نتایج جستجو برای: h71

تعداد نتایج: 132  

2010
Saad Z Usmani Robert D Bona Gabriela Chiosis Zihai Li

BACKGROUND Heat shock protein 90 (HSP90) inhibitors have emerged as a promising class of anti-cancer drugs in both solid and hematologic malignancies. The HSP90 family includes the cytosolic HSP90 (HSP90AA1), the ER paralogue gp96 (HSP90B1) and the mitochondrial member TRAP1 (HSP90L). We evaluated the in vitro anti-tumor activity and mechanism of action of PU-H71, a novel purine scaffold HSP90 ...

2016
Huizi Keiko Li Yoshitaka Matsumoto Yoshiya Furusawa Tadashi Kamada

PU-H71, a heat shock protein 90 (Hsp90) inhibitor, has yielded therapeutic efficacy in many preclinical models and is currently in clinical trials. Carbon-ion radiotherapy (CIRT) has provided successful tumor control; however, there is still room for improvement, particularly in terms of tumor-specific radiosensitization. The Hsp90 inhibitor PU-H71 has been shown to sensitize tumor cells to X-r...

Journal: :The Journal of clinical investigation 2010
Sachie Marubayashi Priya Koppikar Tony Taldone Omar Abdel-Wahab Nathan West Neha Bhagwat Eloisi Caldas-Lopes Kenneth N Ross Mithat Gönen Alex Gozman James H Ahn Anna Rodina Ouathek Ouerfelli Guangbin Yang Cyrus Hedvat James E Bradner Gabriela Chiosis Ross L Levine

JAK2 kinase inhibitors were developed for the treatment of myeloproliferative neoplasms (MPNs), following the discovery of activating JAK2 mutations in the majority of patients with MPN. However, to date JAK2 inhibitor treatment has shown limited efficacy and apparent toxicities in clinical trials. We report here that an HSP90 inhibitor, PU-H71, demonstrated efficacy in cell line and mouse mode...

2017
Kelly G. Bryant Young Chan Chae Rogelio L. Martinez John C. Gordon Khaled M. Elokely Andrew V. Kossenkov Steven Grant Wayne E. Childers Magid Abou-Gharbia Dario C. Altieri

Reprogramming of mitochondrial functions sustains tumor growth and may provide therapeutic opportunities. Here, we targeted the protein folding environment in mitochondria by coupling a purine-based inhibitor of the molecular chaperone Heat Shock Protein-90 (Hsp90), PU-H71 to the mitochondrial-targeting moiety, triphenylphosphonium (TPP). Binding of PU-H71-TPP to ADP-Hsp90, Hsp90 co-chaperone c...

2017
Arefeh Rouhi Christina Miller Sarah Grasedieck Stefanie Reinhart Britta Stolze Hartmut Döhner Florian Kuchenbauer Lars Bullinger Stefan Fröhling Claudia Scholl

Inhibition of the HSP90 chaperone results in depletion of many signaling proteins that drive tumorigenesis, such as downstream effectors of KRAS, the most commonly mutated human oncogene. As a consequence, several small-molecule HSP90 inhibitors are being evaluated in clinical trials as anticancer agents. To prospectively identify mechanisms through which HSP90-dependent cancer cells evade phar...

Journal: :Proceedings of the National Academy of Sciences of the United States of America 2009
Eloisi Caldas-Lopes Leandro Cerchietti James H Ahn Cristina C Clement Ana I Robles Anna Rodina Kamalika Moulick Tony Taldone Alexander Gozman Yunke Guo Nian Wu Elisa de Stanchina Julie White Steven S Gross Yuliang Ma Lyuba Varticovski Ari Melnick Gabriela Chiosis

Triple-negative breast cancers (TNBCs) are defined by a lack of expression of estrogen, progesterone, and HER2 receptors. Because of the absence of identified targets and targeted therapies, and due to a heterogeneous molecular presentation, treatment guidelines for patients with TNBC include only conventional chemotherapy. Such treatment, while effective for some, leaves others with high rates...

Journal: :Cancer research 1985
F J Hendler D Yuan

Three monoclonal antibodies--H59, H71, and H72--which react with human breast cancers have been developed using the estrogen-dependent human breast cancer cell line, ZR-75-1, as the immunogen. H59 bound only to estrogen receptor-positive, estrogen-regulated breast cancer cells in culture, whereas H71 and H72 bound breast cancer cells irrespective of the estrogen receptor content. All three anti...

2013
Dea Shahinas Asongna Folefoc Tony Taldone Gabriela Chiosis Ian Crandall Dylan R. Pillai

BACKGROUND Drug resistance, absence of an effective vaccine, and inadequate public health measures are major impediments to controlling Plasmodium falciparum malaria worldwide. The development of antimalarials to which resistance is less likely is paramount. To this end, we have exploited the chaperone function of P. falciparum Hsp90 (PfHsp90) that serves to facilitate the expression of resista...

Journal: :The Journal of clinical investigation 2015
Rebecca L Goldstein Shao Ning Yang Tony Taldone Betty Chang John Gerecitano Kojo Elenitoba-Johnson Rita Shaknovich Wayne Tam John P Leonard Gabriela Chiosis Leandro Cerchietti Ari Melnick

Rationally designed combinations of targeted therapies for refractory cancers, such as activated B cell-like diffuse large B cell lymphoma (ABC DLBCL), are likely required to achieve potent, durable responses. Here, we used a pharmacoproteomics approach to map the interactome of a tumor-enriched isoform of HSP90 (teHSP90). Specifically, we chemically precipitated teHSP90-client complexes from D...

Journal: :Neuro-oncology 2022

Abstract Diffuse intrinsic pontine glioma (DIPG) is an aggressive pediatric brain tumor. The mean age of onset 7-9 years with a median survival 9 months following diagnosis. Histone 3 (H3) mutations (H3K27M) have been identified in approximately 80% patients, representing intriguing target, but how to do this unclear. To address this, we performed synthetic lethality drug screen over 2400 compo...

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