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  • Her2
  • Abnormal expression of HER2 protein is thought to result in excess growth stimulation, converting HER2 into an oncogene . (ganfyd.org)
  • HER2 can be blocked using a synthetic humanised monoclonal antibody called trastuzumab , although the mechanisms of action may be more complex than just receptor antagonism. (ganfyd.org)
  • The antibodies target the extracellular domain of the HER2 receptor. (perkinelmer.de)
  • HER2 can be shed from the cell surface as a soluble protein (sHER2) via proteolytic cleavage by an unidentified protease. (perkinelmer.de)
  • HSP90 enables the activation of many client proteins of which the most clinically validated is HER2. (aacrjournals.org)
  • In vitro , the combination induced greater decreases in HER2, a G 2 cell-cycle arrest, and increased apoptosis. (aacrjournals.org)
  • To investigate the functional impact of EGFR-HER2 heterodimers on migration of glial tumour cells, we stably transfected different HER2 constructs, including a constitutively active (HER2VE) and a dominant-negative (HER2VEKA) receptor, in the EGFR-overexpressing human glioma cell line LN18. (biologists.org)
  • These results were corroborated by inhibition of EGFR-HER2 signalling with tyrosine kinase inhibitors, because only the blocking of both receptors in HER2VE-cells with the bi-specific inhibitor AEE788 downregulated migration to levels comparable with those in HER2VEKA cells. (biologists.org)
  • As in many other cancer types, including breast and lung cancer, members of the EGF receptor family - particularly EGFR and HER2 - are also implicated in the tumorigenesis and tumour progression of glioblastomas. (biologists.org)
  • Because mutations in the androgen receptor (AR) and activation of HER2 and Akt may account, in part, for prostate cancer progression after castration or treatment with antiandrogens, we sought to determine whether an inhibitor of Hsp90 function could degrade these Hsp90 client proteins and inhibit the growth of prostate cancer xenografts with an acceptable therapeutic index. (aacrjournals.org)
  • HER2 a proto-oncogenic receptor tyrosine kinase of the EGFR family. (phosphosite.org)
  • HSP90
  • The molecular chaperone Hsp90 is one component of a highly complex and interactive cellular proteostasis network (PN) that participates in protein folding, directs misfolded and damaged proteins for destruction, and participates in regulating cellular transcriptional responses to environmental stress, thus promoting cell and organismal survival. (springer.com)
  • Ansamycin antibiotics, including 17allylamino-17-demethoxygeldanamycin (17-AAG), inhibit Hsp90 function and cause the selective degradation of signaling proteins that require this chaperone for folding. (aacrjournals.org)
  • The effect of 17-AAG on the expression of Hsp90 regulated signaling proteins in prostate cancer cells and xenografts was determined. (aacrjournals.org)
  • Occupancy of the Hsp90 pocket by GM causes the degradation of several signaling proteins important in mediating prostate cancer growth. (aacrjournals.org)
  • Molecular studies revealed the binding of GA to members of the heat shock protein 90 (Hsp90) family of molecular chaperones ( Whitesell et al 1994 ). (pubmedcentralcanada.ca)
  • Three concepts are of particular importance: (1) formation of free radicals, (2) assumed inhibition of tyrosine kinases, and (3) binding to and interference with the function of members of the Hsp90 family of proteins. (pubmedcentralcanada.ca)
  • 17-allyl-aminogeldanamycin (17-AAG) is an ansamycin antibiotic that binds to a highly conserved pocket in the Hsp90 chaperone protein and inhibits its function. (aacrjournals.org)
  • Hsp90 is required for the refolding of proteins during cellular stress and the conformational maturation of certain signaling proteins. (aacrjournals.org)
  • In cancer, this role has been attributed to heat shock protein 90 (Hsp90), a molecular chaperone that maintains the functional conformation of multiple proteins involved in cell-specific oncogenic processes. (biomedcentral.com)
  • In this review, we will present recent findings suggesting that heat shock protein 90 (Hsp90) may play a role in maintaining pathogenic changes that lead to neurodegenerative diseases. (biomedcentral.com)
  • Thus, following dysregulation in the abundance, stability or activity of a given protein, cell survival can become critically dependent on the association of client proteins of non-native stability with Hsp90. (biomedcentral.com)
  • Targets
  • The two tables below display ChEMBL single-protein targets which are predicted to interact with CHEMBL553. (ebi.ac.uk)
  • MA5-11367 targets Phospho-HER-2 pTyr1248 in IF, IHC, and WB applications and shows reactivity with Human and Rat samples. (thermofisher.com)
  • aberrant
  • These interactions buffer the local molecular instability and allow for the accumulation of aberrant proteins that ultimately leads to the blossoming of disease. (biomedcentral.com)
  • substrate
  • Buchner J, Grallert H, Jakob U (1998) Analysis of chaperone function using citrate synthase as nonnative substrate protein. (springer.com)
  • tumor
  • The bar plot below shows the proportion of tumor samples that have any kind of altering mutation(s) in the given protein. (phosphosite.org)
  • cancer
  • Before 2010, castration-resistant prostate cancer (CRPC) 2 patients had few treatment options, with the most effective standard chemotherapeutic regimens producing a 2-month improvement in median survival ( 2 , 3 ). (aaccjnls.org)
  • This aggressive form of breast cancer is characterised by the fact that the tumour cells produce the protein ErbB-2. (isciencetimes.com)
  • If ErbB-2 is detected in the tumour cells in the tissue sample taken routinely from all breast cancer patients, they must undergo special and complicated therapy. (isciencetimes.com)
  • For this reason we specifically looked for interaction between these two proteins in breast cancer cells. (isciencetimes.com)
  • To verify this, they switched off the Plexin-B1 in mice with ErbB-2-producing breast cancer. (isciencetimes.com)