M
Milan Bruncko
Researcher at AbbVie
Publications - 45
Citations - 5281
Milan Bruncko is an academic researcher from AbbVie. The author has contributed to research in topics: Cancer & Small molecule. The author has an hindex of 17, co-authored 42 publications receiving 4979 citations. Previous affiliations of Milan Bruncko include Idun Pharmaceuticals.
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Journal ArticleDOI
An inhibitor of Bcl-2 family proteins induces regression of solid tumours
Tilman Oltersdorf,Steven W. Elmore,Alexander R. Shoemaker,Robert C. Armstrong,David J. Augeri,Barbara A. Belli,Milan Bruncko,Thomas L. Deckwerth,Jürgen Dinges,Philip J. Hajduk,Mary K. Joseph,Shinichi Kitada,Stanley J. Korsmeyer,Stanley J. Korsmeyer,Kunzer Aaron R,Anthony Letai,Chi Li,Michael J. Mitten,David G. Nettesheim,Shi Chung Ng,Paul Nimmer,Jacqueline M. O'Connor,Anatol Oleksijew,Andrew M. Petros,John C. Reed,Wang Shen,Stephen K. Tahir,Craig B. Thompson,Kevin J. Tomaselli,Baole Wang,Wendt Michael D,Haichao Zhang,Stephen W. Fesik,Saul H. Rosenberg +33 more
TL;DR: Mechanistic studies reveal that ABT-737 does not directly initiate the apoptotic process, but enhances the effects of death signals, displaying synergistic cytotoxicity with chemotherapeutics and radiation.
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Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax).
Joel D. Leverson,Haichao Zhang,Jun Chen,Stephen K. Tahir,D.C. Phillips,John Xue,Paul Nimmer,Sha S. Jin,Morey L. Smith,Yu Xiao,Peter Kovar,Atsushi Tanaka,Milan Bruncko,George S. Sheppard,Leyu Wang,Sarah Gierke,Lorna Kategaya,Daniel Anderson,Chihunt Wong,Jeffrey Eastham-Anderson,Mary J. C. Ludlam,Deepak Sampath,Wayne J. Fairbrother,Ingrid E. Wertz,Saul H. Rosenberg,Chris Tse,Steven W. Elmore,Andrew J. Souers +27 more
TL;DR: This work represents the first description of small-molecule MCL-1 inhibitors with sufficient potency to induce clear on-target cellular activity, and demonstrates the utility of these molecules as chemical tools for dissecting the basic biology of M CL-1.
Journal ArticleDOI
Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins.
Cheol-Min Park,Milan Bruncko,Jessica Adickes,Joy Bauch,Hong Ding,Kunzer Aaron R,Kennan C. Marsh,Paul Nimmer,Alexander R. Shoemaker,Xiaohong Song,Stephen K. Tahir,Christin Tse,Wang Xilu,Michael D. Wendt,Xiufen Yang,Haichao Zhang,Stephen W. Fesik,Saul H. Rosenberg,Steven W. Elmore +18 more
TL;DR: Targeted modifications at three key positions of 1 resulted in a 20-fold improvement in the pharmacokinetic/pharmacodynamic relationship (PK/PD) between oral exposure (AUC) and in vitro efficacy in human tumor cell lines (EC 50).
Journal ArticleDOI
Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.
Milan Bruncko,Thorsten Oost,Barbara A. Belli,Hong Ding,Mary K. Joseph,Kunzer Aaron R,Darlene Martineau,Mcclellan William J,Michael J. Mitten,Shi-Chu Ng ng,Paul Nimmer,Tilman Oltersdorf,Cheol-Min Park,Andrew M. Petros,Alexander R. Shoemaker,Xiaohong Song,Wang Xilu,Wendt Michael D,Haichao Zhang,Stephen W. Fesik,Saul H. Rosenberg,Steven W. Elmore +21 more
TL;DR: Compound 2 demonstrated single agent efficacy against human follicular lymphoma cell lines that overexpress Bcl-2, and efficacy in a murine xenograft model of lymphoma when given both as a single agent and in combination with etoposide.
Journal ArticleDOI
A Small-Molecule Inhibitor of Bcl-XL Potentiates the Activity of Cytotoxic Drugs In vitro and In vivo
Alex R. Shoemaker,Anatol Oleksijew,Joy Bauch,Barbara A. Belli,Tony Borre,Milan Bruncko,Thomas Deckwirth,David Frost,Ken Jarvis,Mary K. Joseph,Kennan C. Marsh,Mcclellan William J,Hugh N. Nellans,Shi-Chung Ng,Paul Nimmer,Jacqueline M. O'Connor,Tilman Oltersdorf,Weiguo Qing,Wang Shen,Jason Stavropoulos,Stephen K. Tahir,Baole Wang,Robert B. Warner,Haichao Zhang,Stephen W. Fesik,Saul H. Rosenberg,Steven W. Elmore +26 more
TL;DR: A-385358 enhances the in vitro cytotoxic activity of numerous chemotherapeutic agents (pac litaxel, etoposide, cisplatin, and doxorubicin) in several tumor cell lines and potentiates the activity of paclitaxel in vivo.