• Thumbnail for Hsp90 inhibitor
    An Hsp90 inhibitor is a substance that inhibits that activity of the Hsp90 heat shock protein. Since Hsp90 stabilizes a variety of proteins required for...
    20 KB (2,756 words) - 11:53, 23 April 2024
  • Thumbnail for Hsp90
    example, the Hsp90 inhibitor geldanamycin has been used as an anti-tumor agent. The drug was originally thought to function as a kinase inhibitor but was subsequently...
    51 KB (5,551 words) - 04:57, 26 August 2024
  • Thumbnail for Heat shock protein 90kDa alpha (cytosolic), member A1
    that most amenable to inhibitor generation. To date, there are 23 active Hsp90 inhibitor oncology trials, and 13 HSP90 inhibitors are currently undergoing...
    65 KB (8,199 words) - 17:04, 1 August 2024
  • Thumbnail for Luminespib
    it is a resorcinylic isoxazole amide Luminespib is an inhibitor of heat shock protein 90 (Hsp90), which is a chaperone protein that plays a role in the...
    7 KB (484 words) - 00:26, 3 December 2023
  • Thumbnail for Tyrosine kinase inhibitor
    A tyrosine kinase inhibitor (TKI) is a pharmaceutical drug that inhibits tyrosine kinases. Tyrosine kinases are enzymes responsible for the activation...
    10 KB (1,179 words) - 18:31, 8 August 2024
  • Protein 90 (HSP90). HSP90 is key in protein folding and maturation. TopoTarget is currently looking for small molecule drugs that inhibit HSP90 function...
    29 KB (2,980 words) - 04:33, 13 May 2024
  • drugs. Hence small molecule inhibitors of HSPs, especially Hsp90 show promise as anticancer agents. The potent Hsp90 inhibitor 17-AAG was in clinical trials...
    49 KB (5,533 words) - 10:41, 19 July 2024
  • Fuhrmann-Stroissnigg H, Niedernhofer LJ, Robbins PD (2018-05-03). "Hsp90 inhibitors as senolytic drugs to extend healthy aging". Cell Cycle. 17 (9). Informa...
    26 KB (2,028 words) - 10:24, 8 June 2024
  • Thumbnail for FNIP1
    protein 1 (FNIP1) functions as a co-chaperone which inhibits the ATPase activity of the chaperone Hsp90 (heat shock protein-90) and decelerates its chaperone...
    6 KB (707 words) - 09:45, 17 October 2022
  • Thumbnail for Lutetium (177Lu) chloride
    Lundsten S, Spiegelberg D, Stenerlöw B, Nestor M (December 2019). "The HSP90 inhibitor onalespib potentiates 177Lu‑DOTATATE therapy in neuroendocrine tumor...
    11 KB (697 words) - 12:15, 6 August 2024
  • Thumbnail for Hsp70
    et al. (June 2018). "Targeted cancer therapy through 17-DMAG as an Hsp90 inhibitor: Overview and current state of the art". Biomedicine & Pharmacotherapy...
    50 KB (5,687 words) - 16:06, 10 July 2024
  • GM, Lock RB, Liu T (May 2016). "The Bromodomain Inhibitor JQ1 and the Histone Deacetylase Inhibitor Panobinostat Synergistically Reduce N-Myc Expression...
    26 KB (2,974 words) - 05:26, 31 May 2024
  • Thumbnail for Proto-oncogene tyrosine-protein kinase Src
    kinase inhibitor drugs that are in clinical trials include bosutinib, bafetinib, Saracatinib(AZD-0530), XLl-999, KX01 and XL228. HSP90 inhibitor NVP-BEP800...
    21 KB (2,648 words) - 12:12, 26 July 2024
  • Thumbnail for Targeted therapy
    combination with BRAF inhibitors to treat melanoma CDK inhibitors, e.g. PD-0332991, LEE011 in clinical trials Hsp90 inhibitors, some in clinical trials...
    20 KB (2,234 words) - 01:21, 22 July 2024
  • Thumbnail for Pimitespib
    "Taiho Pharmaceutical Obtains Approval to Manufacture and Market HSP90 inhibitor Jeselhy® Tablets 40 mg (Pimitespib) for Gastrointestinal Stromal Tumor...
