Protein kinase small molecule inhibitors for rheumatoid arthritis: Medicinal chemistry/clinical perspectives

doi:10.5312/wjo.v5.i4.496

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Sep 18, 2014 (publication date) through Nov 23, 2024

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World Journal of Orthopedics

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2218-5836

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Baishideng Publishing Group Inc, 7041 Koll Center Parkway, Suite 160, Pleasanton, CA 94566, USA

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World J Orthop. Sep 18, 2014; 5(4): 496-503
Published online Sep 18, 2014. doi: 10.5312/wjo.v5.i4.496

Table 1 Janus kinase small molecule inhibitors in development

SMI	JAK Specificity/other kinase inhibitory activity	Ref.
SAR302503 (Fedratinib)	JAK2	[46]
CEP701 (Lestaurtinib)	JAK2	[47]
SB1518 (Pacritinib)	JAK2/FLT3¹	[48]
XL-019	JAK2	[48]
LY2784544	JAK2/V617F²	[49,50]
AZD1480	JAK2	[51]
NS-108	JAK2/Src³	[52]
BMS-911453	JAK2	[53]

¹FLT3: Fms-like tyrosine kinase 3; a receptor-type tyrosine-protein kinase;

²V617F: A point mutation in JAK2 (V617F) identified in the hematopoietic cells of patients with several chronic myeloproliferative disorders;

³Src: V-src avian sarcoma (Schmidt-Ruppin A-2) viral oncogene homolog; JAK: Janus kinase; SMI: Small molecule inhibitor.

Citation: Malemud CJ, Blumenthal DE. Protein kinase small molecule inhibitors for rheumatoid arthritis: Medicinal chemistry/clinical perspectives. World J Orthop 2014; 5(4): 496-503
URL: https://www.wjgnet.com/2218-5836/full/v5/i4/496.htm
DOI: https://dx.doi.org/10.5312/wjo.v5.i4.496