Retaspimycin (BioDeep_00000776407)
代谢物信息卡片
Retaspimycin
化学式: C31H45N3O8 (587.320649)
中文名称: 瑞他霉素
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CC1CC(C(C(C=C(C(C(C=CC=C(C(=O)NC2=CC(=C(C(=C2O)C1)NCC=C)O)C)OC)OC(=O)N)C)C)O)OC
InChI: InChI=1S/C31H45N3O8/c1-8-12-33-26-21-13-17(2)14-25(41-7)27(36)19(4)15-20(5)29(42-31(32)39)24(40-6)11-9-10-18(3)30(38)34-22(28(21)37)16-23(26)35/h8-11,15-17,19,24-25,27,29,33,35-37H,1,12-14H2,2-7H3,(H2,32,39)(H,34,38)/b11-9-,18-10+,20-15+/t17-,19+,24+,25+,27-,29+/m1/s1
描述信息
C274 - Antineoplastic Agent > C2189 - Signal Transduction Inhibitor > C129824 - Antineoplastic Protein Inhibitor
C274 - Antineoplastic Agent > C186664 - Cytotoxic Chemotherapeutic Agent > C259 - Antineoplastic Antibiotic
D000890 - Anti-Infective Agents > D000900 - Anti-Bacterial Agents > D007769 - Lactams
同义名列表
1 个代谢物同义名
数据库引用编号
6 个数据库交叉引用编号
- ChEBI: CHEBI:71975
- KEGGdrug: D09375
- PubChem: 11534420
- DrugBank: DB05626
- ChEMBL: CHEMBL1184904
- CAS: 857402-23-4
分类词条
相关代谢途径
Reactome(0)
BioCyc(0)
PlantCyc(0)
代谢反应
0 个相关的代谢反应过程信息。
Reactome(0)
BioCyc(0)
WikiPathways(0)
Plant Reactome(0)
INOH(0)
PlantCyc(0)
COVID-19 Disease Map(0)
PathBank(0)
PharmGKB(0)
0 个相关的物种来源信息
在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有：
- PubMed: 来源于PubMed文献库中的文献信息，我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表，这个列表按照代谢物同时出现的文献数量降序排序，取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
- NCBI Taxonomy: 通过文献数据挖掘，得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序，取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
- Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
- Chemical Reaction: 在化学反应过程中，存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。
点击图上的相关代谢物的名称，可以跳转到相关代谢物的信息页面。
文献列表
- Gui-Sheng Xu, Yu-Ning Lin, Qingzhong Zeng, Zhi-Peng Li, Teng Xiao, Yong-Sheng Ye, Zhen-Yan Li, Xuejuan Gao. HSP90-regulated CHIP/TRIM21/p21 Axis Involves in the Senescence of Osteosarcoma Cells.
Protein and peptide letters.
2023; 30(6):513-519. doi:
10.2174/0929866530666230519101148. [PMID: 37211848] - Zeynep Gizem Todurga Seven, Fatma Kubra Tombulturk, Selim Gokdemir, Sibel Ozyazgan. The Effects of the Heat Shock Protein 90 Inhibitor 17-Allylamino-17-Demethoxygeldanamycin, Cannabinoid Agonist WIN 55,212-2, and Nitric Oxide Synthase Inhibitor Nω-Nitro-L-Arginine Methyl Ester Hydrochloride on the Serotonin and Dry Skin-Induced Itch.
International archives of allergy and immunology.
2022; 183(4):443-452. doi:
10.1159/000520509. [PMID: 34864727] - M H Raymonda, J H Ciesla, M Monaghan, J Leach, G Asantewaa, L A Smorodintsev-Schiller, M M Lutz, X L Schafer, T Takimoto, S Dewhurst, J Munger, I S Harris. Pharmacologic profiling reveals lapatinib as a novel antiviral against SARS-CoV-2 in vitro.
Virology.
2022 01; 566(?):60-68. doi:
10.1016/j.virol.2021.11.008. [PMID: 34871905] - Ge Li, Chuang Zhang, Wei Liang, Yanbing Zhang, Yunheng Shen, Xinhui Tian. Berberine regulates the Notch1/PTEN/PI3K/AKT/mTOR pathway and acts synergistically with 17-AAG and SAHA in SW480 colon cancer cells.
Pharmaceutical biology.
2021 Dec; 59(1):21-30. doi:
10.1080/13880209.2020.1865407. [PMID: 33417512] - Cun Li, Hin Chu, Xiaojuan Liu, Man Chun Chiu, Xiaoyu Zhao, Dong Wang, Yuxuan Wei, Yuxin Hou, Huiping Shuai, Jianpiao Cai, Jasper Fuk-Woo Chan, Jie Zhou, Kwok Yung Yuen. Human coronavirus dependency on host heat shock protein 90 reveals an antiviral target.
Emerging microbes & infections.
2020 Dec; 9(1):2663-2672. doi:
10.1080/22221751.2020.1850183. [PMID: 33179566] - Vinícius Couto Pires, Carla Pires Magalhães, Marcos Ferrante, Juliana de Souza Rebouças, Paul Nguewa, Patrícia Severino, Aldina Barral, Patrícia Sampaio Tavares Veras, Fabio Rocha Formiga. Solid lipid nanoparticles as a novel formulation approach for tanespimycin (17-AAG) against leishmania infections: Preparation, characterization and macrophage uptake.
Acta tropica.
