ATSP-7041, a Dual MDM2 and MDMX Targeting Stapled A-helical Peptide Exhibits Potent in Vitro and in Vivo Efficacy in Xenograft Models of Human Cancer

被引：2
|
作者：
Chang, Y. [1 ]
Graves, B. [2 ]
Guerlavais, V. [1 ]
Vassilev, L. [2 ]
Packman, K. [2 ]
Olson, K. [1 ]
Annis, A. [1 ]
Tovar, C. [2 ]
Nash, H. [1 ]
Sawyer, T. [1 ]
机构：
[1] Aileron Therapeut Inc, Cambridge, MA USA
[2] Hoffmann La Roche Inc, Roche Res Ctr, Nutley, NJ 07110 USA
来源：
EUROPEAN JOURNAL OF CANCER | 2012年 / 48卷
关键词：
D O I：
10.1016/S0959-8049(12)72024-5
中图分类号：
R73 [肿瘤学];
学科分类号：
100214 ;
摘要：
226
引用
收藏
页码：68 / 69
页数：2
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  • [1] Design, synthesis, biophysical and structure-activity properties of a novel dual MDM2 and MDMX targeting stapled a-helical peptide, ATSP-7041, that exhibits potent in vitro and in vivo efficacy in xenograft models of human cancer
    Guerlavais, V.
    Graves, B.
    Tovar, C.
    Packman, K.
    Olson, K.
    Kesavan, K.
    Gangurde, P.
    Darlak, K.
    Horstick, J.
    Mukherjee, A.
    Baker, T.
    Shi, E.
    Lentini, S.
    Sun, K.
    Irwin, S.
    Feyfant, E.
    To, T.
    Filipovic, Z.
    Elkin, C.
    Pero, J.
    Santiago, S.
    Bruton, T.
    Sawyer, T.
    Annis, A.
    Fotouhi, N.
    Manning, T.
    Nash, H.
    Vassilev, L. T.
    Chang, Y. S.
    Sawyer, T. K.
    [J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2013, 245
  • [2] ATSP-7041: A Novel Stapled α-Helical Peptide Dual Inhibitor of MDM2 and MDMX Effective In Vivo for p53-Dependent Cancers
    Sawyer, Tomi K.
    [J]. BIOPOLYMERS, 2013, 100 (03) : 236 - 236
  • [3] Stapled α-helical peptide drug development: A potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy
    Chang, Yong S.
    Graves, Bradford
    Guerlavais, Vincent
    Tovar, Christian
    Packman, Kathryn
    To, Kwong-Him
    Olson, Karen A.
    Kesavan, Kamala
    Gangurde, Pranoti
    Mukherjee, Aditi
    Baker, Theresa
    Darlak, Krzysztof
    Elkin, Carl
    Filipovic, Zoran
    Qureshi, Farooq Z.
    Cai, Hongliang
    Berry, Pamela
    Feyfant, Eric
    Shi, Xiangguo E.
    Horstick, James
    Annis, D. Allen
    Manning, Anthony M.
    Fotouhi, Nader
    Nash, Huw
    Vassilev, Lyubomir T.
    Sawyer, Tomi K.
    [J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 2013, 110 (36) : E3445 - E3454
  • [4] Dual Inhibition of Mdmx and Mdm2 Using an Alpha-Helical P53 Stapled Peptide (ALRN-6924) As a Novel Therapeutic Strategy in Acute Myeloid Leukemia
    Carvajal, Luis A.
    Ben-Neriah, Daniela
    Senecal, Adrien
    Bernard, Lumie
    Narayanagari, Swathi-Rao
    Kenworthy, Charles
    Thiruthuvanathan, Victor
    Guerlavais, Vincent
    Annis, D. Allen
    Bartholdy, Boris
    Will, Britta
    Anampa, Jesus
    Mantzaris, Ioannis
    Aivado, Manuel A.
    Singer, Robert H.
    Coleman, Robert
    Verma, Amit
    Steidl, Ulrich G.
    [J]. BLOOD, 2017, 130
  • [5] Harnessing the anticancer activity of the stapled peptide ALRN-6924, a dual inhibitor of MDMX and MDM2, using rational combination strategies for breast cancer and other malignancies
    Annis, A.
    Ren, J. G.
    Carvajal, L. A.
    Santiago, S.
    Narasimhan, N.
    Sutton, D.
    Pairawan, S. S.
    Guerlavais, V.
    Meric-Bernstam, F.
    Aivado, M.
    [J]. EUROPEAN JOURNAL OF CANCER, 2018, 103 : E143 - E144
  • [6] The stapled peptide ALRN-6924, a dual inhibitor of MDMX and MDM2, and the CDK4/6 inhibitors palbociclib or abemaciclib synergistically enhance each other's in vitro and in vivo anticancer activity
    Annis, A.
    Carvajal, L. A.
    Ren, J-G
    Sutton, D.
    Santiago, S.
    Narasimhan, N.
    Guerlavais, V.
    Aivado, M.
    [J]. CANCER RESEARCH, 2019, 79 (04)
  • [7] The stapled peptide ALRN-6924, a dual inhibitor of MDMX and MDM2, enhances antitumor efficacy of paclitaxel and Nab-paclitaxel in TP53 wild-type MCF-7 breast cancer models
    Pairawan, S. S.
    Yuca, E.
    Evans, K.
    Annis, A.
    Narasimhan, N.
    Sutton, D.
    Carvajal, L. A.
    Ren, J-G
    Santiago, S.
    Guerlavais, V.
    Akcakanat, A.
    Tapia, C.
    Dumbrava, E. E. Illeana
    Aivado, M.
    Meric-Bernstam, F.
    [J]. CANCER RESEARCH, 2019, 79 (04)
  • [8] In Vitro andpre-Clinical In Vivo evidence Support MDMX/MDM2 As Common Vulnerabilities across TP53 -Wild-Type T-Cell Lymphomas That Are Targetable with the α-Helical p53 Stapled Peptide Alrn-6924
    Koch, Raphael
    Christie, Amanda L.
    Yoshida, Noriaki
    Ng, Samuel Y.
    Shigemori, Kay
    Morrow, Sara N.
    Van Scoyk, Alexandria
    Horwitz, Steven M.
    Jacobsen, Eric
    Santiago, Solimar
    Ren, Jian-Guo
    Guerlavais, Vincent
    Annis, D. Allan
    Aivado, Manuel A.
    Weinstock, David M.
    [J]. BLOOD, 2017, 130
  • [9] AR36A36.11.1, a monoclonal antibody targeting CD59, enhances complement activity and exhibits potent in vivo efficacy in multiple human cancer models
    Mak, Baldwin C.
    McConkey, Fortunata
    Feng, Ningping
    O'Reilly, Kevin
    Rubinstein, Daniel
    Kasprzyk, Philip G.
    Hahn, Susan E.
    Pereira, Daniel S.
    Findlay, Helen
    Young, David S.
    [J]. MOLECULAR IMMUNOLOGY, 2007, 44 (16) : 3948 - 3949
  • [10] AR36A36.11.1, a monoclonal antibody targeting CD59, enhances complement activity and exhibits potent in vivo efficacy in multiple human cancer models
    Mak, Baldwin C.
    McConkey, Fortunata
    Feng, Ningping
    O'Reilly, Kevin
    Kasprzyk, Philip G.
    Rubinstein, Daniel
    Hahn, Susan E.
    Pereira, Daniel S.
    Findlay, Helen
    Young, David S.
    [J]. MOLECULAR CANCER THERAPEUTICS, 2007, 6 (12) : 3357S - 3358S
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