, Xin Wang, Jingkang Shen, Ker Yu,

While the tyrosine kinase inhibitor (TKI) therapy and immunotherapy have significantly improved lung cancer management, many patients do not benefit or become resistant to treatment, highlighting the need for novel treatments. We found elevated CD73 expression to be prevalent in non-small cell lung cancer (NSCLC) including those harboring the RAS- ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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Efficacy, tolerability and pharmacokinetics of combined targeted MEK and dual mTORC1/2 inhibition in a preclinical model of mucosal melanoma.

Bih-Rong Wei, Shelley B Hoover, Cody J Peer, Jennifer E Dwyer, Hibret A Adissu, Priya Shankarappa, Howard Yang, Maxwell Lee, Tyler J Peat, William D Figg, R Mark Simpson,

Melanomas arising in the mucous membranes are a rare and aggressive subtype. New treatment approaches are needed, yet accumulating sufficient evidence to improve patient outcomes is difficult. Clinical and pathological correlates between human and canine mucosal melanomas (MM) are substantial, and the relatively greater incidence of spontaneous naturally occurring MM ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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Microparticle Encapsulation of a Prostate-Targeted Biologic for the Treatment of Liver Metastases in a Preclinical Model of Castration-Resistant Prostate Cancer.

Oliver C Rogers, Lizamma Antony, Oren Levy, Nitin Joshi, Brian W Simons, Susan Dalrymple, Marc Rosen, Andrew Pickering, Haoyue Lan, Heidi Kuang, Sudhir H Ranganath, Lei Zheng, Jeffrey M Karp, S Peter Howard, Samuel R Denmeade, John T Isaacs, W Nathaniel Brennen,

PRX302 is a highly potent mutant bacterial pore-forming biologic protoxin engineered for selective activation by prostate specific antigen (PSA), a serine protease expressed by benign and malignant prostate epithelial cells. Though being developed as a local therapy for benign prostatic hyperplasia and localized prostate cancer, PRX302 cannot be administered systemically ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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Osimertinib, an EGFR tyrosine kinase inhibitor, exerts anti-tumor activity in preclinical NSCLC models harboring the uncommon EGFR mutations G719X or L861Q or S768I.

Nicolas Floc'h, Sangbin Lim, Sue Bickerton, Afshan Ahmed, Jonathan Orme, Jelena Urosevic, Matthew J Martin, Darren Ae Cross, Byoung Chul Cho, Paul D Smith,

Osimertinib is an oral, third-generation, irreversible epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) that selectively inhibits both EGFR-TKI-sensitizing and EGFR T790M resistance mutations with lower activity against wild-type EGFR and has demonstrated efficacy in NSCLC CNS metastases. The sensitizing mutations, the in-frame deletions in exon 19 and the L858R ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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Enhanced immunotherapy with LHRH-R targeted lytic peptide in ovarian cancer.

Mark Seungwook Kim, Shaolin Ma, Anca Chelariu-Raicu, Carola Leuschner, Hector W Alila, Sanghoon Lee, Robert L Coleman, Anil K Sood,

Here, We examined the role of EP-100 (luteinizing hormone-releasing hormone (LHRH) ligand joined to a lytic peptide), improving the efficacy of immune checkpoint blockade. LHRH-R-positive murine ovarian cancer cells (ID8, IG10, IF5, and 2C12) were sensitive to EP-100 and were specifically killed at low micromolar levels through LHRH-R. EP-100 increased ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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Synthetic Lethal Metabolic Targeting of Androgen Deprived Prostate Cancer Cells with Metformin.

Bing Yang, Shivashankar Damodaran, Tariq A Khemees, Mikolaj J Filon, Adam Schultz, Joseph Gawdzik, Tyler Etheridge, Dmitry Malin, Kyle A Richards, Vincent L Cryns, David F Jarrard,

The initiation of androgen deprivation therapy (ADT) induces susceptibilities in prostate cancer (PC) cells that make them vulnerable to synergistic treatment and enhanced cell death. Senescence results in cell cycle arrest, but cells remain viable. In this study, we investigated the mechanisms by which PC cells undergo senescence in response ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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Therapeutic Targeting of Mitochondrial One-Carbon Metabolism in Cancer.

