-
1
-
-
67650073265
-
-
While the initial rationale for developing a CDK2 selective inhibitor inspired the undertaking of this work, the continuing examination of the cell cycle has revealed that the roles of the CDKs are more complex. Reviews on the more recent aspects may be found in: S. Lapenna, and A. Giordano Nat. Rev. Drug Disc. 8 2009 547
-
(2009)
Nat. Rev. Drug Disc.
, vol.8
, pp. 547
-
-
Lapenna, S.1
Giordano, A.2
-
8
-
-
10744231650
-
-
J.J. Liu, A. Dermatakis, C. Lukacs, F. Konzelmann, Y. Chen, U. Kammlott, W. Depinto, H. Yang, X. Yin, Y. Chen, A. Schutt, M.E. Simcox, and K.C. Luk Bioorg. Med. Chem. Lett. 13 2003 2465
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 2465
-
-
Liu, J.J.1
Dermatakis, A.2
Lukacs, C.3
Konzelmann, F.4
Chen, Y.5
Kammlott, U.6
Depinto, W.7
Yang, H.8
Yin, X.9
Chen, Y.10
Schutt, A.11
Simcox, M.E.12
Luk, K.C.13
-
9
-
-
77956915961
-
-
U.S. Patent 6
-
Ding, Q.; Liu, J. J.; Pizzolato, G.; Wei, C. C.; Wovkulich, P. U.S. Patent 6,440,959, 2002.
-
(2002)
, vol.440
, pp. 959
-
-
Ding, Q.1
Liu, J.J.2
Pizzolato, G.3
Wei, C.C.4
Wovkulich, P.5
-
10
-
-
0001463034
-
-
L.H. Sternbach, R.I. Fryer, O. Keller, W. Metlesics, G. Sach, and N. Steiger J. Med. Chem. 6 1963 261
-
(1963)
J. Med. Chem.
, vol.6
, pp. 261
-
-
Sternbach, L.H.1
Fryer, R.I.2
Keller, O.3
Metlesics, W.4
Sach, G.5
Steiger, N.6
-
11
-
-
77956938744
-
-
L.H. Sternbach, G. Saucy, F.A. Smith, M. Mueller, and J. Lee Helv. Chim. Acta 46 1963 1720
-
(1963)
Helv. Chim. Acta
, vol.46
, pp. 1720
-
-
Sternbach, L.H.1
Saucy, G.2
Smith, F.A.3
Mueller, M.4
Lee, J.5
-
13
-
-
0000165443
-
-
L.H. Sternbach, R.I. Fryer, W. Metlesics, G. Sach, and A. Stempel J. Org. Chem. 27 1962 3781
-
(1962)
J. Org. Chem.
, vol.27
, pp. 3781
-
-
Sternbach, L.H.1
Fryer, R.I.2
Metlesics, W.3
Sach, G.4
Stempel, A.5
-
14
-
-
0038761719
-
-
L.H. Sternbach, R.I. Fryer, W. Metlesics, E. Reeder, G. Sach, G. Saucy, and A. Stempel J. Org. Chem. 27 1962 3788
-
(1962)
J. Org. Chem.
, vol.27
, pp. 3788
-
-
Sternbach, L.H.1
Fryer, R.I.2
Metlesics, W.3
Reeder, E.4
Sach, G.5
Saucy, G.6
Stempel, A.7
-
16
-
-
77956926985
-
-
note
-
Crystals of the CDK2:3a complex were grown at 4 °C by the vapor diffusion method. CDK2(1-298) at 12 mg/mL was mixed with a five molar excess of compound and equilibrated against 10% PEG 3350, 0.2 M ammonium fluoride, 0.1 M Tris pH 8.5. 0.2% DTT was added to the reservoir after mixing of the drop. Cryoprotectant was the same as the reservoir with 20% PEG 3350 and the addition of 15% ethylene glycol. X-ray data was collected at beamline X8C at Brookhaven National Laboratories. Data was processed to 2.0 with the HKL package (Otwinowski, Z., Minor, W. Methods Enzymol. 1997, 276, 307). The structure was determined by molecular replacement using AmoRe (Navaza, J. Acta Crystallogr. 1994, A50, 157) and was refined with CNX (CNX v.99.0-BETA, Molecular Simulations Inc.) to an R-factor/Rfree of 0.196/0.243. The structure has been deposited to the PDB with the code 3LE6.
-
-
-
-
19
-
-
0030952289
-
-
W. Risau Nature 386 1997 671
-
(1997)
Nature
, vol.386
, pp. 671
-
-
Risau, W.1
-
21
-
-
33748376678
-
-
M. Muruganandham, M. Lupu, J.P. Dyke, C. Matei, M. Linn, K. Packman, K. Kolinsky, B. Higgins, and J.A. Koutcher Mol. Cancer Ther. 5 2006 1950
-
(2006)
Mol. Cancer Ther.
, vol.5
, pp. 1950
-
-
Muruganandham, M.1
Lupu, M.2
Dyke, J.P.3
Matei, C.4
Linn, M.5
Packman, K.6
Kolinsky, K.7
Higgins, B.8
Koutcher, J.A.9
-
22
-
-
77956903560
-
-
1/2 = 2.7 h.
-
1/2 = 2.7 h.
-
(2005)
17th AACR-NCI-EORTC Int Conf Mol Targets Cancer Ther
-
-
Higgins, B.1
Kolinsky, K.2
Yang, H.3
Tovar, C.4
Carvaial, D.5
Yin, X.6
Bachynsky, M.7
Margolis, R.8
Nevins, T.9
Geng, W.10
Lamb, M.11
Linn, M.12
Liu, J.J.13
Wovkulich, P.14
Packman, K.15
Ju, G.16
|