2020 Nov; 211(?):105595. doi:
10.1016/j.actatropica.2020.105595. [PMID: 32585150] - Mohammed M Kassem, Furqan Muqri, Mary Dacosta, David Bruch, Vivian Gahtan, Kristopher G Maier. Inhibition of heat shock protein 90 attenuates post‑angioplasty intimal hyperplasia.
Molecular medicine reports.
2020 04; 21(4):1959-1964. doi:
10.3892/mmr.2020.10994. [PMID: 32319637] - Jianrong Wu, Shiwei Niu, David H Bremner, Wei Nie, Zi Fu, Dejian Li, Li-Min Zhu. A Tumor Microenvironment-Responsive Biodegradable Mesoporous Nanosystem for Anti-Inflammation and Cancer Theranostics.
Advanced healthcare materials.
2020 01; 9(2):e1901307. doi:
10.1002/adhm.201901307. [PMID: 31814332] - Kay Yi Chong, Min Kang, Francesca Garofalo, Daiki Ueno, Huamao Liang, Sarah Cady, Oluwagbemisola Madarikan, Nicholas Pitruzzello, Cheng-Hsiu Tsai, Tobias M P Hartwich, Brian M Shuch, Yang Yang-Hartwich. Inhibition of Heat Shock Protein 90 suppresses TWIST1 Transcription.
Molecular pharmacology.
2019 08; 96(2):168-179. doi:
10.1124/mol.119.116137. [PMID: 31175180] - Yumiko Asahi, Fumimasa Nomura, Yasuyuki Abe, Masafumi Doi, Tomoko Sakakura, Kiyoshi Takasuna, Kenji Yasuda. Electrophysiological evaluation of pentamidine and 17-AAG in human stem cell-derived cardiomyocytes for safety assessment.
European journal of pharmacology.
2019 Jan; 842(?):221-230. doi:
10.1016/j.ejphar.2018.10.046. [PMID: 30391349] - Markus Dietrich, Muhammad Salman Malik, Filip Nikolaysen, Marianne Skeie, Espen Stang. Protein kinase C mediated internalization of ErbB2 is independent of clathrin, ubiquitination and Hsp90 dissociation.
Experimental cell research.
2018 10; 371(1):139-150. doi:
10.1016/j.yexcr.2018.08.004. [PMID: 30098331] - Chao Lv, Hua-Wu Zeng, Jin-Xin Wang, Xing Yuan, Chuang Zhang, Ting Fang, Pei-Ming Yang, Tong Wu, Yu-Dong Zhou, Dale G Nagle, Wei-Dong Zhang. The antitumor natural product tanshinone IIA inhibits protein kinase C and acts synergistically with 17-AAG.
Cell death & disease.
2018 02; 9(2):165. doi:
10.1038/s41419-017-0247-5. [PMID: 29416003] - Kinga A Kocemba-Pilarczyk, Barbara Ostrowska, Sonia Trojan, Ecce Aslan, Dorota Kusior, Małgorzata Lasota, Claire Lenouvel, Joanna Dulińska-Litewka. Targeting the hypoxia pathway in malignant plasma cells by using 17-allylamino-17-demethoxygeldanamycin.
Acta biochimica Polonica.
2018; 65(1):101-109. doi:
10.18388/abp.2017_1630. [PMID: 29543923] - Liang Ma, Dawei Yang, Zhaoxin Li, Xin Zhang, Lei Pu. Co-delivery of paclitaxel and tanespimycin in lipid nanoparticles enhanced anti-gastric-tumor effect in vitro and in vivo.
Artificial cells, nanomedicine, and biotechnology.
2018; 46(sup2):904-911. doi:
10.1080/21691401.2018.1472101. [PMID: 29757014] - Ayodeji Odunewu-Aderibigbe, Larry Fliegel. Protein mediated regulation of the NHE1 isoform of the Na+/H+ exchanger in renal cells. A regulatory role of Hsp90 and AKT kinase.
Cellular signalling.
2017 08; 36(?):145-153. doi:
10.1016/j.cellsig.2017.05.003. [PMID: 28483634] - Biki Gupta, Shiva Pathak, Bijay Kumar Poudel, Shobha Regmi, Hima Bindu Ruttala, Milan Gautam, Jong Seong Lee, Jee-Heon Jeong, Han-Gon Choi, Chul Soon Yong, Jong Oh Kim. Folate receptor-targeted hybrid lipid-core nanocapsules for sequential delivery of doxorubicin and tanespimycin.
Colloids and surfaces. B, Biointerfaces.
2017 Jul; 155(?):83-92. doi:
10.1016/j.colsurfb.2017.04.010. [PMID: 28410515] - Hang Jung Lee, DO Hyung Kim, Seung Jin Lee. 17-Allylamino-17-demethoxygeldanamycin-induced Changes in [18F]Fluorothymidine Uptake.
Anticancer research.
2017 06; 37(6):2993-2999. doi:
10.21873/anticanres.11653. [PMID: 28551637] - Sarah Crunkhorn. Epilepsy: HSP90 inhibition suppresses seizures.
Nature reviews. Drug discovery.
2017 Feb; 16(2):88. doi:
10.1038/nrd.2017.9. [PMID: 28148937] - Mariangela Centrone, Marianna Ranieri, Annarita Di Mise, Sante Princiero Berlingerio, Annamaria Russo, Peter M T Deen, Olivier Staub, Giovanna Valenti, Grazia Tamma. AQP2 Abundance is Regulated by the E3-Ligase CHIP Via HSP70.
Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology.
