Cancer Chemistry最新文献

{"title":"Abstract 324: Unbiased proteomic and phosphoproteomic analysis identifies response signatures and novel susceptibilities after combined MEK and mTOR inhibition in BRAFV600Emutant glioma","authors":"Micah J. Maxwell, A. Arnold, Heather Sweeney, Ljun Chen, T. Lih, M. Schnaubelt, C. Eberhart, Jeffrey A. Rubens, Hui Zhang, D. Clark, E. Raabe","doi":"10.1158/1538-7445.AM2021-324","DOIUrl":"https://doi.org/10.1158/1538-7445.AM2021-324","url":null,"abstract":"","PeriodicalId":9563,"journal":{"name":"Cancer Chemistry","volume":"74 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79849264","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Abstract 267: Light-activated molecular nanomachines kill bladder cancer cells","authors":"S. Nagaraju, Alexis van Venrooy, P. Hensley, K. Bree, C. Ayala-Orozco, N. Brooks, D. Izhaky, J. Tour, A. Kamat","doi":"10.1158/1538-7445.AM2021-267","DOIUrl":"https://doi.org/10.1158/1538-7445.AM2021-267","url":null,"abstract":"","PeriodicalId":9563,"journal":{"name":"Cancer Chemistry","volume":"10 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79946325","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Abstract 286: Conception and preparation of new potent antimicrotubule agents","authors":"Mathieu Gagné-Boulet, Chahrazed Bouzriba, Atziri Corin Chavez Alvarez, S. Fortin","doi":"10.1158/1538-7445.AM2021-286","DOIUrl":"https://doi.org/10.1158/1538-7445.AM2021-286","url":null,"abstract":"","PeriodicalId":9563,"journal":{"name":"Cancer Chemistry","volume":"42 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85170290","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Abstract 319: MALDI-IMS of N-glycan profiles of molecular subclasses of human hepatocellular carcinoma","authors":"A. DelaCourt, A. Mehta, Alyson P. Black, R. Drake, P. Angel, Y. Hoshida","doi":"10.1158/1538-7445.AM2021-319","DOIUrl":"https://doi.org/10.1158/1538-7445.AM2021-319","url":null,"abstract":"","PeriodicalId":9563,"journal":{"name":"Cancer Chemistry","volume":"31 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91299719","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Abstract 17: Proteogenomic characterization of pancreatic ductal adenocarcinoma","authors":"Liwei Cao, Chen Huang, D. Zhou, O. Bathe, Daniel W. Chan, R. Hruban, Lisha Ding, Bing Zhang, Hui Zhang","doi":"10.1158/1538-7445.AM2021-17","DOIUrl":"https://doi.org/10.1158/1538-7445.AM2021-17","url":null,"abstract":"","PeriodicalId":9563,"journal":{"name":"Cancer Chemistry","volume":"60 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77891862","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Abstract 305: ELU001, a targeted C'Dot drug conjugate (CDC) for the treatment of folate receptor alpha (FRα) overexpressing cancers","authors":"G. Adams, Kai Ma, A. Venkatesan, F. Chen, Feixuan Wu, Melik Z. Turker, Thomas C. Gardinier, Pei-Ming Chen, Vaibhav Patel, E. Bayever, Paul Rudick, Geno Germano","doi":"10.1158/1538-7445.AM2021-305","DOIUrl":"https://doi.org/10.1158/1538-7445.AM2021-305","url":null,"abstract":"CDCs are novel ultra-small (6-7 nm) nanoparticle drug conjugates that have been demonstrated to be capable of faster tumor targeting and deeper tumor penetration than antibody drug conjugates in animal models. CDCs are capable of targeting tumors in the brain and pancreas that are difficult to access, while exhibiting limited exposure to normal tissues due their efficient renal elimination. CDCs are composed of a silica core, in which Cy5, a far red dye is covalently encapsulated. The silica core is covalently coated with a layer of polyethylene glycol which is then functionalized with targeting moieties and payloads. ELU001 is a CDC functionalized with ~20 molecules of the topoisomerase-1 inhibitor exatecan linked via a proteolytic cleavable linker as a payload and ~15 folic acids to provide targeting to FRα overexpressing cancers. ELU001 is rapidly internalized into FRα expressing cells and is trafficked to the lysosome where the payload is released from the CDC. ELU001 exhibits potency in the low single digit nanomolar to sub-nanomolar range against cancer cells that express 3+ (KB, IGROV-1) and 2+ (SK-OV-3, HCC827 and OVCAR-3) levels of FRα after a 6-hr exposure in a 7-day viability study. In contrast, an anti-FRα ADC based ADC mirvetuximab soravtansine exhibits lower potency (>100 nM IC50) against SK-OV-3 and HCC827 cells and 40 nM IC50 against OVCAR-3 cells. ELU001 exhibits potent efficacy against established s.c. KB human cervical tumor xenografts in immunodeficient mice with significantly better efficacy and safety than free exatecan payload. It is also effective in treating established SK-OV-3 tumors with lower (2+) FRα expression, a setting where the ADC is again less effective. IND-enabling nonclinical studies are currently underway to prepare for initiation of a first-in-human phase 1 clinical trial in subjects with FRα overexpressing cancers in the second half of 2021. Citation Format: Gregory Paul Adams, Kai Ma, Aranapakam