نتایج جستجو برای: r58 j30 h71
تعداد نتایج: 354 فیلتر نتایج به سال:
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...
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...
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...
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...
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...
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...
Article history: Received 24 February 2010 Available online 5 March 2012 JEL classification: C73 D82 L14 J30
Article history: Received 17 February 2014 Received in revised form 7 May 2014 Accepted 7 May 2014 Available online xxxx JEL classification: A13 C23 J30
BACKGROUND The positron-emitting radionuclide (89)Zr (t(1/2) = 3.17 days) was used to prepare (89)Zr-radiolabeled trastuzumab for use as a radiotracer for characterizing HER2/neu-positive breast tumors. In addition, pharmacodynamic studies on HER2/neu expression levels in response to therapeutic doses of PU-H71 (a specific inhibitor of heat-shock protein 90 [Hsp90]) were conducted. METHODOLOG...
Crystallization and preliminary X-ray diffraction analysis of Trap1 complexed with Hsp90 inhibitors.
Hsp90 is a molecular chaperone responsible for the assembly and regulation of many cellular client proteins. In particular, Trap1, a mitochondrial Hsp90 homologue, plays a pivotal role in maintaining mitochondrial integrity, protecting against apoptosis in cancer cells. The N (N-terminal)-M (middle) domain of human Trap1 was crystallized in complex with Hsp90 inhibitors (PU-H71 and BIIB-021) by...
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