2017; 44(2):515-531. doi:
10.1159/000485088. [PMID: 29145196] - Guangjin Ding, Peilin Chen, Hui Zhang, Xiaojie Huang, Yi Zang, Jiwen Li, Jia Li, Jiemin Wong. Regulation of Ubiquitin-like with Plant Homeodomain and RING Finger Domain 1 (UHRF1) Protein Stability by Heat Shock Protein 90 Chaperone Machinery.
The Journal of biological chemistry.
2016 09; 291(38):20125-35. doi:
10.1074/jbc.m116.727214. [PMID: 27489107] - Guo-Kun Wang, Song-Hua Li, Zhi-Min Zhao, Su-Xuan Liu, Guan-Xin Zhang, Fan Yang, Yang Wang, Feng Wu, Xian-Xian Zhao, Zhi-Yun Xu. Inhibition of heat shock protein 90 improves pulmonary arteriole remodeling in pulmonary arterial hypertension.
Oncotarget.
2016 Aug; 7(34):54263-54273. doi:
10.18632/oncotarget.10855. [PMID: 27472464] - Pheroze Joshi, Ekaterina Maidji, Cheryl A Stoddart. Inhibition of Heat Shock Protein 90 Prevents HIV Rebound.
The Journal of biological chemistry.
2016 May; 291(19):10332-46. doi:
10.1074/jbc.m116.717538. [PMID: 26957545] - Paul A Johnston, Minh M Nguyen, Javid A Dar, Junkui Ai, Yujuan Wang, Khalid Z Masoodi, Tongying Shun, Sunita Shinde, Daniel P Camarco, Yun Hua, Donna M Huryn, Gabriela Mustata Wilson, John S Lazo, Joel B Nelson, Peter Wipf, Zhou Wang. Development and Implementation of a High-Throughput High-Content Screening Assay to Identify Inhibitors of Androgen Receptor Nuclear Localization in Castration-Resistant Prostate Cancer Cells.
Assay and drug development technologies.
2016 05; 14(4):226-39. doi:
10.1089/adt.2016.716. [PMID: 27187604] - Min Chul Park, Hyobin Jeong, Sung Hwa Son, YounHa Kim, Daeyoung Han, Peter C Goughnour, Taehee Kang, Nam Hoon Kwon, Hyo Eun Moon, Sun Ha Paek, Daehee Hwang, Ho Jun Seol, Do-Hyun Nam, Sunghoon Kim. Novel Morphologic and Genetic Analysis of Cancer Cells in a 3D Microenvironment Identifies STAT3 as a Regulator of Tumor Permeability Barrier Function.
Cancer research.
2016 Mar; 76(5):1044-54. doi:
10.1158/0008-5472.can-14-2611. [PMID: 26676754] - Zhiyong Wang, Jinhua Wang, Songling Yang, Shuying Hou. Construction and in vitro/in vivo evaluation of 17-allylamino-17-demethoxygeldanamycin (17AAG)-loaded PEGylated nanostructured lipid carriers.
Drug development and industrial pharmacy.
2016 Jan; 42(1):91-98. doi:
10.3109/03639045.2015.1031138. [PMID: 25853294] - Katrina S Pedersen, George P Kim, Nathan R Foster, Andrea Wang-Gillam, Charles Erlichman, Robert R McWilliams. Phase II trial of gemcitabine and tanespimycin (17AAG) in metastatic pancreatic cancer: a Mayo Clinic Phase II Consortium study.
Investigational new drugs.
2015 Aug; 33(4):963-8. doi:
10.1007/s10637-015-0246-2. [PMID: 25952464] - Aya Sugiyama, Kazunori Kageyama, Shingo Murasawa, Noriko Ishigame, Kanako Niioka, Makoto Daimon. Inhibition of heat shock protein 90 decreases ACTH production and cell proliferation in AtT-20 cells.
Pituitary.
2015 Aug; 18(4):542-53. doi:
10.1007/s11102-014-0607-4. [PMID: 25280813] - Swetha Raman, Kaza Suguna. Functional characterization of heat-shock protein 90 from Oryza sativa and crystal structure of its N-terminal domain.
Acta crystallographica. Section F, Structural biology communications.
2015 Jun; 71(Pt 6):688-96. doi:
10.1107/s2053230x15006639. [PMID: 26057797] - Jing Li, Alfredo Csibi, Sun Yang, Gregory R Hoffman, Chenggang Li, Erik Zhang, Jane J Yu, John Blenis. Synthetic lethality of combined glutaminase and Hsp90 inhibition in mTORC1-driven tumor cells.
Proceedings of the National Academy of Sciences of the United States of America.
2015 Jan; 112(1):E21-9. doi:
10.1073/pnas.1417015112. [PMID: 25524627] - Anup Kasi Loknath Kumar, Christopher Dakhil, Megha Teeka Satyan, Nisreen Haideri. Extramedullary progression of multiple myeloma despite concomitant medullary response to multiple combination therapies and autologous transplant: a case report.
Journal of medical case reports.
2014 Sep; 8(?):299. doi:
10.1186/1752-1947-8-299. [PMID: 25200389] - Rubén E Varela-M, Cristina Mollinedo-Gajate, Antonio Muro, Faustino Mollinedo. The HSP90 inhibitor 17-AAG potentiates the antileishmanial activity of the ether lipid edelfosine.
Acta tropica.
2014 Mar; 131(?):32-6. doi:
10.1016/j.actatropica.2013.11.018. [PMID: 24299925] - Dan Zhou, Yuan Liu, Josephine Ye, Weiwen Ying, Luisa Shin Ogawa, Takayo Inoue, Noriaki Tatsuta, Yumiko Wada, Keizo Koya, Qin Huang, Richard C Bates, Andrew J Sonderfan. A rat retinal damage model predicts for potential clinical visual disturbances induced by Hsp90 inhibitors.
