Page 313 - Read Online
P. 313
Page 18 of 18 Qureshy et al. J Cancer Metastasis Treat 2020;6:27 I http://dx.doi.org/10.20517/2394-4722.2020.58
arthritis: results from two randomized, controlled phase 2b trials. Rheumatol Ther 2020;7:173-90.
162. Van Rompaey L, Galien R, van der Aar EM, Clement-Lacroix P, Nelles L, et al. Preclinical characterization of GLPG0634, a selective
Page 18 of 18 Qureshy et al. J Cancer Metastasis Treat 2020;6:27 I http://dx.doi.org/10.20517/2394-4722.2020.58 inhibitor of JAK1, for
the treatment of inflammatory diseases. J Immunol 2013;191:3568-77.
163. Chuang CH, Greenside PG, Rogers ZN, Brady JJ, Yang D, et al. Molecular definition of a metastatic lung cancer state reveals a targetable
CD109-Janus kinase-Stat axis. Nat Med 2017;23:291-300. 164. Huang Z, Zhou W, Li Y, Cao M, Wang T, et al. Novel hybrid molecule
overcomes the limited response of solid tumours to HDAC inhibitors via suppressing JAK1-STAT3-BCL2 signalling. Theranostics
2018;8:4995-5011.
165. Hexner EO, Serdikoff C, Jan M, Swider CR, Robinson C, et al. Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5
signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders. Blood 2008;111:5663-71.
166. Pinto N, Prokopec SD, Vizeacoumar F, Searle K, Lowerison M, et al. Lestaurtinib is a potent inhibitor of anaplastic thyroid cancer cell
line models. PLoS One 2018;13:e0207152.
167. Takeuchi T, Tanaka Y, Iwasaki M, Ishikura H, Saeki S, et al. Efficacy and safety of the oral Janus kinase inhibitor peficitinib (ASP015K)
monotherapy in patients with moderate to severe rheumatoid arthritis in Japan: a 12-week, randomised, double-blind, placebo-controlled
phase IIb study. Ann Rheum Dis 2016;75:1057-64.
168. Kivitz AJ, Gutierrez-Ureña SR, Poiley J, Genovese MC, Kristy R, et al. Peficitinib, a JAK inhibitor, in the treatment of moderate-tosevere
rheumatoid arthritis in patients with an inadequate response to methotrexate. Arthritis Rheumatol 2017;69:709-19.
169. Ruan Z, Yang X, Cheng W. OCT4 accelerates tumorigenesis through activating JAK/STAT signaling in ovarian cancer side population
cells. Cancer Manag Res 2019;11:389-99.
170. Schwartz DM, Kanno Y, Villarino A, Ward M, Gadina M, et al. JAK inhibition as a therapeutic strategy for immune and inflammatory
diseases. Nat Rev Drug Discov 2017;17:78.
171. Levitzki A. Tyrphostins: tyrosine kinase blockers as novel antiproliferative agents and dissectors of signal transduction. FASEB J
1992;6:3275-82.
172. Ioannidis S, Lamb ML, Wang T, Almeida L, Block MH, et al. Discovery of 5-chloro- N 2-[(1 S)-1-(5-fluoropyrimidin-2-yl) ethyl]- N
4-(5-methyl-1 H -pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the jak/stat pathway. J Med Chem 2011;54:262-
76.
173. Cao JJ, Hood J, Lohse D, Mak CC, McPherson A, et al. WO2007053452A1 - Bi-aryl meta-pyrimidine inhibitors of kinases. Accessed
from: https://patents.google.com/patent/WO2007053452A1/el. [Accessed on 12 Aug 2020]
174. Menet CJ, Fletcher SR, Van Lommen G, Geney R, Blanc J, et al. Triazolopyridines as selective JAK1 inhibitors: from hit identification to
GLPG0634. J Med Chem 2014;57:9323-42.
175. Huang T, Xue CB, Wang A, Kong L, Ye HF, et al. WO2011112662A1 Piperidin-4-yl azetidine derivatives as jak1 inhibitors. Accessed
from: https://patents.google.com/patent/WO2011112662A1/en. [Accessed on 12 Aug 2020]
176. Thompson JE, Cubbon RM, Cummings RT, Wicker LS, Frankshun R, et al. Photochemical preparation of a pyridone containing
tetracycle: a Jak protein kinase inhibitor. Bioorganic Med Chem Lett 2002;12:1219-23.
177. Gingrich DE, Hudkins RL. Synthesis and kinase inhibitory activity of 3′-(S)-epi-K-252a. Bioorganic Med Chem Lett 2002;12:2829-31.
178. Tyner JW, Bumm TG, Deininger J, Wood L, Aichberger KJ, et al. CYT387, a novel JAK2 inhibitor, induces hematologic responses and
normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood 2010;115:5232-40.
179. William AD, Lee ACH, Blanchard S, Poulsen A, Teo EL, et al. Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-
dioxa-5,7, 26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent
Janus Kinase 2/Fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymphoma. J Med Chem
2011;54:4638-58.
180. Hamaguchi H, Amano Y, Moritomo A, Shirakami S, Nakajima Y, et al. Discovery and structural characterization of peficitinib (ASP015K)
as a novel and potent JAK inhibitor. Bioorganic Med Chem 2018;26:4971-83.
181. Fridman J, Nussenzveig R, Liu P, Rodgers J, Burn T, et al. Discovery and preclinical characterization of INCB018424, a selective JAK2
inhibitor for the treatment of myeloproliferative disorders. Blood 2007;110:3538.
182. Flanagan ME, Blumenkopf TA, Brissette WH, Brown MF, Casavant JM, et al. Discovery of CP-690,550: a potent and selective janus
kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection. J Med Chem 2010;53:8468-84.
183. Verstovsek S, Manshouri T, Quintás-Cardama A, Harris D, Cortes J, et al. WP1066, a novel JAK2 inhibitor, suppresses proliferation and
induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation. Clin Cancer Res 2008;14:788-96.