Venkatesan, Feng Chen, Fei Wu, Melik Turker, Thomas Gardinier, Peiming Chen, Vaibhav Patel, Eliel Bayever, Paul Rudick, Geno Germano. ELU001, a targeted C9Dot drug conjugate (CDC) for the treatment of folate receptor alpha (FRα) overexpressing cancers [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2021; 2021 Apr 10-15 and May 17-21. Philadelphia (PA): AACR; Cancer Res 2021;81(13_Suppl):Abstract nr 305.","PeriodicalId":9563,"journal":{"name":"Cancer Chemistry","volume":"571 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77786844","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Abstract 313: Synergistic interaction between gingerol, shogaol and paradol with platinum-based chemotherapeutic drugs against naïve and resistant breast cancer cells","authors":"A. S. Bawadood, F. Al-Abbasi, A. El-Halawany, A. M. Al-Abd","doi":"10.1158/1538-7445.AM2021-313","DOIUrl":"https://doi.org/10.1158/1538-7445.AM2021-313","url":null,"abstract":"Breast cancer is one of the most common female cancers and contributes 25.4% of the total diagnosed malignancies in women in 2018. Shogaol, paradol, and gingerol are obtained from many plants belonging to the family Zingiberaceae such as dried ginger and grain of paradise and shows different pharmacological activities. The current study evaluated the anticancer potential of these compounds in combination with chemotherapeutic platinum drugs against breast cancer cells. Cytotoxicity assay, apoptosis assay, immunofluorescent staining cell surface marker analysis, and wound healing assay were used for evaluating the cytotoxic potential of these compounds alone and in combination with platinum chemotherapeutics agents against naive and resistant breast cancer cell lines (MDA-MB-231 and MCF-7adr, respectively). Platinum drugs showed synergism in combination with shogaol and gingerol against the resistant breast cancer cells (MCF-7adr) with a Combination Index (CI) values of 0.39 and 0.54, respectively. A significant increase was observed in the percentages of early and late apoptotic cells for MDA-MB-231 cells treated with 6-shogaol for 24h. Significant decrease in CD44+/CD24- subpopulation was recorded in both cell lines using flowcytometric analysis. In the Wound healing assay, cells treated with the test compounds migrated significantly slower than control and needed a longer time to heal the scratch. In conclusion, gingerol, shogaol, and paradol compounds showed synergistic cytotoxicity with platinum-based drug and augmented their migration inhibitory activity, apoptotic effects, and tumor-associated stem cell suppressive the potential within naive and resistant breast cancer cells. Citation Format: Aziza S. Bawadood, Fahad A. Al-Abbasi, Ali M. El-Halawany, Ahmed M. Al-Abd. Synergistic interaction between gingerol, shogaol and paradol with platinum-based chemotherapeutic drugs against naive and resistant breast cancer cells [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2021; 2021 Apr 10-15 and May 17-21. Philadelphia (PA): AACR; Cancer Res 2021;81(13_Suppl):Abstract nr 313.","PeriodicalId":9563,"journal":{"name":"Cancer Chemistry","volume":"25 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90300169","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Abstract 21: LiP-MS, a machine learning-based chemoproteomic approach to identify drug targets in complex proteomes","authors":"N. Beaton, Yuehan Feng, R. Bruderer, Adam Hendricks, Ghaith M. Hamza, Eric Miele, Rick Davies, K. Beeler, Ilaria Piazza, P. Picotti, P. Castaldi, L. Reiter","doi":"10.1158/1538-7445.AM2021-21","DOIUrl":"https://doi.org/10.1158/1538-7445.AM2021-21","url":null,"abstract":"","PeriodicalId":9563,"journal":{"name":"Cancer Chemistry","volume":"18 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73927834","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Abstract 320: Glycan analysis from tissue to serum, identification and validation of a biomarker for the early detection of hepatocellular carcinoma","authors":"A. Mehta, Mengjun Wang, Connor A. West, Alyson P. Black, P. Angel, Richard Drakje","doi":"10.1158/1538-7445.AM2021-320","DOIUrl":"https://doi.org/10.1158/1538-7445.AM2021-320","url":null,"abstract":"","PeriodicalId":9563,"journal":{"name":"Cancer Chemistry","volume":"27 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89445597","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Abstract 285: Development of phenyl 4-(2-oxo-3-alkylimidazolidin-1-yl)benzenesulfonates as new antimitotic cytochrome P450 1A1-activated prodrugs selective toward breast cancers: Evaluation of branched alkyl chains","authors":"Chahrazed Bouzriba, Atziri Corin Chavez Alvarez, Mathieu Gagné-Boulet, J. Lacroix, M. Côté, René C.-Gaudrault, S. Fortin","doi":"10.1158/1538-7445.AM2021-285","DOIUrl":"https://doi.org/10.1158/1538-7445.AM2021-285","url":null,"abstract":"","PeriodicalId":9563,"journal":{"name":"Cancer Chemistry","volume":"1994 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82428663","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}