L
Lyubomir T. Vassilev
Researcher at Merck Serono
Publications - 125
Citations - 14924
Lyubomir T. Vassilev is an academic researcher from Merck Serono. The author has contributed to research in topics: Cancer cell & Apoptosis. The author has an hindex of 47, co-authored 117 publications receiving 13722 citations. Previous affiliations of Lyubomir T. Vassilev include Mount Sinai Hospital & University of Texas MD Anderson Cancer Center.
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Journal ArticleDOI
In vivo activation of the p53 pathway by small-molecule antagonists of MDM2.
Lyubomir T. Vassilev,Binh Thanh Vu,Bradford Graves,Daisy Carvajal,Frank John Podlaski,Zoran Filipovic,Norman Kong,Ursula Kammlott,Christine Lukacs,Christian Klein,Nader Fotouhi,Liu Emily Aijun +11 more
TL;DR: In this article, the authors identify potent and selective small-molecule antagonists of MDM2 and confirm their mode of action through the crystal structures of complexes, leading to cell cycle arrest, apoptosis, and growth inhibition of human tumor xenografts.
Journal ArticleDOI
Selective small-molecule inhibitor reveals critical mitotic functions of human CDK1.
Lyubomir T. Vassilev,Christian Tovar,Shaoqing Chen,Dejan Knezevic,Xiaolan Zhao,Hongmao Sun,David C. Heimbrook,Li Chen +7 more
TL;DR: A selective small-molecule inhibitor of CDK1 is identified that reversibly arrests human cells at the G(2)/M border of the cell cycle and allows for effective cell synchronization in early mitosis.
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Small-molecule MDM2 antagonists reveal aberrant p53 signaling in cancer: implications for therapy.
Christian Tovar,Jim Rosinski,Zoran Filipovic,Brian Higgins,Kenneth Kolinsky,Holly Hilton,Xiaolan Zhao,Binh Thanh Vu,Weiguo Qing,Packman Kathryn E,Ola Myklebost,David C. Heimbrook,Lyubomir T. Vassilev +12 more
TL;DR: It is found that the cell-cycle arrest function of the p53 pathway is preserved in multiple tumor-derived cell lines expressing wild-type p53, but many have a reduced ability to undergo p53-dependent apoptosis.
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Stapled α−helical peptide drug development: A potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy
Yong S. Chang,Bradford Graves,Vincent Guerlavais,Christian Tovar,Packman Kathryn E,Kwong-Him To,Karen A. Olson,Kamala Kesavan,Pranoti Gangurde,Aditi Mukherjee,Theresa Baker,Krzysztof Darlak,Carl Elkin,Zoran Filipovic,Farooq Qureshi,Hongliang Cai,Pamela Berry,Eric Feyfant,Xiangguo E. Shi,James Horstick,D. Allen Annis,Anthony M. Manning,Nader Fotouhi,Huw M. Nash,Lyubomir T. Vassilev,Tomi K. Sawyer +25 more
TL;DR: Overall, ATSP-7041 demonstrates in vitro and in vivo proof-of-concept that stapled peptides can be developed as therapeutically relevant inhibitors of protein–protein interaction and may offer a viable modality for cancer therapy.
Journal ArticleDOI
MDM2 inhibitors for cancer therapy
TL;DR: The new developments in the quest for pharmacological p53 activators are reviewed with an emphasis on small-molecule inhibitors of the p53-MDM2 interaction.