Toxicology and applied pharmacology.
2013 Dec; 273(2):401-9. doi:
10.1016/j.taap.2013.09.018. [PMID: 24090817] - Naohiro Nomura, Kazusaku Kamiya, Katsuhisa Ikeda, Naofumi Yui, Motoko Chiga, Eisei Sohara, Tatemitu Rai, Sei Sakaki, Shinich Uchida. Treatment with 17-allylamino-17-demethoxygeldanamycin ameliorated symptoms of Bartter syndrome type IV caused by mutated Bsnd in mice.
Biochemical and biophysical research communications.
2013 Nov; 441(3):544-9. doi:
10.1016/j.bbrc.2013.10.129. [PMID: 24189473] - M W Saif, C Erlichman, T Dragovich, D Mendelson, D Toft, F Burrows, C Storgard, D Von Hoff. Open-label, dose-escalation, safety, pharmacokinetic, and pharmacodynamic study of intravenously administered CNF1010 (17-(allylamino)-17-demethoxygeldanamycin [17-AAG]) in patients with solid tumors.
Cancer chemotherapy and pharmacology.
2013 May; 71(5):1345-55. doi:
10.1007/s00280-013-2134-9. [PMID: 23564374] - Tram Thu Vuong, Christian Berger, Vibeke Bertelsen, Marianne Skeie Rødland, Espen Stang, Inger Helene Madshus. Preubiquitinated chimeric ErbB2 is constitutively endocytosed and subsequently degraded in lysosomes.
Experimental cell research.
2013 Feb; 319(3):32-45. doi:
10.1016/j.yexcr.2012.10.010. [PMID: 23127513] - Takashi Kasukabe, Junko Okabe-Kado, Yu Haranosono, Nobuo Kato, Yoshio Honma. Inhibition of rapamycin-induced Akt phosphorylation by cotylenin A correlates with their synergistic growth inhibition of cancer cells.
International journal of oncology.
2013 Feb; 42(2):767-75. doi:
10.3892/ijo.2012.1745. [PMID: 23255002] - Chi Keung Lam, Wen Zhao, Wenfeng Cai, Elizabeth Vafiadaki, Stela M Florea, Xiaoping Ren, Yong Liu, Nathan Robbins, Zhiguo Zhang, Xiaoyang Zhou, Min Jiang, Jack Rubinstein, W Keith Jones, Evangelia G Kranias. Novel role of HAX-1 in ischemic injury protection involvement of heat shock protein 90.
Circulation research.
2013 Jan; 112(1):79-89. doi:
10.1161/circresaha.112.279935. [PMID: 22982986] - Alessio Giubellino, Carole Sourbier, Min-Jung Lee, Brad Scroggins, Petra Bullova, Michael Landau, Weiwen Ying, Len Neckers, Jane B Trepel, Karel Pacak. Targeting heat shock protein 90 for the treatment of malignant pheochromocytoma.
PloS one.
2013; 8(2):e56083. doi:
10.1371/journal.pone.0056083. [PMID: 23457505] - Keng Wu, Wenming Xu, Qiong You, Runmin Guo, Jianqiang Feng, Changran Zhang, Wen Wu. Increased expression of heat shock protein 90 under chemical hypoxic conditions protects cardiomyocytes against injury induced by serum and glucose deprivation.
International journal of molecular medicine.
2012 Nov; 30(5):1138-44. doi:
10.3892/ijmm.2012.1099. [PMID: 22922826] - Hyunjin Noh, Hyun J Kim, Mi R Yu, Wan-Young Kim, Jin Kim, Jung H Ryu, Soon H Kwon, Jin S Jeon, Dong C Han, Fuad Ziyadeh. Heat shock protein 90 inhibitor attenuates renal fibrosis through degradation of transforming growth factor-β type II receptor.
Laboratory investigation; a journal of technical methods and pathology.
2012 Nov; 92(11):1583-96. doi:
10.1038/labinvest.2012.127. [PMID: 22964853] - Ho-Chul Shin, Hyunah Cho, Tsz Chung Lai, Kevin R Kozak, Jill M Kolesar, Glen S Kwon. Pharmacokinetic study of 3-in-1 poly(ethylene glycol)-block-poly(D, L-lactic acid) micelles carrying paclitaxel, 17-allylamino-17-demethoxygeldanamycin, and rapamycin.
Journal of controlled release : official journal of the Controlled Release Society.
2012 Oct; 163(1):93-9. doi:
10.1016/j.jconrel.2012.04.024. [PMID: 22549011] - Takeshi Shimamura, Samanthi A Perera, Kevin P Foley, Jim Sang, Scott J Rodig, Takayo Inoue, Liang Chen, Danan Li, Julian Carretero, Yu-Chen Li, Papiya Sinha, Christopher D Carey, Christa L Borgman, John-Paul Jimenez, Matthew Meyerson, Weiwen Ying, James Barsoum, Kwok-Kin Wong, Geoffrey I Shapiro. Ganetespib (STA-9090), a nongeldanamycin HSP90 inhibitor, has potent antitumor activity in in vitro and in vivo models of non-small cell lung cancer.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2012 Sep; 18(18):4973-85. doi:
10.1158/1078-0432.ccr-11-2967. [PMID: 22806877] - Kanghyun Lee, Tae-Joon Hong, Ji-Sook Hahn. Roles of 17-AAG-induced molecular chaperones and Rma1 E3 ubiquitin ligase in folding and degradation of Pendrin.
