In-Vitro and in-Vivo Evaluation of the Orally Active Proteasome Inhibitor MLN9708 in Hematological Models of Human Cancer

Erik Kupperman; Edmund Lee; Yueying Cao; Bret Bannerman; Michael Fitzgerald; Allison J. Berger; Jie Yu; Julie Zhang; Paul Hales; Frank Bruzzese; Jane Liu; Jonathan Blank; Khristofer Garcia; Christopher Tsu; Larry Dick; Paul Fleming; Li Yu; Mark G. Manfredi; Mark Rolfe; Joseph Bolen

doi:10.1182/blood.V114.22.2709.2709

In-Vitro and in-Vivo Evaluation of the Orally Active Proteasome Inhibitor MLN9708 in Hematological Models of Human Cancer

Erik Kupperman, Edmund Lee, Yueying Cao, Bret Bannerman, Michael Fitzgerald, Allison J. Berger, Jie Yu, Julie Zhang, Paul Hales, Frank Bruzzese, Jane Liu, Jonathan Blank, Khristofer Garcia, Christopher Tsu, Larry Dick, Paul Fleming, Li Yu, Mark G. Manfredi, Mark Rolfe, Joseph Bolen

Research output: Contribution to journal › Article

Abstract

The ubiquitin-proteasome system processes the majority of cellular proteins and is the principal manner by which cells regulate protein homeostasis. The successful development of bortezomib for multiple myeloma and previously treated mantle cell lymphoma has validated the proteasome as a therapeutic target for hematological malignancies. MLN9708 was identified in screens for a proteasome inhibitor with greater antitumor activity than bortezomib in preclinical xenograft models. MLN9708 immediately hydrolyzes to MLN2238, the biologically active form, upon exposure to aqueous solutions or plasma. MLN2238 was used for all preclinical studies described below

Original language	Unknown
Pages (from-to)	1061
Number of pages	1
Journal	BLOOD
Volume	114
Issue number	22
DOIs	https://doi.org/10.1182/blood.V114.22.2709.2709
Publication status	Published - 20 Nov 2009
Externally published	Yes

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10.1182/blood.V114.22.2709.2709

Cite this

Kupperman, E., Lee, E., Cao, Y., Bannerman, B., Fitzgerald, M., Berger, A. J., Yu, J., Zhang, J., Hales, P., Bruzzese, F., Liu, J., Blank, J., Garcia, K., Tsu, C., Dick, L., Fleming, P., Yu, L., Manfredi, M. G., Rolfe, M., & Bolen, J. (2009). In-Vitro and in-Vivo Evaluation of the Orally Active Proteasome Inhibitor MLN9708 in Hematological Models of Human Cancer. BLOOD, 114(22), 1061. https://doi.org/10.1182/blood.V114.22.2709.2709

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title = "In-Vitro and in-Vivo Evaluation of the Orally Active Proteasome Inhibitor MLN9708 in Hematological Models of Human Cancer",

abstract = "The ubiquitin-proteasome system processes the majority of cellular proteins and is the principal manner by which cells regulate protein homeostasis. The successful development of bortezomib for multiple myeloma and previously treated mantle cell lymphoma has validated the proteasome as a therapeutic target for hematological malignancies. MLN9708 was identified in screens for a proteasome inhibitor with greater antitumor activity than bortezomib in preclinical xenograft models. MLN9708 immediately hydrolyzes to MLN2238, the biologically active form, upon exposure to aqueous solutions or plasma. MLN2238 was used for all preclinical studies described below",

author = "Erik Kupperman and Edmund Lee and Yueying Cao and Bret Bannerman and Michael Fitzgerald and Berger, \{Allison J.\} and Jie Yu and Julie Zhang and Paul Hales and Frank Bruzzese and Jane Liu and Jonathan Blank and Khristofer Garcia and Christopher Tsu and Larry Dick and Paul Fleming and Li Yu and Manfredi, \{Mark G.\} and Mark Rolfe and Joseph Bolen",

note = "51st Annual Meeting of the American-Society-of-Hematology, New Orleans, LA, DEC 05-08, 2009",

year = "2009",

month = nov,

day = "20",

doi = "10.1182/blood.V114.22.2709.2709",

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Kupperman, E, Lee, E, Cao, Y, Bannerman, B, Fitzgerald, M, Berger, AJ, Yu, J, Zhang, J, Hales, P, Bruzzese, F, Liu, J, Blank, J, Garcia, K, Tsu, C, Dick, L, Fleming, P, Yu, L, Manfredi, MG, Rolfe, M & Bolen, J 2009, 'In-Vitro and in-Vivo Evaluation of the Orally Active Proteasome Inhibitor MLN9708 in Hematological Models of Human Cancer', BLOOD, vol. 114, no. 22, pp. 1061. https://doi.org/10.1182/blood.V114.22.2709.2709

TY - JOUR

T1 - In-Vitro and in-Vivo Evaluation of the Orally Active Proteasome Inhibitor MLN9708 in Hematological Models of Human Cancer

AU - Kupperman, Erik

AU - Lee, Edmund

AU - Cao, Yueying

AU - Bannerman, Bret

AU - Fitzgerald, Michael

AU - Berger, Allison J.

AU - Yu, Jie

AU - Zhang, Julie

AU - Hales, Paul

AU - Bruzzese, Frank

AU - Liu, Jane

AU - Blank, Jonathan

AU - Garcia, Khristofer

AU - Tsu, Christopher

AU - Dick, Larry

AU - Fleming, Paul

AU - Yu, Li

AU - Manfredi, Mark G.

AU - Rolfe, Mark

AU - Bolen, Joseph

N1 - 51st Annual Meeting of the American-Society-of-Hematology, New Orleans, LA, DEC 05-08, 2009

PY - 2009/11/20

Y1 - 2009/11/20

N2 - The ubiquitin-proteasome system processes the majority of cellular proteins and is the principal manner by which cells regulate protein homeostasis. The successful development of bortezomib for multiple myeloma and previously treated mantle cell lymphoma has validated the proteasome as a therapeutic target for hematological malignancies. MLN9708 was identified in screens for a proteasome inhibitor with greater antitumor activity than bortezomib in preclinical xenograft models. MLN9708 immediately hydrolyzes to MLN2238, the biologically active form, upon exposure to aqueous solutions or plasma. MLN2238 was used for all preclinical studies described below

AB - The ubiquitin-proteasome system processes the majority of cellular proteins and is the principal manner by which cells regulate protein homeostasis. The successful development of bortezomib for multiple myeloma and previously treated mantle cell lymphoma has validated the proteasome as a therapeutic target for hematological malignancies. MLN9708 was identified in screens for a proteasome inhibitor with greater antitumor activity than bortezomib in preclinical xenograft models. MLN9708 immediately hydrolyzes to MLN2238, the biologically active form, upon exposure to aqueous solutions or plasma. MLN2238 was used for all preclinical studies described below

U2 - 10.1182/blood.V114.22.2709.2709

DO - 10.1182/blood.V114.22.2709.2709

M3 - Erthygl

SN - 0006-4971

VL - 114

SP - 1061

JO - BLOOD

JF - BLOOD

IS - 22

ER -