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HSP90-dependent PUS7 overexpression facilitates the metastasis of colorectal cancer cells by regulating LASP1 abundance.
Song D, Guo M, Xu S, Song X, Bai B, Li Z, Chen J, An Y, Nie Y, Wu K, Wang S, Zhao Q. Song D, et al. J Exp Clin Cancer Res. 2021 May 14;40(1):170. doi: 10.1186/s13046-021-01951-5. J Exp Clin Cancer Res. 2021. PMID: 33990203 Free PMC article.
Furthermore, HSP90 was identified as a client protein of PUS7, associated with the increased PUS7 abundance in CRC. NMS-E973, a specific HSP90 inhibitor, also showed higher anti-metastatic activity when combined with PUS7 repression. ...
Furthermore, HSP90 was identified as a client protein of PUS7, associated with the increased PUS7 abundance in CRC. NMS-E973, …
Evaluation of [(11)C]NMS-E973 as a PET tracer for in vivo visualisation of HSP90.
Vermeulen K, Naus E, Ahamed M, Attili B, Siemons M, Luyten K, Celen S, Schymkowitz J, Rousseau F, Bormans G. Vermeulen K, et al. Theranostics. 2019 Jan 1;9(2):554-572. doi: 10.7150/thno.27213. eCollection 2019. Theranostics. 2019. PMID: 30809293 Free PMC article.
Pretreatment of B16.F10 melanoma mice with PU-H71 or Ganetespib (50 mg/kg) completely blocked tumour accumulation of [(11)C]NMS-E973 and confirmed in vivo HSP90 binding specificity. HSP90-specific binding of [(11)C]NMS-E973 was observed in blood, lungs …
Pretreatment of B16.F10 melanoma mice with PU-H71 or Ganetespib (50 mg/kg) completely blocked tumour accumulation of [(11)C]NMS-E9 …
Hsp90 inhibitor NMS-E973 exerts the anticancer effect against glioblastoma via induction of PUMA-mediated apoptosis.
Sun L, Yang S, Chi G, Jin X. Sun L, et al. Onco Targets Ther. 2018 Mar 20;11:1583-1593. doi: 10.2147/OTT.S160813. eCollection 2018. Onco Targets Ther. 2018. PMID: 29593424 Free PMC article.
Furthermore, PUMA was induced by NMS-E973 treatment in xenograft tumors, and deficiency in PUMA significantly suppressed the antitumor effects of NMS-E973. CONCLUSION: Our study suggests that PUMA-mediated apoptosis is important for the therapeutic res …
Furthermore, PUMA was induced by NMS-E973 treatment in xenograft tumors, and deficiency in PUMA significantly suppressed the a …
Combined inhibition of Hsp90 and heme oxygenase-1 induces apoptosis and endoplasmic reticulum stress in melanoma.
Barbagallo I, Parenti R, Zappalà A, Vanella L, Tibullo D, Pepe F, Onni T, Li Volti G. Barbagallo I, et al. Acta Histochem. 2015 Oct;117(8):705-11. doi: 10.1016/j.acthis.2015.09.005. Epub 2015 Oct 19. Acta Histochem. 2015. PMID: 26493719
In the present study we investigated the chemotherapic effects of combining an Hsp90 inhibitor (NMS E973) and an HO-1 inhibitor (SnMP) on A375 melanoma cells. NMS E973 treatment was able to reduce cell viability and induce endoplasmic reticulum (ER) st …
In the present study we investigated the chemotherapic effects of combining an Hsp90 inhibitor (NMS E973) and an HO-1 inhibito …
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).
Brasca MG, Mantegani S, Amboldi N, Bindi S, Caronni D, Casale E, Ceccarelli W, Colombo N, De Ponti A, Donati D, Ermoli A, Fachin G, Felder ER, Ferguson RD, Fiorelli C, Guanci M, Isacchi A, Pesenti E, Polucci P, Riceputi L, Sola F, Visco C, Zuccotto F, Fogliatto G. Brasca MG, et al. Bioorg Med Chem. 2013 Nov 15;21(22):7047-63. doi: 10.1016/j.bmc.2013.09.018. Epub 2013 Sep 19. Bioorg Med Chem. 2013. PMID: 24100158
Novel small molecule inhibitors of heat shock protein 90 (Hsp90) were discovered with the help of a fragment based drug discovery approach (FBDD) and subsequent optimization with a combination of structure guided design, parallel synthesis and application of medicinal chemistry p …
Novel small molecule inhibitors of heat shock protein 90 (Hsp90) were discovered with the help of a fragment based drug discovery approach ( …
NMS-E973, a novel synthetic inhibitor of Hsp90 with activity against multiple models of drug resistance to targeted agents, including intracranial metastases.
Fogliatto G, Gianellini L, Brasca MG, Casale E, Ballinari D, Ciomei M, Degrassi A, De Ponti A, Germani M, Guanci M, Paolucci M, Polucci P, Russo M, Sola F, Valsasina B, Visco C, Zuccotto F, Donati D, Felder E, Pesenti E, Galvani A, Mantegani S, Isacchi A. Fogliatto G, et al. Clin Cancer Res. 2013 Jul 1;19(13):3520-32. doi: 10.1158/1078-0432.CCR-12-3512. Epub 2013 May 14. Clin Cancer Res. 2013. PMID: 23674492
EXPERIMENTAL DESIGN: Here is described a detailed biochemical and crystallographic characterization of NMS-E973. Mechanism-based anticancer activity was described in cell models, including models of resistance to kinase inhibitors. ...Moreover, consistent with its b …
EXPERIMENTAL DESIGN: Here is described a detailed biochemical and crystallographic characterization of NMS-E973. Mechanism-bas …