FEBS letters.
2012 Jul; 586(16):2535-41. doi:
10.1016/j.febslet.2012.06.023. [PMID: 22750442] - Akinori Sato, Takako Asano, Keiichi Ito, Tomohiko Asano. 17-Allylamino-17-demethoxygeldanamycin and ritonavir inhibit renal cancer growth by inhibiting the expression of heat shock factor-1.
International journal of oncology.
2012 Jul; 41(1):46-52. doi:
10.3892/ijo.2012.1419. [PMID: 22470109] - Sabrina Manni, Alessandra Brancalion, Laura Quotti Tubi, Anna Colpo, Laura Pavan, Anna Cabrelle, Elisa Ave, Fortunato Zaffino, Giovanni Di Maira, Maria Ruzzene, Fausto Adami, Renato Zambello, Maria Rita Pitari, Pierfrancesco Tassone, Lorenzo A Pinna, Carmela Gurrieri, Gianpietro Semenzato, Francesco Piazza. Protein kinase CK2 protects multiple myeloma cells from ER stress-induced apoptosis and from the cytotoxic effect of HSP90 inhibition through regulation of the unfolded protein response.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2012 Apr; 18(7):1888-900. doi:
10.1158/1078-0432.ccr-11-1789. [PMID: 22351691] - Ying Wen Huang, Chung Chi Hu, Ming Ru Liou, Ban Yang Chang, Ching Hsiu Tsai, Menghsiao Meng, Na Sheng Lin, Yau Heiu Hsu. Hsp90 interacts specifically with viral RNA and differentially regulates replication initiation of Bamboo mosaic virus and associated satellite RNA.
PLoS pathogens.
2012; 8(5):e1002726. doi:
10.1371/journal.ppat.1002726. [PMID: 22654666] - Francois Lamoureux, Christian Thomas, Min-Jean Yin, Hidetoshi Kuruma, Ladan Fazli, Martin E Gleave, Amina Zoubeidi. A novel HSP90 inhibitor delays castrate-resistant prostate cancer without altering serum PSA levels and inhibits osteoclastogenesis.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2011 Apr; 17(8):2301-13. doi:
10.1158/1078-0432.ccr-10-3077. [PMID: 21349995] - Qian Xie, Robert Wondergem, Yuehai Shen, Greg Cavey, Jiyuan Ke, Ryan Thompson, Robert Bradley, Jennifer Daugherty-Holtrop, Jennifer Daughtery-Holtrop, Yong Xu, Edwin Chen, Hanan Omar, Neal Rosen, David Wenkert, H Eric Xu, George F Vande Woude. Benzoquinone ansamycin 17AAG binds to mitochondrial voltage-dependent anion channel and inhibits cell invasion.
Proceedings of the National Academy of Sciences of the United States of America.
2011 Mar; 108(10):4105-10. doi:
10.1073/pnas.1015181108. [PMID: 21368131] - Margaret A Park, Hossein A Hamed, Clint Mitchell, Nichola Cruickshanks, Rupesh Dash, Jeremy Allegood, Igor P Dmitriev, Gary Tye, Besim Ogretmen, Sarah Spiegel, Adly Yacoub, Steven Grant, David T Curiel, Paul B Fisher, Paul Dent. A serotype 5/3 adenovirus expressing MDA-7/IL-24 infects renal carcinoma cells and promotes toxicity of agents that increase ROS and ceramide levels.
Molecular pharmacology.
2011 Mar; 79(3):368-80. doi:
10.1124/mol.110.069484. [PMID: 21119025] - Yanyan Li, Tao Zhang, Steven J Schwartz, Duxin Sun. Sulforaphane potentiates the efficacy of 17-allylamino 17-demethoxygeldanamycin against pancreatic cancer through enhanced abrogation of Hsp90 chaperone function.
Nutrition and cancer.
2011; 63(7):1151-9. doi:
10.1080/01635581.2011.596645. [PMID: 21875325] - Bonnie Tillotson, Kelly Slocum, John Coco, Nigel Whitebread, Brian Thomas, Kip A West, John MacDougall, Jie Ge, Janid A Ali, Vito J Palombella, Emmanuel Normant, Julian Adams, Christian C Fritz. Hsp90 (heat shock protein 90) inhibitor occupancy is a direct determinant of client protein degradation and tumor growth arrest in vivo.
The Journal of biological chemistry.
2010 Dec; 285(51):39835-43. doi:
10.1074/jbc.m110.141580. [PMID: 20940293] - Nourdine Faresse, Dorothée Ruffieux-Daidie, Mélanie Salamin, Celso E Gomez-Sanchez, Olivier Staub. Mineralocorticoid receptor degradation is promoted by Hsp90 inhibition and the ubiquitin-protein ligase CHIP.
American journal of physiology. Renal physiology.
2010 Dec; 299(6):F1462-72. doi:
10.1152/ajprenal.00285.2010. [PMID: 20861078] - Paul G Richardson, Asher A Chanan-Khan, Melissa Alsina, Maher Albitar, David Berman, Marianne Messina, Constantine S Mitsiades, Kenneth C Anderson. Tanespimycin monotherapy in relapsed multiple myeloma: results of a phase 1 dose-escalation study.
British journal of haematology.
2010 Aug; 150(4):438-45. doi:
10.1111/j.1365-2141.2010.08265.x. [PMID: 20618337] - Paul G Richardson, Ashraf Z Badros, Sundar Jagannath, Stefano Tarantolo, Jeffrey L Wolf, Maher Albitar, David Berman, Marianne Messina, Kenneth C Anderson. Tanespimycin with bortezomib: activity in relapsed/refractory patients with multiple myeloma.
