Dineli Wickramasinghe
Amgen
15 Papers
67 Citations
Dineli Wickramasinghe is an academic researcher from Amgen. The author has contributed to research in topics: Smoothened & Kinase. The author has an hindex of 10, co-authored 15 publications.
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Papers
Preclinical Evaluation of AMG 925, a FLT3/CDK4 Dual Kinase Inhibitor for Treating Acute Myeloid Leukemia
Kathleen S. Keegan,Cong Li,Zhihong Li,Ji Ma,Mark L. Ragains,Suzanne Coberly,David Hollenback,John Eksterowicz,Lingming Liang,Margaret F. Weidner,Justin N. Huard,Xianghong Wang,Grace Alba,Jessica Orf,Mei-Chu Lo,Sharon Zhao,Rachel Ngo,Ada Chen,Lily Liu,Timothy J. Carlson,Christophe Queva,Lawrence R. McGee,Julio C. Medina,Alexander Kamb,Dineli Wickramasinghe,Kang Dai +25 more
TL;DR: Preclinical evaluation of AMG 925, a potent, selective, and bioavailable FLT3/cyclin-dependent kinase 4 (CDK4) dual kinase inhibitor, which combines inhibition of two kinases essential for proliferation and survival ofFLT3-mutated AML cells, may improve and prolong clinical responses.
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Addressing PXR liabilities of phthalazine-based hedgehog/smoothened antagonists using novel pyridopyridazines
Jacob Kaizerman,Wade Aaron,Songzhu An,Richard J. Austin,Matthew L. Brown,Angela Chong,Tom Huang,Randall W. Hungate,Ben Jiang,Michael G. Johnson,Gary Lee,Brian Lucas,Jessica Orf,Minqing Rong,Maria M. Toteva,Dineli Wickramasinghe,Guifen Xu,Qiuping Ye,Wendy Zhong,Dustin McMinn +19 more
TL;DR: Pyridopyridazine antagonists of the hedgehog signaling pathway are described in this paper, where a representative compound eliminates a PXR liability while retaining potency and in vitro metabolic stability.
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Design of 1-piperazinyl-4-arylphthalazines as potent Smoothened antagonists.
Brian Lucas,Wade Aaron,Songzhu An,Richard J. Austin,Matthew L. Brown,Hon Chan,Angela Chong,Randall W. Hungate,Tom Huang,Ben Jiang,Michael G. Johnson,Jacob Kaizerman,Gary Lee,Dustin McMinn,Jessica Orf,Jay P. Powers,Minqing Rong,Maria M. Toteva,Craig Uyeda,Dineli Wickramasinghe,Guifen Xu,Qiuping Ye,Wendy Zhong +22 more
TL;DR: A series of 1-amino-4-arylphthalazines was developed as potent and orally bioavailable inhibitors of Smoothened, and a representative compound demonstrated significant tumor volume reduction in a mouse medulloblastoma model.
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Patent
Antibody constructs for cdh19 and cd3
Peter Kufer,Patrick Hoffmann,Tobias Raum,Ralf Lutterbuese,Elisabeth Nahrwold,Claudia Blümel,Shouhua Xiao,Zheng Pan,Dineli Wickramasinghe +8 more
- 27 Jan 2014
TL;DR: In this paper, the authors presented an antibody construct comprising a first human binding domain capable of binding to human CDH19 on the surface of a target cell and a second domain able to binding to the human CD3 on the T cell.
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Discovery of amide replacements that improve activity and metabolic stability of a bis-amide smoothened antagonist hit
Matthew L. Brown,Wade Aaron,Richard J. Austin,Angela Chong,Tom Huang,Ben Jiang,Jacob Kaizerman,Gary Lee,Brian Lucas,Dustin McMinn,Jessica Orf,Minqing Rong,Maria M. Toteva,Guifen Xu,Qiuping Ye,Wendy Zhong,Michael DeGraffenreid,Dineli Wickramasinghe,Jay P. Powers,Randall W. Hungate,Michael G. Johnson +20 more
TL;DR: A bis-amide antagonist of Smoothened, a seven-transmembrane receptor in the Hedgehog signaling pathway, was discovered via high throughput screening and several bioisosteric replacements of the labile amide that maintained in vitro potency were identified and shown to be metabolically stable in vitro and in vivo.
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