L
Lyssikatos Joseph P
Publications - 11
Citations - 623
Lyssikatos Joseph P is an academic researcher. The author has contributed to research in topics: In vivo & Kinase. The author has an hindex of 6, co-authored 11 publications receiving 597 citations.
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Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor.
Tammie C. Yeh,Vivienne Marsh,Bryan Bernat,Josh Ballard,Heidi Colwell,Ronald Evans,Janet Parry,Darin Smith,Barbara J. Brandhuber,Stefan Gross,Allison L. Marlow,Hurley Brian T,Lyssikatos Joseph P,Patrice Lee,James D. Winkler,Kevin Koch,Eli M. Wallace +16 more
TL;DR: ARRY-142886 is a potent and selective MEK1/2 inhibitor that is highly active in both in vitro and in vivo tumor models.
Journal Article
ARRY-334543, A potent, orally active small molecule inhibitor of EGFR and ErbB-2
Greg Miknis,Eli M. Wallace,Lyssikatos Joseph P,Patrice Lee,Qian Zhao,Jeremy Hans,George T. Topalov,Alexandre J. Buckmelter,Gene Tarlton,Li Ren,Josh Tullis,Bryan Bernat,Lisa Pieti Opie,Ira von Carlowitz,Janet Parry,Tony Morales,Michelle Perrier,Rich Woessner,Tracy Pheneger,Keith Hoffman,Jim Winkler,Kevin Koch +21 more
TL;DR: It is demonstrated that ARRY-334543 is a novel, potent, orally active dual inhibitor of EGFR and ErbB-2, a reversible ATP-competitive inhibitor with nanomolar potency against both kinases in vitro.
Journal Article
Preclinical development of ARRY-142886, a potent and selective MEK inhibitor
Eli M. Wallace,Tammie C. Yeh,Lyssikatos Joseph P,Jim Winkler,Patrice Lee,Allison L. Marlow,Hurley Brian T,Vivienne Marsh,Bryan Bernat,Ronald M. Evans,Heidi Colwell,Josh Ballard,Tony Morales,Darin Smith,Barb Brandhuber,Stefan Gross,Greg Poch,Kevin Litwiler,G. P. Hingorani,Jennifer N. Otten,Francis J. Sullivan,Jim Blake,Tracy Pheneger,Michelle Goyette,Kevin Koch +24 more
TL;DR: ARRY-142886 is especially potent in inhibiting the cell proliferation of mutant Ras and B-Raf cell lines such as HT29, Malme-3M, SK-MEL-28, MIA PaCa2, and SK-mEL-2 and demonstrates other desirable attributes for development including good physical chemical characteristics, low clearance, Caco-2 permeability and minimal predicted drug-drug interactions.
Journal Article
Abstract #1795: In Vitro and in vivo activity of ARRY-380: A potent, small molecule inhibitor of ErbB2.
Tracy Pheneger,Karyn Bouhana,Deborah J. Anderson,Jennifer Garrus,Kateri Ahrendt,Shelley Allen,Ira von Carlowitz,Julie Marie Greschuk,Stefan Gross,Keith Hoffman,Christine Lemieux,Lyssikatos Joseph P,Michele Callejo,Gene Tarlton,Eli M. Wallace,Shannon L. Winski,Rich Woessner,Qian Zhao,Fred P. Marmsater,Patrice Lee +19 more
TL;DR: In this paper, an orally active, selective, small molecule inhibitor of ErbB2, ARRY-380, has been proposed for tumor growth inhibition in patients with solid tumors.
Journal Article
ARRY-520, a KSP inhibitor with efficacy and pharmacodynamic activity in animal models of solid tumors
Richard Woessner,Chris Corrette,Shelley Allen,Jeremy Hans,Qian Zhao,Aicher Tom,Lyssikatos Joseph P,John H. Robinson,Greg Poch,Laura Hayter,April Cox,Patrice Lee,Jim Winkler,Kevin Koch,Eli M. Wallace +14 more
TL;DR: ARRY-520 as mentioned in this paper is a mitotic-specific kinesin spindle protein (KSP) inhibitor that plays a key role in spindle pole separation and production of the bipolar spindle.