    4 KB (167 words) - 10:33, 12 January 2024
  • Thumbnail for Chaperone (protein)
    classified based on their observed molecular weights into Hsp60, Hsp70, Hsp90, Hsp104, and small Hsps. The Hsp60 family of protein chaperones are termed...
    29 KB (3,499 words) - 07:16, 20 February 2024
  • Archived from the original on 2012-04-16. Retrieved 2012-04-17. "Exelixis HSP90 inhibitor XL888". Archived from the original on 2016-09-18. Retrieved 2016-09-16...
    18 KB (1,656 words) - 12:20, 31 March 2024
  • hypoxia and heat. The small molecule Hsp90 inhibitor, PU-H71, has been found to have a preferential binding to Hsp90 when it is in the highly integrated...
    6 KB (733 words) - 18:02, 29 April 2024
  • Thumbnail for Tyrosin-protein kinase Lck
    rafts. Masitinib also inhibits Lck, which may have some impact on its therapeutic effects in canine mastocytoma. HSP90 inhibitor NVP-BEP800 has been described...
    36 KB (4,466 words) - 12:30, 11 May 2024
  • Thumbnail for LYN
    rheostat that modulates signaling rather than as a binary on-off switch. HSP90 inhibitor NVP-BEP800 has been described to affect stability of LYN kinase and...
    32 KB (3,807 words) - 13:31, 4 April 2024
  • Thumbnail for GHKL domain
    (June 2004). "Structure-activity relationships in purine-based inhibitor binding to HSP90 isoforms". Chem. Biol. 11 (6): 775–85. doi:10.1016/j.chembiol...
    7 KB (437 words) - 02:06, 31 July 2023
  • Thumbnail for Cyclin-dependent kinase 4
    (June 1996). "Mammalian p50Cdc37 is a protein kinase-targeting subunit of Hsp90 that binds and stabilizes Cdk4". Genes & Development. 10 (12): 1491–1502...
    21 KB (2,340 words) - 12:00, 3 September 2024
  • Thumbnail for Geldanamycin
    antibiotic that inhibits the function of Hsp90 (Heat Shock Protein 90) by binding to the unusual ADP/ATP-binding pocket of the protein. HSP90 client proteins...
    10 KB (657 words) - 15:24, 2 June 2024
  • Thumbnail for Vernalis Research
    July 2015. Additionally, luminespib (AUY922) is a novel intravenous Hsp90 inhibitor with the potential to target a range of cancers, which arose from a...
    14 KB (1,160 words) - 21:43, 17 May 2024
  • Thumbnail for Resorcinol
    1002/cber.187600902133. Sidera, K.; Patsavoudi, E. (January 2014). "HSP90 inhibitors: current development and potential in cancer therapy". Recent Patents...
    20 KB (2,040 words) - 05:37, 17 April 2024
  • Thumbnail for Novobiocin
    Novobiocin (category Topoisomerase inhibitors)
    [citation needed] Novobiocin has been shown to weakly inhibit the C-terminus of the eukaryotic Hsp90 protein (high micromolar IC50). Modification of the...
    21 KB (2,266 words) - 08:08, 24 June 2024
  • Thumbnail for Radicicol
    monorden, is a natural product that binds to Hsp90 (Heat Shock Protein 90) and alters its function. HSP90 client proteins play important roles in the regulation...
    5 KB (269 words) - 14:19, 23 December 2023
  • functions to bind to DNA gyrase and inhibits ATPase activity. It acts as a competitive inhibitor and specifically inhibits Hsp90 and TopII. Novobiocin has been...
    85 KB (9,593 words) - 04:11, 17 June 2024
  • Thumbnail for Clusterin
    that blocks the CLU mRNA transcript, enhanced heat-shock protein 90 (HSP90) inhibitor activity by suppressing the heat-shock response in castrate-resistant...
    22 KB (2,433 words) - 05:09, 24 January 2024
  • sometimes susceptible to drugs that inhibit chaperones and disrupt proteostasis, such as Hsp90 inhibitors or proteasome inhibitors. Furthermore, cancer cells tend...
    25 KB (2,922 words) - 16:16, 10 January 2024