Innovation in the Identifications of Drug-targets using Affinity Resins
1) T. Tamura, T. Terada, A.Tanaka. A Quantitative Analysis and Chemical
Approach for the Reduction of Nonspecific
Binding Proteins on Affinity Resins. Bioconjugate Chem., 14(6), 1222-1230
(2003).
2) T. Shiyama, M. Furuya, A. Yamazaki, T. Terada, A.Tanaka. Design and
Synthesis of Novel Hydrophilic Spacers for the Reduction of Nonspecific
Binding Proteins on Affinity Resins. Bioorg. Med. Chem., 12(11), 2831-2841
(2004).
3) T. Takahashi, T. Shiyama, K. Hosoya, A.Tanaka. Development of Chemically
Stable Solid-phases for the Target Isolation with Reduced Nonspecific Binding
Proteins. Bioorg. Med. Chem. Lett., 16(2), 447-450 (2006).
4) K. Yamamoto, A. Yamazaki, M. Takeuchi, A.Tanaka. A versatile method
of identifying specific binding proteins on affinity resins. Anal. Biochem.,
352(1), 15-23 (2006).
5) M. Furuya, M. Haramura, A.Tanaka. Reduction of Nonspecific Binding Proteins
to Self-assembled Monolayer on Gold Surface. Bioorg. Med. Chem., 14(2),
537-543 (2006).
6) Mori, K. Hosoya, A.Tanaka. Isolation of the Whole Target Proteins of FK506 using Affinity Resins from Novel Solid Phases. Anal. Bioanal. Chem. 385(1), 122-127 (2006).
7) T. Mori, T. Takahashi, T. Shiyama, A. Tanaka, N. Hira, N. Tanaka, K.
Hosoya. An easy preparation of 'monolithic type' hydrophilic solid phase:
Capability ofr affnity resin to isolate target proteins. Bioorg. Med. Chem.
14(16), 5549-5554 (2006).
8) 原村昌幸、田中明人. 古くて新しいテーマ：アフィニティ樹脂による網羅的ターゲット探索〜非特異的蛋白質の抑制〜.
ゲノム医学、5 (2), 191-195 (2004).
9) 東山喜三彦、土屋耕一、原村昌幸、田中明人. SDS-PAGEゲル内タンパク質を高感度かつ安定的に同定するMSシステム構築の試み.
J. Mass Spectrom. Soc. Jpn. 54(3), 109-115 (2006).
10) E. Iwaoka, T. Mori, T. Shimizu, K. Hosoya, A. Tanaka. Improvement of
monolithic solid material by utilization of spacer for identification of
the target using affinity resins. Bioorg. Med. Chem. Lett. 19, 1469-1472 (2009)
11) R. Furumai, A. Matsuyama, N. Kobashi, K. H. Lee, M. Nishiyama, H. Nakajima,
A. Tanaka, Y. Komatsu, N. Nishino, M. Yoshida, S. Horinouchi. FK228 (depsipeptide)
as a natural prodrug that inhibits class I histone deacetylases. Cancer
Res. 62(17), 4916-4921 (2002).
12) A.Tanaka. Identification of the Specific Binding Proteins of Bioactive
Small Compound Using Affinity resins. Methods in Molecular Biology, 577,
181-195 (2009).
13) Miyuki Mabuchi, Masayuki Haramura, Tadashi Shimizu, Akito Tanaka. Selective elution of target protein from affinity resins by a simple
reductant with a thiol group. Bioorg. Med. Chem. Lett. 20(24), 7361-7364 (2010)
14) Miyuki Mabuchi, Tadashi Shimizu, Masahiro Ueda, Kuniko Mitamura, Shigeo
Ikegawa,Akito Tanaka. SImprovement of solid material for affinity resins
by application of long PEG spacers to capture the whole target complex
of FK506. Bioorg. Med. Chem. Lett. 25, 2788-2792 (201)
15) Miyuki Mabuchi, Tadashi Shimiz, Masayuki Haramura, Akito Tanaka. SIdentification
and purification of target protein using affinity resin bearing a photo-labile
linker. Bioorg. Med. Chem. Lett. 25, 3373-3377(2015)
Medicinal Chemistry: PCA-1 inhibitor(HUHS015)
1) S. Nakao, M. Mabuchi, T. Shimizu, Y. Itoh, Y. Takeuchi, M. Ueda, H.
