Emmanuel Normant
Harvard University
16 Papers
102 Citations
Emmanuel Normant is an academic researcher from Harvard University. The author has contributed to research in topics: GiST & Hsp90 inhibitor. The author has an hindex of 10, co-authored 16 publications.
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Papers
Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90.
Jie Ge,Emmanuel Normant,James R Porter,Janid A. Ali,Marlene S Dembski,Yun Gao,Asimina T. Georges,Louis Grenier,Roger H. Pak,Jon Patterson,Jens Sydor,Thomas T. Tibbitts,Jeffrey K. Tong,Julian Adams,Vito J. Palombella +14 more
TL;DR: The synthesis and evaluation of a highly soluble hydroquinone hydrochloride derivative of 17-AAG, 1a (IPI-504), and several of the physiological metabolites show comparable binding affinity to human Hsp90 and its endoplasmic reticulum (ER) homologue, the 94 kDa glucose regulated protein (Grp94).
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The Hsp90 inhibitor IPI-504 overcomes bortezomib resistance in mantle cell lymphoma in vitro and in vivo by down-regulation of the prosurvival ER chaperone BiP/Grp78
Gaël Roué,Patricia Pérez-Galán,Ana Mozos,Mónica López-Guerra,Silvia Xargay-Torrent,Laia Rosich,Ifigènia Saborit-Villarroya,Emmanuel Normant,Elias Campo,Dolors Colomer +9 more
TL;DR: Targeting unfolded protein response activation by the inhibition of Hsp90 may be an attractive model for the design of a new bortezomib-based combination therapy for MCL.
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A Phase I Study of the HSP90 Inhibitor Retaspimycin Hydrochloride (IPI-504) in Patients with Gastrointestinal Stromal Tumors or Soft-Tissue Sarcomas
Andrew J. Wagner,Rashmi Chugh,Lee S. Rosen,Jeffrey A. Morgan,Suzanne George,Michael S. Gordon,Joi Dunbar,Emmanuel Normant,David Grayzel,George D. Demetri +9 more
TL;DR: In this study of advanced GIST or other STS, IPI-504 was generally well-tolerated with some evidence of antitumor activity, serving as a clinical proof-of-concept that HSP90 inhibition remains a promising strategy.
The Novel HSP90 Inhibitor, IPI-493, Is Highly Effective in Human Gastrostrointestinal Stromal Tumor Xenografts Carrying Heterogeneous KIT Mutations
Giuseppe Floris,Raf Sciot,Agnieszka Wozniak,Thomas Van Looy,Jasmien Wellens,Gavino Faa,Emmanuel Normant,Maria Debiec-Rychter,Patrick Schöffski +8 more
TL;DR: The novel HSP90 inhibitor IPI-493 has consistent antitumor activity and induces KIT downregulation in GISTs with heterogeneous KIT mutations and synergizes with TKIs that are commonly used for the treatment of advanced or IMA-resistant GIST.
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Antitumor activity of the Hsp90 inhibitor IPI-504 in HER2-positive trastuzumab-resistant breast cancer.
Maurizio Scaltriti,Violeta Serra,Emmanuel Normant,Marta Guzman,Olga Graciela Cantu Rodriguez,Alice R. Lim,Kelly Slocum,Kip A. West,Varenka Rodriguez,Ludmila Prudkin,José Antonio Jiménez,Claudia Aura,José Baselga +12 more
TL;DR: Assessment of the antitumor activity of the Hsp90 inhibitor IPI-504 in trastuzumab-resistant, HER2-overexpressing breast cancer cells found it to represent a novel therapeutic approach in trastsized and refractory Her2-positive breast cancer.
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