British journal of haematology.
2010 Aug; 150(4):428-37. doi:
10.1111/j.1365-2141.2010.08264.x. [PMID: 20618338] - Ulka N Vaishampayan, Angelika M Burger, Edward A Sausville, Lance K Heilbrun, Jing Li, M Naomi Horiba, Merrill J Egorin, Percy Ivy, Simon Pacey, Patricia M Lorusso. Safety, efficacy, pharmacokinetics, and pharmacodynamics of the combination of sorafenib and tanespimycin.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2010 Jul; 16(14):3795-804. doi:
10.1158/1078-0432.ccr-10-0503. [PMID: 20525756] - Mounia Beloueche-Babari, Vaitha Arunan, L Elizabeth Jackson, Nina Perusinghe, Swee Y Sharp, Paul Workman, Martin O Leach. Modulation of melanoma cell phospholipid metabolism in response to heat shock protein 90 inhibition.
Oncotarget.
2010 Jul; 1(3):185-97. doi:
10.18632/oncotarget.125. [PMID: 21037799] - Julio Madrigal-Matute, Oscar López-Franco, Luis Miguel Blanco-Colio, Begoña Muñoz-García, Priscila Ramos-Mozo, Luis Ortega, Jesus Egido, Jose Luis Martín-Ventura. Heat shock protein 90 inhibitors attenuate inflammatory responses in atherosclerosis.
Cardiovascular research.
2010 May; 86(2):330-7. doi:
10.1093/cvr/cvq046. [PMID: 20154064] - Jeffrey J Lin, Charles S Hemenway. Hsp90 directly modulates the spatial distribution of AF9/MLLT3 and affects target gene expression.
The Journal of biological chemistry.
2010 Apr; 285(16):11966-73. doi:
10.1074/jbc.m110.101642. [PMID: 20159978] - Fabiola Cervantes-Gomez, Ramadevi Nimmanapalli, Varsha Gandhi. Transcription inhibition of heat shock proteins: a strategy for combination of 17-allylamino-17-demethoxygeldanamycin and actinomycin d.
Cancer research.
2009 May; 69(9):3947-54. doi:
10.1158/0008-5472.can-08-4406. [PMID: 19383903] - May P Xiong, Jaime A Yáñez, Glen S Kwon, Neal M Davies, M Laird Forrest. A cremophor-free formulation for tanespimycin (17-AAG) using PEO-b-PDLLA micelles: characterization and pharmacokinetics in rats.
Journal of pharmaceutical sciences.
2009 Apr; 98(4):1577-86. doi:
10.1002/jps.21509. [PMID: 18752263] - David B Solit, Iman Osman, David Polsky, Katherine S Panageas, Adil Daud, James S Goydos, Jerrold Teitcher, Jedd D Wolchok, F Joseph Germino, Susan E Krown, Daniel Coit, Neal Rosen, Paul B Chapman. Phase II trial of 17-allylamino-17-demethoxygeldanamycin in patients with metastatic melanoma.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2008 Dec; 14(24):8302-7. doi:
10.1158/1078-0432.ccr-08-1002. [PMID: 19088048] - Wenchang Guo, David Siegel, David Ross. Stability of the Hsp90 inhibitor 17AAG hydroquinone and prevention of metal-catalyzed oxidation.
Journal of pharmaceutical sciences.
2008 Dec; 97(12):5147-57. doi:
10.1002/jps.21394. [PMID: 18393300] - Itai Pashtan, Shinji Tsutsumi, Suiquan Wang, Wanping Xu, Len Neckers. Targeting Hsp90 prevents escape of breast cancer cells from tyrosine kinase inhibition.
Cell cycle (Georgetown, Tex.).
2008 Sep; 7(18):2936-41. doi:
10.4161/cc.7.18.6701. [PMID: 18769157] - Margaret A Park, Guo Zhang, Clint Mitchell, Mohamed Rahmani, Hossein Hamed, Michael P Hagan, Adly Yacoub, David T Curiel, Paul B Fisher, Steven Grant, Paul Dent. Mitogen-activated protein kinase kinase 1/2 inhibitors and 17-allylamino-17-demethoxygeldanamycin synergize to kill human gastrointestinal tumor cells in vitro via suppression of c-FLIP-s levels and activation of CD95.
Molecular cancer therapeutics.
2008 Sep; 7(9):2633-48. doi:
10.1158/1535-7163.mct-08-0400. [PMID: 18790746] - Jeffrey S Johnston, Mitch A Phelps, Kristie A Blum, William Blum, Michael R Grever, Katherine L Farley, James T Dalton. Development and validation of a rapid and sensitive high-performance liquid chromatography-mass spectroscopy assay for determination of 17-(allylamino)-17-demethoxygeldanamycin and 17-(amino)-17-demethoxygeldanamycin in human plasma.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2008 Aug; 871(1):15-21. doi:
10.1016/j.jchromb.2008.06.029. [PMID: 18635408] - Ewen M Harrison, Eva Sharpe, Christopher O Bellamy, Stephen J McNally, Luke Devey, O James Garden, James A Ross, Stephen J Wigmore. Heat shock protein 90-binding agents protect renal cells from oxidative stress and reduce kidney ischemia-reperfusion injury.
American journal of physiology. Renal physiology.
