L
Louis Grenier
Researcher at Boehringer Ingelheim
Publications - 70
Citations - 3235
Louis Grenier is an academic researcher from Boehringer Ingelheim. The author has contributed to research in topics: Fatty acid amide hydrolase & Ansamycin. The author has an hindex of 23, co-authored 70 publications receiving 3122 citations. Previous affiliations of Louis Grenier include Millennium Pharmaceuticals.
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Journal ArticleDOI
Potent and selective inhibitors of the proteasome: Dipeptidyl boronic acids
Julian Adams,Mark L. Behnke,Shaowu Chen,Amy A. Cruickshank,Lawrence R. Dick,Louis Grenier,Janice M. Klunder,Yu-Ting Ma,Louis Plamondon,Ross L. Stein +9 more
TL;DR: Potent and selective dipeptidyl boronic acid proteasome inhibitors are described, which are promising new therapeutics for treatment of cancer and inflammatory diseases.
Journal ArticleDOI
Mechanistic studies on the inactivation of the proteasome by lactacystin: a central role for clasto-lactacystin beta-lactone.
Lawrence R. Dick,Amy A. Cruikshank,Louis Grenier,Francesco D. Melandri,Sandra L. Nunes,Ross L. Stein +5 more
TL;DR: It is suggested that lactacystin acts as a precursor for clasto-lacticstin β-l lactone and that the latter is the sole species that interacts with the proteasome.
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Mechanistic Studies on the Inactivation of the Proteasome by Lactacystin in Cultured Cells
Lawrence R. Dick,Amy A. Cruikshank,Antonia T. Destree,Louis Grenier,Teresa A. McCormack,Francesco D. Melandri,Sandra L. Nunes,Vito J. Palombella,Lana A. Parent,Louis Plamondon,Ross L. Stein +10 more
TL;DR: In this paper, the authors show that when the beta-lactone is added to mammalian cells in culture, it rapidly enters the cells, where it can react with the sulfhydryl of glutathione to form a thioester adduct that is both structurally and functionally analogous to lactacystin.
Journal ArticleDOI
Novel IKK inhibitors: β-carbolines
Alfredo C. Castro,Luan C. Dang,Francois Soucy,Louis Grenier,Hormoz Mazdiyasni,Maria Hottelet,Lana A. Parent,Christine S. Pien,Vito Palombella,Julian Adams +9 more
TL;DR: It is shown that one of these β-carboline analogues inhibits the phosphorylation of IκBα and subsequent activation of NF-κB in whole cells, as well as blocking TNF-α release in LPS-challenged mice.
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Development of 17-allylamino-17-demethoxygeldanamycin hydroquinone hydrochloride (IPI-504), an anti-cancer agent directed against Hsp90.
Jens R. Sydor,Emmanuel Normant,Christine S. Pien,James R. Porter,Jie Ge,Louis Grenier,Roger H. Pak,Janid A. Ali,Marlene Dembski,Jebecka Hudak,Jon S. Patterson,Courtney Penders,Melissa Pink,Margaret Read,Jim Sang,Caroline N. Woodward,Yilong Zhang,David Grayzel,James D. Wright,John A. Barrett,Vito J. Palombella,Julian Adams,Jeffrey K. Tong +22 more
TL;DR: IPI-504, a potent inhibitor of Hsp90, is efficacious in cellular and animal models of myeloma and is synergistically efficacious with the proteasome inhibitor bortezomib and is preferentially retained in tumor tissues relative to plasma.