Mizuno, N. Shigi, I. Ohshio, K. Jinguji, Y. Ueda, M. Yamamoto, T. Furukawa,
S. Aoki, K. Tsujikawa, A. Tanaka, “Design and synthesis of prostate cancer
antigen-1 (PCA-1/ALKBH3) inhibitors as anti-prostate cancer drugs”, Bioorganic
& Medicinal Chemistry Letters 24 (2014) 1071?1074.
2) Mabuchi M, Shimizu T, Ueda M, Sasakawa Y, Nakao S, Ueda Y, Kawamura
A, Tsujikawa K, Tanaka A."Improving the Bioavailability and Anticancer Effect of the PCA-1/ALKBH3
Inhibitor HUHS015 Using Sodium Salt”, In Vivo, 29(1), 39-43 (2015).
FR122047 (specific COX1 inhibitor)
9) Tanaka A, Ito K, Nishino S, Motoyama Y, Takasugi H Studies on Antiplatelet Agents. I. Synthesis and Platelet Inhibitory Activity of 5-Alkyl-2-aryl-4-pyridylimidazoles. Chem. Pharm. Bull., 40(12), 3206-3213 (1992).
10) Dohi M, Sakata Y, Seki J, Namikawa Y, Fujisaki J, Tanaka A, Takasugi
H, Motoyama Y, Yoshida K. The anti-platelet actions of FR122047, a novel
cyclooxygenase inhibitor. Eur J Pharmacol. 243(2), 179-184 (1993).
11) Tanaka A, Ito K, Nishino S, Motoyama Y, Takasugi H. Studies on Antiplatelet
Agents. II. Synthesis and Platelet-Inhibitory Activity of 5-Methyl-4-(3-pyridyl)-2-(substituted-Benzimidazol
-5-yl)imidazoles. Chem. Pharm. Bull., 42(3), 560-569 (1994).
12) Tanaka A, Motoyama Y, Takasugi H. Studies on Antiplatelet Agents. IV.
A Series of 2-Substituted 4,5-Bis-(4-methoxyphenyl)-pyrimidines as Novel
Anti-platelet Agents. Chem. Pharm. Bull., 42(9), 1828-1834 (1994).
13) Tanaka A, Sakai H, Ishikawa T, Motoyama Y, Takasugi H. Studies on Antiplatelet
Agents. V. Synthesis and Structure-Activity Relationship of 3-Substituted
5,6-Bis(4-methoxyphenyl)-1,2,4 -triazines. Chem. Pharm. Bull., 42(9), 1835-1840
(1994).
14) Tanaka A, Sakai H, Motoyama Y, Ishikawa T, Takasugi H. Antiplatelet
Agents Based on Cyclooxygenase Inhibition without Ulcerogenesis. Evaluation
and Synthesis of 4,5-Bis(4-methoxyphenyl)-2-substituted-thiazoles. J. Med.
Chem., 37(8), 1189-1199 (1994).
FK633 (specific GPIIb/IIIa antagonist
15) Aoki T, Cox D, Senzaki K, Seki J, Tanaka A, Takasugi H, Motoyama Y.
The Anti-platelet and Anmti-Thrombotic Effects of FK633, A Peptide-Mimetic
GPIIb/IIIa Antagonist. Thromb. Res., 81(4), 439-450 (1996).
16) Tanaka A, Rational drug design of the fibrinogen inhibitors FK633 and
FR158999. Drugs of the Future 23(3), 291-299 (1998).
17) Aoki T, Cox D, Senzaki K, Seki J, Tanaka A, Takasugi H, Motoyama Y.
Comparison of the antithrombotic effects of FK633, GPIIb/IIIa antagonist,
and aspirin in a guinea pig thrombosis model. Thromb. Res. 89(3), 129-136
(1998).
18) Aoki T, Tomiyama Y, Honda S, Senzaki K, Tanaka A, Okubo M, Takahashi
F, Takasugi H, Seki J. Difference of (Ca2+)i movements in platelets stimulated
by thrombin and TRAP. The involvement of aIIbIII-mediated TXA2 synthesis.
Thromb. Haemostasis, 79(6), 1184-1190 (1998).
19) T. Aoki, K. Harada, J. Seki, A. Tanaka, H. Takasugi, Y. Motoyama FK633:
a potent and selective platelet GPIIb/IIIa antagonist. Cardiovasc. Drug
Rev., 17(2), 147-159 (1999).
