James Kanter
Millennium Pharmaceuticals
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Publication
Featured researches published by James Kanter.
Proceedings of the National Academy of Sciences of the United States of America | 2003
Suzanne J. Bakewell; Patrick Nestor; Srinivasa Prasad; Michael H. Tomasson; Nikki Dowland; Mukund Mehrotra; Robert M. Scarborough; James Kanter; Keith Abe; David H. Phillips; Katherine N. Weilbaecher
Mice with a targeted deletion of β3 integrin were used to examine the process by which tumor cells metastasize and destroy bone. Injection of B16 melanoma cells into the left cardiac ventricle resulted in osteolytic bone metastasis in 74% of β3+/+ mice by 14 days. In contrast, only 4% of β3–/– mice developed bone lesions. Direct intratibial inoculation of tumor resulted in marrow replacement by tumor in β3–/– mice, but no associated trabecular bone resorption as seen inβ3+/+ mice. Bone marrow transplantation studies showed that susceptibility to bone metastasis was conferred by a bone marrow-derived cell. To dissect the roles of osteoclast and platelet β3 integrins in this model of bone metastasis, osteoclast-defective src–/– mice were used. Src-null mice were protected from tumor-associated bone destruction but were not protected from tumor cell metastasis to bone. In contrast, a highly specific platelet aggregation inhibitor of activated αIIbβ3 prevented B16 metastases. These data demonstrate a critical role for platelet αIIbβ3 in tumor entry into bone and suggest a mechanism by which antiplatelet therapy may be beneficial in preventing the metastasis of solid tumors.
Bioorganic & Medicinal Chemistry Letters | 2009
Penglie Zhang; Wenrong Huang; Lingyan Wang; Liang Bao; Zhaozhong J. Jia; Shawn M. Bauer; Erick A. Goldman; Gary D. Probst; Yonghong Song; Ting Su; Jingmei Fan; Yanhong Wu; Wenhao Li; John Woolfrey; Uma Sinha; Paul Wong; Susan T. Edwards; Ann E. Arfsten; Lane Clizbe; James Kanter; Anjali Pandey; Gary Park; Athiwat Hutchaleelaha; Joseph L. Lambing; Stanley J. Hollenbach; Robert M. Scarborough; Bing-Yan Zhu
Systematic SAR studies of in vitro factor Xa inhibitory activity around compound 1 were performed by modifying each of the three phenyl rings. A class of highly potent, selective, efficacious and orally bioavailable direct factor Xa inhibitors was discovered. These compounds were screened in hERG binding assays to examine the effects of substitution groups on the hERG channel affinity. From the leading compounds, betrixaban (compound 11, PRT054021) has been selected as the clinical candidate for development.
Bioorganic & Medicinal Chemistry Letters | 2002
Yonghong Song; Lane Clizbe; Chhaya Bhakta; Willy Teng; Wenhao Li; Yanhong Wu; Zhaozhong Jon Jia; Penglie Zhang; Lingyan Wang; Brandon Doughan; Ting Su; James Kanter; John Woolfrey; Paul Wong; Brian Huang; Katherine Tran; Uma Sinha; Gary Park; Andrea Reed; John Malinowski; Stan Hollenbach; Robert M. Scarborough; Bing-Yan Zhu
Substituted acrylamides were used as templates that bridge P1 and P4 binding elements, resulting in a series of potent (sub-nanomolar) and selective factor Xa inhibitors. In this template, cis-geometry of P1 and P4 ligands is highly preferred. SAR on the substituting groups, as well as on modification of P1 and P4 moieties is described. Compounds in this series show good in vivo efficacy in animal models.
Bioorganic & Medicinal Chemistry Letters | 2001
Ting Su; Yanhong Wu; Brandon Doughan; Kim Kane-Maguire; Charles K. Marlowe; James Kanter; John Woolfrey; Brian Huang; Paul Wong; Uma Sinha; Gary Park; John Malinowski; Stan Hollenbach; Robert M. Scarborough; Bing-Yan Zhu
A series of glycolic and mandelic acid derivatives was synthesized and investigated for their factor Xa inhibitory activity. These analogues are highly potent and selective inhibitors against fXa. In a rabbit deep vein thrombosis model, compound 26 showed significant antithrombotic effects (81% inhibition of thrombus formation) at 1.1 microM plasma concentration following intravenous administration.
Handbook of experimental pharmacology | 2000
Bing-Yan Zhu; Zhaozhong Jon Jia; Wenrong Huang; Yonghong Song; James Kanter; Robert M. Scarborough
Archive | 2006
Craig M. Grant; James Kanter; Graeme Langlands
Archive | 2007
Robert M. Scarborough; James Kanter; Keiko Sujino; Sharique Zuberi
Archive | 2006
Craig M. Grant; James Kanter; Graeme Langlands
Archive | 2009
James Kanter; Anjali Pandey; James Robinson; Robert M. Scarborough
Archive | 2001
James Kanter; Anjali Pandey; James Robinson; Robert M. Scarborough