Aamod S Dekhne, Zhanjun Hou, Aleem Gangjee, Larry H Matherly,

One-carbon (1C) metabolism encompasses folate-mediated 1C transfer reactions and related processes, including nucleotide and amino acid biosynthesis, antioxidant regeneration, and epigenetic regulation. 1C pathways are compartmentalized in the cytosol, mitochondria and nucleus. 1C metabolism in the cytosol has been an important therapeutic target for cancer since the inception of modern ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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Selected Articles from This Issue.

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, 19(9):1761]

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An RNA-binding protein, Hu-antigen R, in pancreatic cancer epithelial to mesenchymal transition, metastasis, and cancer stem cells.

Ruochen Dong, Ping Chen, Kishore Polireddy, Xiaoqing Wu, Tao Wang, Remya Ramesh, Dan A Dixon, Liang Xu, Jeffrey Aubé, Qi Chen,

Pancreatic cancer has poor prognosis and treatment outcomes due to its highly metastatic nature and resistance to current treatments. The RNA binding protein (RBP) Hu-antigen R (HuR) is a central player in posttranscriptional regulation of cancer related gene expression, and contributes to tumorigenesis, tumor growth, metastasis and drug resistance. HuR ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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Menin-mediated repression of glycolysis in combination with autophagy protects colon cancer against small molecule EGFR inhibitors.

Bryson W Katona, Taylor Hojnacki, Rebecca A Glynn, Kayla E Paulosky, Katherine M Szigety, Yan Cao, Xuyao Zhang, Zijie Feng, Xin He, Jian Ma, Xianxin Hua,

Menin serves both tumor suppressor and promoter roles in a highly tumor-specific manner. In colorectal cancer (CRC) menin is over-expressed and plays a critical role in regulating transcription of SKP2, and combined treatment with a menin inhibitor (MI) and small molecule EGFR inhibitor (EGFRi) leads to synergistic killing of CRC ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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Correction: In Vitro and In Vivo Synergistic Antitumor Activity of the Combination of BKM120 and Erlotinib in Head and Neck Cancer: Mechanism of Apoptosis and Resistance.

Abu Syed Md Anisuzzaman, Abedul Haque, Dongsheng Wang, Mohammad Aminur Rahman, Chao Zhang, Zhengjia Chen, Zhuo Georgia Chen, Dong M Shin, A R M Ruhul Amin,

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, 19(9):1955]

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LILRB4-Targeting Antibody-Drug Conjugates for the Treatment of Acute Myeloid Leukemia.

Yasuaki Anami, Mi Deng, Xun Gui, Aiko Yamaguchi, Chisato M Yamazaki, Ningyan Zhang, Chengcheng Zhang, Zhiqiang An, Kyoji Tsuchikama,

Acute myeloid leukemia (AML) is the most common and aggressive blood cancer in adults. In particular, significant unmet medical needs exist for effective treatment strategies for M4 and M5 AML subtypes. Antibody-drug conjugates (ADCs) are a promising drug class for AML therapy, as demonstrated by the FDA-approved anti-CD33 ADC gemutuzumab ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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Concurrent Targeting of Potential Cancer Stem Cells Regulating Pathways Sensitizes Lung Adenocarcinoma to Standard Chemotherapy.

Masahiro Shibata, Akira Ooki, Yoshikuni Inokawa, Pritam Sadhukhan, M Talha Ugurlu, Evgeny Izumchenko, Enrico Munari, Giuseppe Bogina, Charles M Rudin, Edward Gabrielson, Anju Singh, Mohammad O Hoque,

Cancer stem cells (CSC) are highly resistant to conventional chemotherapeutic drugs. YAP1 and STAT3 are the two transcription factors that facilitate the therapeutic resistance and expansion of CSCs. The objective of this study was to understand the cross-talk between YAP1 and STAT3 activities and to determine the therapeutic efficacy of ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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The dual androgen receptor and glucocorticoid receptor antagonist CB-03-10 as potential treatment for tumors that have acquired GR-mediated resistance to AR blockade.