Visiting Scientist for Stuart L. Schreiber Labs in Harvard University
1) Albers MW, Williams RT, Brown EJ, Tanaka A, Hall FL, Schreiber SL. FKBP-Rapamycin
Inhibits a Cyclin-dependent Kinase Activity and a Cyclin D1-Cdk. Association
in Early G1 of an Osteosarcoma Cell. J. Biol. Chem., 268(30), 22825-22829
(1993).
2) Albers MW, Brown EJ, Tanaka A, Williams RT, Hall FL, Schreiber SL. An
FKBP-Rapamycin-Sensitive, Cyclin-Dependent Kinase Activity that Correlates
with the FKBP-Rapamycin-Induced G1 Arrest Point in MG-63 Cells. Ann N Y
Acad Sci. 696, 54-62 (1993).
3) J. K. Chen, W. S. Lane, A. W. Brauer, A. Tanaka, S. L. Schreiber. Biased
Combinatorial Libraries: Novel Ligands for the SH3 Domain of Phosphatidylinositol
3-Kinase. J. Amer. Chem. Soc., 115(26), 12591-12592 (1993).
4) F. A. Gomez, J. K. Chen, A. Tanaka, S. L. Schreiber, G. M. Whitesides.
Affinity Capillary Electrophoresis: Insights into the Binding of SH3 Domains
by Peptides. Derived from an SH3-Binding Protein. J. Org. Chem., 59(10),
2885-2886 (1994).
Development of Novel Descriptor for Hydrophobicity: logPmw (water/micellar)
1) Tanaka A, Nakamura K, Nakanishi I, Fujiwara H. A Novel and Useful Descriptor
for Hydrophobicity,Partition Coefficient Micellar-Water, and Its Application
to A QSAR Study of Antiplatelet Agents. J. Med. Chem., 37(26), 4563-4566
(1994).
2) Tanaka A, Fujiwara H. Quantitative Structure-Activity Relationship Study
of Fibrinogen Inhibitors, 4-(4-Amidinophenoxy)butanoylaspartylvaline (FK633)
Derivatives, Using A Novel Hydrophobic Descriptor. J. Med. Chem., 39(25),
5017-5020 (1996).
3) Tanaka A, Murata M, Fujiwara H. QSAR Study of the Peptidic Fibrinogen
Inhibitors FK633, FR158999 and Related Derivatives, Using a Novel and Useful
Hydrophobic Descriptor (logPmw ).Bioorg. Med. Chem Lett. 8(18), 2483-2488
(1998).
SBDD & Rational Drug Design
1) Akito Tanaka, Hiroyoshi Sakai, Takatoshi Ishikawa, Isao Nakanishi, Mitsuru
Ohkubo, Toshiaki Aoki, Yukio Motoyama and Hisashi Takasugi. Design, Synthesis,
and Evaluation of Fibrinogen Inhibitors, -(p-Amidinophenoxy)alkanoylaspartic
acid Derivatives. Bioorg. Med. Chem. Lett., 6(13), 1443-1448 (1996).
2) Tanaka A, Hiroyoshi Sakai, Takatoshi Ishikawa, Toshiaki Aoki, Yukio
Motoyama, Hisashi Takasugi Design, Synthesis, and Evaluation of Orally
Active Fibrinogen Inhibitors. Bioorg. Med. Chem Lett. 7(5), 521-526 (1997).
3) Tanaka A, Rational drug design of the fibrinogen inhibitors FK633 and
FR158999. Drugs of the Future 23(3), 291-299 (1998).
4) Hitoshi Oyasu, Isao Nakanishi, Akito Tanaka, Kenji Murano, Masaaki Matsuo.
Conformational studies on the four stereoisomers of the novel anticholinergic
4-(dimethylamino)-2-phenyl-2 -(2-pyridyl)pentanamide. J.Comput.-Aided Mol.
Des., 9(2), 171-180 (1995).
5) T. Takagi, A. Tanaka, S. Maeda, S. Matsuo, H. Fujiwara, Y. Sasaki. A Novel Development for the Simulator of Intermolecular Potentials. Bull. Chem. Soc. Jpn., 59, 1317-1320 (1986).
6) T. Takagi, A. Tanaka, S. Matsuo, H. Maezaki, M. Tani, H. Fujiwara, Y.
Sasaki. Computational Studies on CH/π Interactions. J. Chem. Soc. Perkin
Trans. II, 1015-1018 (1987).
