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kinase-1 using knowledge-based virtual screening.
J Med Chem
2004;
47
:1962
Presented at 228th ACS National Meeting, Philadelphia, USA,
22
8.
99. Ashwell S, Caleb B, Deng C, et al. Preclinical identification of
AZD7762, a novel, potent and selective inhibitor of Checkpoint
kinases.
Mol Cancer Ther
2007;
6
. Abst A232.
100. Almeida L, Ashwell S, Ayres D, et al. Structure activity and
structure property relationships of a novel series of potent
inhibitors of Checkpoint kinases.
Mol Cancer Ther
2007;
6
. Abst
A233.
101. Zabludoff S, Deng C, Grondine M, et al. AZD7762, a novel
checkpoint kinase inhibitor, drives checkpoint abrogation and
potentiates DNA-targeted
e
26 August 2004.
118. Marshall M, King C, Barnard H,
et al
. Characterization and
preclinical development of LY2606368, a second generation Chk1
inhibitor. Presented at 22
nd
EORTC-NCI-AACR symposium on
“Molecular targets and Cancer Therapeutics,” Berlin, Germany,
16
e
19 November 2010.
119. Marshall M, Barnard D, Diaz H,
et al
. Evaluation of the antitumor
activity of pemetrexed in combination with the Chk1 inhibitor
LY2603618. Presented at 22
nd
EORTC-NCI-AACR symposium on
“Molecular Targets and Cancer Therapeutics,” Berlin, Germany,
16
e
therapies.
Mol
Cancer
Ther
19 November 2010.
120. Weiss G, Donehower E, Westin A,
et al
. A phase 1 dose-escalation
study to examine the safety and tolerability of LY2603618
administered 1 day after pemetrexed 500 mg/m
2
every 21 days in
patients with cancer. Presented at 22
nd
EORTC-NCI-AACR
symposium on “Molecular Targets and Cancer Therapeutics,”
Berlin, Germany, 16
e
66.
102. Janetka J, Almeida L, Ashwell S, et al. Discovery of a novel class
of 2-ureido thiophene carboxamide checkpoint kinase inhibitors.
Bioorg Med Chem Letts
2008;
18
:4242
2008;
7
:2955
e
8.
103. Mitchell JB, Choudhuri R, Fabre K, et al. In vitro and in vivo
radiosensitization of human tumor cells by a novel checkpoint
kinase inhibitor, AZD7762.
Clin Cancer Res
2010;
16
:2076
e
19 November 2010.
121. Parry DA. Targeting the replication checkpoint with a potent and
selective Chk1 inhibitor. Presented at 2009 AACR Annual
Meeting, Denver, USA, 18
e
84.
104. Morgan MA, Parsels LA, Zhao L, et al. Mechanism of radio-
sensitization by the Chk1/2 inhibitor AZD7762 involves abro-
gation of the G2 checkpoint and inhibition of homologous
recombinational DNA repair.
Cancer Res
2010;
70
:4972
e
22April 2009.
122. Eastman A, Montano RE, Garner KM,
et al
. Efficacy of the Chk1
inhibitor SCH-900776 at abrogating cell cycle arrest and
enhancing DNA damage-induced cytotoxicity: comparison with
UCN-01. Presented at 2010 AACR Annual Meeting, Washington,
DC, USA, 17
e
91.
105. Sampath D, Rao VA, Plunkett W. Mechanisms of apoptosis
induction by nucleoside analogs.
Oncogene
2003;
22
:9063
e
74.
106. Petermann E, Maya-Mendoza A, Zachos G, et al. Chk1 require-
ment for high global rates of replication fork progression during
normal vertebrate S phase.
Mol Cell Biol
2006;
26
:3319
e
21 April 2010.
123. Daud AA. phase I dose-escalation study of SCH 900776, a selec-
tive inhibitor of checkpoint kinase 1 (Chk1), in combination with
gemcitabine (Gem) in subjects with advanced solid tumors.
J Clin
Oncol
2010;
15s
. Abst 3064.
124. Mueller PR, Coleman TR, Kumagai A, Dunphy WG. Myt1:
a membrane-associated inhibitory kinase that phosphorylates
Cdc2 on both threonine-14 and tyrosine-15.
Science
1995;
270
:
86
e
26.
107. Karnitz LM, Flatten KS, Wagner JM, et al. Gemcitabine-induced
activation of checkpoint signaling pathways that affect tumor cell
survival.
Mol Pharmacol
2005;
68
:1636
e
44.
108. Flatten K, Dai NT, Vroman BT, et al. The role of checkpoint kinase
1 in sensitivity to topoisomerase I poisons.
