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Title: | Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor. | Authors: | Habets G.;Powell B.;West B.L.;Matusow B.;Tsang G.;Shellooe R.;Carias H.;Nguyen H.;Marimuthu A.;Zhang K.Y.J.;Oh A.;Bremer R.;Hurt C.R.;Artis D.R.;Wu G.;Nespi M.;Spevak W.;Lin P.;Nolop K.;Hirth P.;Tesch G.H.;Bollag G.;Zhang C.;Ibrahim P.N.;Zhang J.;Burton E.A.;Zhang Y. | Institution: | (Zhang, Ibrahim, Zhang, Burton, Habets, Zhang, Powell, West, Matusow, Tsang, Shellooe, Carias, Nguyen, Marimuthu, Zhang, Oh, Bremer, Hurt, Artis, Wu, Nespi, Spevak, Lin, Nolop, Hirth, Bollag) Plexxikon Inc., Berkeley, CA 94710, United States (Tesch) Department of Nephrology, Monash Medical Centre, Monash University, Clayton, VIC 3168, Australia | Issue Date: | 15-Apr-2013 | Copyright year: | 2013 | Publisher: | National Academy of Sciences (2101 Constitution Avenue NW, Washington DC 20418, United States) | Place of publication: | United States | Publication information: | Proceedings of the National Academy of Sciences of the United States of America. 110 (14) (pp 5689-5694), 2013. Date of Publication: 02 Apr 2013. | Abstract: | Inflammation and cancer, two therapeutic areas historically addressed by separate drug discovery efforts, are now coupled in treatment approaches by a growing understanding of the dynamic molecular dialogues between immune and cancer cells. Agents that target specific compartments of the immune system, therefore, not only bring new disease modifying modalities to inflammatory diseases, but also offer a new avenue to cancer therapy by disrupting immune components of the microenvironment that foster tumor growth, progression, immune evasion, and treatment resistance. McDonough feline sarcoma viral (v-fms) oncogene homolog (FMS) and v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog (KIT) are two hematopoietic cell surface receptors that regulate the development and function of macrophages and mast cells, respectively. We disclose a highly specific dual FMS and KIT kinase inhibitor developed from a multifaceted chemical scaffold. As expected, this inhibitor blocks the activation of macrophages, osteoclasts, and mast cells controlled by these two receptors. More importantly, the dual FMS and KIT inhibition profile has translated into a combination of benefits in preclinical disease models of inflammation and cancer. | DOI: | http://monash.idm.oclc.org/login?url=http://dx.doi.org/10.1073/pnas.1219457110 | PubMed URL: | 23493555 [http://www.ncbi.nlm.nih.gov/pubmed/?term=23493555] | ISSN: | 0027-8424 | URI: | https://repository.monashhealth.org/monashhealthjspui/handle/1/42649 | Type: | Article |
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