Caridad Rosette, Frances J Agan, Niccolette Rosette, Alessandro Mazzetti, Luigi Moro, Mara Gerloni,

CB-03-10 (cortexolone 17α-valerate-21-propionate) is a synthetic steroidal compound derived from cortexolone (11-deoxycortisone), an intermediate in cortisol biosynthesis. Characterization of the activity of CB-03-10 and its main related compound CB-03-05 (cortexolone 17α-valerate) included in vitro binding to the androgen and glucocorticoid receptors (AR and GR), antagonism of AR and GR transcriptional ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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Dysregulation of EAAT2 and VGLUT2 spinal glutamate transports via histone deacetylase 2 (HDAC2) contributes to paclitaxel-induced painful neuropathy.

Xiao-Min Wang, Pan Gu, Leorey Saligan, Michael Iadarola, Lian Kah Ti, Stanley Wong, Chi Wai Cheung,

Effective treatments for chemotherapy-induced peripheral neuropathy (CIPN) remain unavailable. Given the significance of spinal cord glutamate transporters in neuronal plasticity and central sensitization, this study investigated the role of excitatory amino acid transporter 2 (EAAT2) and vesicular-glutamate transporter 2 (VGLUT2) in the development of paclitaxel-induced painful neuropathy. Paclitaxel (2 mg/kg, ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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Antihistamine Drug Ebastine inhibits cancer growth by targeting Polycomb Group Protein EZH2.

Qiaqia Li, Kilia Y Liu, Qipeng Liu, Guangyu Wang, Weihua Jiang, Qingshu Meng, Yang Yi, Yongyong Yang, Rui Wang, Sen Zhu, Chao Li, Longxiang Wu, Dongyu Zhao, Lin Yan, Lili Zhang, Jung-Sun Kim, Xiongbing Zu, Anthony J Kozielski, Wei Qian, Jenny C Chang, Akash Patnaik, Kaifu Chen, Qi Cao,

Enhancer of Zester Homolog 2 (EZH2), a histone lysine methyltransferase and the catalytic component of Polycomb Repressive Complex 2, has been extensively investigated as a chromatin regulator and a transcriptional suppressor by methylating H3 at lysine 27 (H3K27). EZH2 is upregulated or mutated in most cancers, and its expression levels ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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Dual epitope targeting and enhanced hexamerization by DR5 antibodies as a novel approach to induce potent anti-tumor activity through DR5 agonism.

Marije B Overdijk, Kristin Strumane, Frank J Beurskens, Antonio Ortiz Buijsse, Claudine Vermot-Desroches, Boris S Vuillermoz, Thessa Kroes, Bart de Jong, Naomi Hoevenaars, Richard G Hibbert, Andreas Lingnau, Ulf Forssmann, Janine Schuurman, Paul W H I Parren, Rob N de Jong, Esther C W Breij,

Higher order DR5 clustering can induce tumor cell death, however therapeutic compounds targeting DR5 have achieved limited clinical efficacy. We describe HexaBody-DR5/DR5, an equimolar mixture of two DR5-specific IgG1 antibodies with an Fc-domain mutation that augments antibody hexamerization after cell surface target binding. The two antibodies do not compete for ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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Targeting Multiple EGFR Expressing Tumors with a Highly Potent Tumor-Selective Antibody Drug Conjugate.

Mark G Anderson, Hugh D Falls, Michael J Mitten, Anatol Oleksijew, Kedar S Vaidya, Erwin R Boghaert, Wenqing Gao, Joann P Palma, Diana Cao, Puey-Ling Chia, Thomas John, Hui K Gan, Andrew M Scott, Edward B Reilly,

ABBV-321 (serclutamab talirine), a next-generation epidermal growth factor receptor (EGFR)-targeted antibody-drug conjugate (ADC) incorporates a potent pyrrolobenzodiazepine (PBD) dimer toxin conjugated to the EGFR-targeting ABT-806 affinity matured AM1 antibody. ABBV-321 follows the development of related EGFR targeted ADCs including depatuxizumab mafodotin (depatux-m, ABT-414), ABT-806 conjugated to monomethyl auristatin F (MMAF), ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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Targeted radionuclide therapy in patient-derived xenografts using 177Lu-EB-RGD.