7) T. Takagi, A. Tanaka, M. Tani, H. Maezaki, H. Fujiwara, Y. Sasaki Development
and Applications for the Simulator of Intermolecular Potentials. II. Hydration
Effects on the Conformation of Tyramine. Bull. Chem. Soc. Jpn., 61(2),
329-332 (1988).
Combinatorial Chemistry
1) J. K. Chen, W. S. Lane, A. W. Brauer, A. Tanaka, S. L. Schreiber. Biased
Combinatorial Libraries: Novel Ligands for the SH3 Domain of Phosphatidylinositol
3-Kinase. J. Amer. Chem. Soc., 115(26), 12591-12592 (1993).
2) K.Mikami, K. Ding, A. Ishii, A. Tanaka, N. Sawada, K. Kudo. Super High
Throughput Screening (SHTS) of Combinatorial Libraries of Chiral Ligands
and Activators by HPLC-CD and Combinatorial Chemistry Factory. Chromatography,
20(1), 65-70 (1999).
Others
1) M. Haramura, A. Tanaka, T. Akimoto, N. Hirayama. Crystal Structure of
Vigabatrin. Anal.Sci.19, x9-x10 (2003).
2) M. Haramura, A. Tanaka, T. Akimoto, N. Hirayama. Crystal Structure of
Dichlorphenamide. Anal. Sci. 19, x35-x36 (2003).
3) M. Haramura, A. Tanaka, T. Akimoto, N. Hirayama. Crystal Structure of
Clobetasol Propionate. Anal. Sci. 19, x37-x38 (2003).
4) M. Haramura, A. Tanaka, T. Akimoto, N. Hirayama. Crystal Structure of
Streptozocin. Anal. Sci. 19, x77-x78 (2003).
5) K. Horio, R. Tanaka, H. Akama, M. Haramura, A. Tanaka, T. Akimoto, N.
Hirayama. Crystal Structure of Carisoprodol. Anal. Sci. 20, x43-x44 (2004).
6) R. Tanaka, K. Horio, M. Haramura, A. Tanaka, N. Hirayama. Structure
of Nifenazone. Anal. Sci. 20, x171-x172 (2004).
7) R. Tanaka, M. Haramura, A. Tanaka N. Hirayama. Structure of Gefitinib.
Anal. Sci. 20, x173-x174 (2004).
8) R. Tanaka, M. Haramura, A. Tanaka, T. Akimoto, N. Hirayama. Crystal
Structure of 2-(3-Carboxypropyl)-6-(4-hydroxyphenyl)-3H-pyridazin -3-ylidene-ammonium
bromide . Anal. Sci. 20, x41-x42 (2004).
9) R. Tanaka, T. Akimoto, M. Haramura, A. Tanaka, N. Hirayama. Crystal
Structure of Minoxidil. Anal. Sci. 20, x29-x30 (2004).
10) R. Tanaka, T. Akimoto, M. Haramura, A. Tanaka, N. Hirayama. Crystal
Structure of Dantrolene. Anal. Sci. 20, x97-x98 (2004).
11) R. Tanaka, T. Akimoto, M. Haramura, A. Tanaka, N. Hirayama. Crystal
Structure of Hydroflumethiazide. Anal. Sci. 20, x139-x140 (2004).
12) R. Tanaka, M. Haramura, A. Tanaka, N. Hirayama. Structure of Trimetazidine.
Anal. Sci. 21, x3-x4 (2005).
13) R. Tanaka, M. Haramura, A. Tanaka, N. Hirayama. Structure of Guanethidine
Monosulfate. Anal. Sci. 21, x111-x112 (2005).
14) R. Tanaka, M. Haramura, A. Tanaka, N. Hirayama. Structure of Nadolol.
Anal. Sci. 21, x159-x160 (2005).
15) R. Tanaka, M. Haramura, A. Tanaka, N. Hirayama. Structure of Flurandrenolide.
Anal. Sci. 21, x161-x162 (2005).
16) R. Tanaka, M. Haramura, A. Tanaka, N. Hirayama. Structure of Pimethixene
Maleate. Anal. Sci. 21, x163-x164 (2005).
17) R. Tanaka, M. Haramura, A. Tanaka, N. Hirayama. Structure of Etophylline.
Anal. Sci. 21, x165-x166 (2005).
18) R. Tanaka, M. Haramura, A. Tanaka, N. Hirayama. Structure of Fipexide Hydrochloride Monohydrate. Anal. Sci. 22, x31-x32 (2006).