2008 Aug; 295(2):F397-405. doi:
10.1152/ajprenal.00361.2007. [PMID: 18562631] - M A Shammas, H Koley, R C Bertheau, P Neri, M Fulciniti, P Tassone, S Blotta, A Protopopov, C Mitsiades, R B Batchu, K C Anderson, A Chin, S Gryaznov, N C Munshi. Telomerase inhibitor GRN163L inhibits myeloma cell growth in vitro and in vivo.
Leukemia.
2008 Jul; 22(7):1410-8. doi:
10.1038/leu.2008.81. [PMID: 18449204] - Jon Patterson, Vito J Palombella, Christian Fritz, Emmanuel Normant. IPI-504, a novel and soluble HSP-90 inhibitor, blocks the unfolded protein response in multiple myeloma cells.
Cancer chemotherapy and pharmacology.
2008 May; 61(6):923-32. doi:
10.1007/s00280-007-0546-0. [PMID: 17624530] - Chen Daozhen, Liu Lu, Yang Min, Jiang Xinyu, Huang Ying. Synthesis of (131)I-labeled-[(131)I]iodo-17-allylamino-17-demethoxy geldanamycin ([(131)I]iodo-17-AAG) and its biodistribution in mice.
Cancer biotherapy & radiopharmaceuticals.
2007 Oct; 22(5):607-12. doi:
10.1089/cbr.2006.363. [PMID: 17979563] - Anuran Chatterjee, Christiana Dimitropoulou, Fotios Drakopanayiotakis, Galina Antonova, Connie Snead, Joseph Cannon, Richard C Venema, John D Catravas. Heat shock protein 90 inhibitors prolong survival, attenuate inflammation, and reduce lung injury in murine sepsis.
American journal of respiratory and critical care medicine.
2007 Oct; 176(7):667-75. doi:
10.1164/rccm.200702-291oc. [PMID: 17615388] - Evdoxia Hatjiharissi, Hai Ngo, Alexey A Leontovich, Xavier Leleu, Michael Timm, Mona Melhem, Diane George, Ganwei Lu, Joanna Ghobrial, Yazan Alsayed, Steven Zeismer, Miguel Cabanela, Alex Nehme, Xiaoying Jia, Anne Sophie Moreau, Steven P Treon, Rafael Fonseca, Morie A Gertz, Kenneth C Anderson, Thomas E Witzig, Irene M Ghobrial. Proteomic analysis of waldenstrom macroglobulinemia.
Cancer research.
2007 Apr; 67(8):3777-84. doi:
10.1158/0008-5472.can-06-3089. [PMID: 17440091] - Julie L Eiseman, Jianxia Guo, Ramesh K Ramanathan, Chandra P Belani, David B Solit, Howard I Scher, S Percy Ivy, Eleanor G Zuhowski, Merrill J Egorin. Evaluation of plasma insulin-like growth factor binding protein 2 and Her-2 extracellular domain as biomarkers for 17-allylamino-17-demethoxygeldanamycin treatment of adult patients with advanced solid tumors.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2007 Apr; 13(7):2121-7. doi:
10.1158/1078-0432.ccr-06-2286. [PMID: 17404095] - David B Solit, S Percy Ivy, Catherine Kopil, Rachel Sikorski, Michael J Morris, Susan F Slovin, W Kevin Kelly, Anthony DeLaCruz, Tracy Curley, Glenn Heller, Steven Larson, Lawrence Schwartz, Merrill J Egorin, Neal Rosen, Howard I Scher. Phase I trial of 17-allylamino-17-demethoxygeldanamycin in patients with advanced cancer.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2007 Mar; 13(6):1775-82. doi:
10.1158/1078-0432.ccr-06-1863. [PMID: 17363532] - Brenda J Weigel, Susan M Blaney, Joel M Reid, Stephanie L Safgren, Rochelle Bagatell, John Kersey, Joseph P Neglia, S Percy Ivy, Ashish M Ingle, Luke Whitesell, Richard J Gilbertson, Mark Krailo, Matthew Ames, Peter C Adamson. A phase I study of 17-allylaminogeldanamycin in relapsed/refractory pediatric patients with solid tumors: a Children's Oncology Group study.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2007 Mar; 13(6):1789-93. doi:
10.1158/1078-0432.ccr-06-2270. [PMID: 17363534] - Jens R Sydor, Emmanuel Normant, Christine S Pien, James R Porter, Jie Ge, Louis Grenier, Roger H Pak, Janid A Ali, Marlene S Dembski, Jebecka Hudak, Jon Patterson, Courtney Penders, Melissa Pink, Margaret A Read, Jim Sang, Caroline Woodward, Yilong Zhang, David S Grayzel, Jim Wright, John A Barrett, Vito J Palombella, Julian Adams, Jeffrey K Tong. Development of 17-allylamino-17-demethoxygeldanamycin hydroquinone hydrochloride (IPI-504), an anti-cancer agent directed against Hsp90.
Proceedings of the National Academy of Sciences of the United States of America.
2006 Nov; 103(46):17408-13. doi:
10.1073/pnas.0608372103. [PMID: 17090671] - Ellen A Ronnen, G Varuni Kondagunta, Nicole Ishill, Suzanne M Sweeney, John K Deluca, Lawrence Schwartz, Jennifer Bacik, Robert J Motzer. A phase II trial of 17-(Allylamino)-17-demethoxygeldanamycin in patients with papillary and clear cell renal cell carcinoma.
Investigational new drugs.