Liang Zhao, Haojun Chen, Zhide Guo, Kaili Fu, Lanlin Yao, Li Fu, Weixi Guo, Xuejun Wen, Orit Jacobson, Xianzhong Zhang, Long Sun, Hua Wu, Qin Lin, Xiaoyuan Chen,

Currently, most patients with non-small cell lung cancer (NSCLC) are diagnosed in advanced stages with a poor five-year survival rate. Therefore, intensive research aimed at finding novel therapeutic strategies has been ongoing; experimental models that reliably emulate NSCLC disease are greatly needed to predict responses to novel therapeutics. Therefore, we ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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Pharmacologic Properties and Preclinical Activity of Sasanlimab, A High-Affinity Engineered Anti-Human PD-1 Antibody.

Amir A Al-Khami, Sawsan Youssef, Yasmina Abdiche, HoangKim Nguyen, Joyce Chou, Christopher R Kimberlin, Sherman M Chin, Cris Kamperschroer, Bart Jessen, Brent Kern, Natalija Budimir, Christopher P Dillon, Allison Xu, Jerry D Clark, Jeffrey Chou, Eugenia Kraynov, Arvind Rajpal, John C Lin, Shahram Salek-Ardakani,

Development of antagonistic monoclonal antibodies that specifically target the immune checkpoint receptor, programmed cell death protein 1 (PD-1) is of great interest for cancer immunotherapy. Here we report the biophysical characteristics and non-clinical antagonistic activities of sasanlimab (PF-06801591), a humanized anti-PD-1 antibody of IgG4 isotype. We show that sasanlimab binds ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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Nf1 mutant tumors undergo transcriptome and kinome re-modeling after inhibition of either mTOR or MEK.

Daniela Pucciarelli, Steven P Angus, Benjamin Huang, Chi Zhang, Hiroki J Nakaoka, Ganesh Krishnamurthi, Sourav Bandyopadhyay, D Wade Clapp, Kevin Shannon, Gary L Johnson, Jean L Nakamura,

Loss of the tumor suppressor NF1 leads to activation of RAS effector pathways, which are therapeutically targeted by inhibition of mTOR (mTORi) or MEK (MEKi). However, therapeutic inhibition of RAS effectors leads to the development of drug resistance and ultimately disease progression. To investigate molecular signatures in the context of ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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Phase I, pharmacogenomic, drug-interaction study of sorafenib and bevacizumab in combination with paclitaxel in patients with advanced refractory solid tumors.

E Gabriela Chiorean, Susan M Perkins, Robert M Strother, Anne Younger, Jennifer M Funke, Safi G Shahda, Noah M Hahn, Kumaresan Sandrasegaran, David R Jones, Todd C Skaar, Bryan P Schneider, Christopher J Sweeney, Daniela E Matei,

Vascular endothelial growth factor (VEGF) blockade does not uniformly result in clinical benefit. We evaluated safety, dose-limiting toxicities (DLTs), recommended phase II dose (RP2D), antitumor efficacy, and exploratory biomarkers including pharmacogenomics and pharmacokinetics with sorafenib, bevacizumab and paclitaxel in refractory cancer patients. The study had a "3+3" design, using paclitaxel ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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Circulating Tumor Cells In Advanced Cervical Cancer: NRG Oncology - Gynecologic Oncology Group Study 240 (NCT 00803062).

Krishnansu S Tewari, Michael W Sill, Bradley J Monk, Richard T Penson, David H Moore, Heather A Lankes, Lois M Ramondetta, Lisa M Landrum, Leslie M Randall, Ana Oaknin, Mario M Leitao, Eric L Eisenhauer, Paul DiSilvestro, Linda Van Le, Michael L Pearl, James J Burke, Ritu Salani, Debra L Richardson, Helen E Michael, David W Kindelberger, Michael J Birrer,

PURPOSE:To isolate circulating tumor cells (CTCs) from women with advanced cervical cancer and estimate the impact of CTCs and treatment on overall survival (OS) and progression-free survival (PFS). EXPERIMENTAL DESIGN:7.5 mL of whole blood was drawn pre-cycle 1 and 36 days post-cycle 1 from patients enrolled on Gynecologic Oncology Group ... Read more >>

Mol. Cancer Ther. (Molecular cancer therapeutics)
[2020, :]

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