J Biol Chem
2005;
280
:
14349
e
55.
109. Blasina A, Kornmann JF, Chen E, et al. A novel inhibitor of the
protein kinase Chk1: Studies on the mechanism of action.
Proc
Am Assoc Cancer Res
2005;
46
. Abst 4416.
110. Anderes KL, Blasina A, Castillo R, et al. Small molecule Chk1
inhibitor potentiates antitumour activity of chemotherapeutic
agents in vivo.
Proc Am. Assoc Cancer Res
2005;
46
. Abst 4417.
111. McArthur GA. Imaging with FLT-PET demonstrates that
PF00477736, an inhibitor of Chk1 kinase, overcomes a cell cycle
checkpoint induced by gemcitabine in PC-3 xenografts.
Proc Am
Soc Clin Oncol
2006;
25
. Abst 3045.
112. Blasina A, Kornmann JF, Chen E, et al. Characterization of a novel
and selective inhibitor of checkpoint kinase 1: Breaching the
tumour's last checkpoint defense against chemotherapeutic
agents.
Eur J Cancer Suppl
2006;
4
:115.
113. Hallin M, Zhang C, Yan Z, et al. PF00477736 an inhibitor of Chk1
enhances the antitumour activity of docetaxel indicating a role for
Chk1 in the mitotic spindle checkpoint.
Proc Am Assoc Cancer Res
2007;
48
. Abst 4373.
114. Cullinane C, Raleigh J, Anderes K, McArthur GA. Mechanisms of
radiation enhancement by the Chk1 inhibitor PF00477736.
Proc
Am Assoc Cancer Res
2007;
48
. Abst 5386.
115. Li G, Elder RT, Qin K, et al. Mechanisms of radiation enhance-
ment by the Chk1 inhibitor PF00477736.
J Biol Chem
2007;
282
:
7287
e
90.
125. Mason K, Pickett C, Ware H, et al. Preclinical in vivo evaluation
of a novel treatment strategy combining a Wee1 inhibitor with
radiotherapy.
J Clin Oncol
2010;
15s
. Abst 10596.
126. Leijen S, Schellens JH, Shapiro G, et al. Phase I pharmacological
and pharmacodynamic study of MK-1775, a Wee1 tyrosine kinase
inhibitor, in monotherapy and combination with gemcitabine,
cisplatin, or carboplatin in patients with advanced solid tumors.
J
Clin Oncol
2010;
15s
. Abst 3067.
127. Chaturvedi P, Eng WK, Zhu Y, et al. Mammalian Chk2 is
a downstream effector of the ATM-dependent DNA damage
checkpoint pathway.
Oncogene
1999;
18
:4047
e
54.
128. Kastan MB, Bartek J. Cell cycle checkpoints and cancer.
Nature
2004;
432
:316
e
23.
129. Rainey MD, Black EJ, Zachos G, Gillespie DA. Chk2 is required
for optimal mitotic delay in response to irradiation-induced DNA
damage incurred in G2 phase.
Oncogene
2008;
27
:896
e
906.
130. Carlessi L, Buscemi G, Larson G, et al. Biochemical and cellular
characterization of VRX0466617, a novel and selective inhibitor
for the checkpoint kinase Chk2.
Mol Cancer Ther
2007;
6
:935
e
44.
131. Hirao A, Cheung A, Cuncan G, et al. Chk2 is a tumor suppressor
that regulates apoptosis in both an ATM-dependent and ATM
independent manner.
Mol Cell Biol
2002;
22
:6521
e
32.
132. Jack MT, Woo RA, Hirao A, et al. Chk2 is dispensable for p53-
mediated G1 arrest but is required for a latent p53-mediated
apoptotic response.
Proc Natl Acad Sci USA
2002;
99
:9825
e
98.
116. Brega N, McArthur GA, Britten C, et al. Phase I clinical trial of
gemcitabine (GEM) in combination with PF00477736 (PF-736),
a selective inhibitor of Chk1 kinase.
J Clin Oncol
2010;
28
. Abst
3062.
117. Kesicki EA, Gaudino JJ, Cook AW,
et al
. Discovery of pyrazinyl
ureas as inhibitors of the cell-cycle checkpoint kinase Chk1.
e
9.
133. Hirao A, Kong YY, Matsuoka S, et al. DNA damage-induced
activation of p53 by the checkpoint kinase Chk2.
Science
2000;
287
:1824
e
7.
134. in A, Yan XJ, Rosales N, et al, in A. UCN-01 in ovary cancer
cells; effective as a single agent and in combination with
e