2006 Nov; 24(6):543-6. doi:
10.1007/s10637-006-9208-z. [PMID: 16832603] - Rossella Elisei, Agnese Vivaldi, Raffaele Ciampi, Pinuccia Faviana, Fulvio Basolo, Ferruccio Santini, Claudio Traino, Furio Pacini, Aldo Pinchera. Treatment with drugs able to reduce iodine efflux significantly increases the intracellular retention time in thyroid cancer cells stably transfected with sodium iodide symporter complementary deoxyribonucleic acid.
The Journal of clinical endocrinology and metabolism.
2006 Jun; 91(6):2389-95. doi:
10.1210/jc.2005-2480. [PMID: 16537683] - Jefferson Terry, Joanna M Lubieniecka, Wanda Kwan, Suzanne Liu, Torsten O Nielsen. Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin prevents synovial sarcoma proliferation via apoptosis in in vitro models.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2005 Aug; 11(15):5631-8. doi:
10.1158/1078-0432.ccr-05-0398. [PMID: 16061882] - Udai Banerji, Anne O'Donnell, Michelle Scurr, Simon Pacey, Sarah Stapleton, Yasmin Asad, Laura Simmons, Alison Maloney, Florence Raynaud, Maeli Campbell, Michael Walton, Sunil Lakhani, Stanley Kaye, Paul Workman, Ian Judson. Phase I pharmacokinetic and pharmacodynamic study of 17-allylamino, 17-demethoxygeldanamycin in patients with advanced malignancies.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
2005 Jun; 23(18):4152-61. doi:
10.1200/jco.2005.00.612. [PMID: 15961763] - Ramesh K Ramanathan, Donald L Trump, Julie L Eiseman, Chandra P Belani, Sanjiv S Agarwala, Eleanor G Zuhowski, Jing Lan, Douglas M Potter, S Percy Ivy, Sakkaraiappan Ramalingam, Adam M Brufsky, Michael K K Wong, Susan Tutchko, Merrill J Egorin. Phase I pharmacokinetic-pharmacodynamic study of 17-(allylamino)-17-demethoxygeldanamycin (17AAG, NSC 330507), a novel inhibitor of heat shock protein 90, in patients with refractory advanced cancers.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2005 May; 11(9):3385-91. doi:
10.1158/1078-0432.ccr-04-2322. [PMID: 15867239] - Jean L Grem, Geraldine Morrison, Xiao-Du Guo, Elizabeth Agnew, Chris H Takimoto, Rebecca Thomas, Eva Szabo, Louise Grochow, Frank Grollman, J Michael Hamilton, Len Neckers, Richard H Wilson. Phase I and pharmacologic study of 17-(allylamino)-17-demethoxygeldanamycin in adult patients with solid tumors.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
2005 Mar; 23(9):1885-93. doi:
10.1200/jco.2005.12.085. [PMID: 15774780] - Xueyu Chen, Robert R Bies, Ramesh K Ramanathan, Eleanor G Zuhowski, Donald L Trump, Merrill J Egorin. Population pharmacokinetic analysis of 17-(allylamino)-17-demethoxygeldanamycin (17AAG) in adult patients with advanced malignancies.
Cancer chemotherapy and pharmacology.
2005 Mar; 55(3):237-43. doi:
10.1007/s00280-004-0836-8. [PMID: 15503027] - Steven M Musser, Merrill J Egorin, Eleanor G Zuhowski, Deborah R Hamburger, Robert A Parise, Joseph M Covey, Kevin D White, Julie L Eiseman. Biliary excretion of 17-(allylamino)-17-demethoxygeldanamycin (NSC 330507) and metabolites by Fischer 344 rats.
Cancer chemotherapy and pharmacology.
2003 Aug; 52(2):139-46. doi:
10.1007/s00280-003-0630-z. [PMID: 12761648] - Lu Xu, Julie L Eiseman, Merrill J Egorin, David Z D'Argenio. Physiologically-based pharmacokinetics and molecular pharmacodynamics of 17-(allylamino)-17-demethoxygeldanamycin and its active metabolite in tumor-bearing mice.
Journal of pharmacokinetics and pharmacodynamics.
2003 Jun; 30(3):185-219. doi:
10.1023/a:1025542026488. [PMID: 14571691] - E B Agnew, R H Wilson, J L Grem, L Neckers, D Bi, C H Takimoto. Measurement of the novel antitumor agent 17-(allylamino)-17-demethoxygeldanamycin in human plasma by high-performance liquid chromatography.
Journal of chromatography. B, Biomedical sciences and applications.
2001 May; 755(1-2):237-43. doi:
10.1016/s0378-4347(01)00113-x. [PMID: 11393709] - P N Münster, M Srethapakdi, M M Moasser, N Rosen. Inhibition of heat shock protein 90 function by ansamycins causes the morphological and functional differentiation of breast cancer cells.
Cancer research.
2001 Apr; 61(7):2945-52. doi:
". [PMID: 11306472] - M J Egorin, E G Zuhowski, D M Rosen, D L Sentz, J M Covey, J L Eiseman. Plasma pharmacokinetics and tissue distribution of 17-(allylamino)-17-demethoxygeldanamycin (NSC 330507) in CD2F1 mice1.
Cancer chemotherapy and pharmacology.
2001 Apr; 47(4):291-302. doi:
10.1007/s002800000242. [PMID: 11345645] - M J Egorin, D M Rosen, J H Wolff, P S Callery, S M Musser, J L Eiseman. Metabolism of 17-(allylamino)-17-demethoxygeldanamycin (NSC 330507) by murine and human hepatic preparations.
Cancer research.
1998 Jun; 58(11):2385-96. doi:
. [PMID: 9622079]