RIKEN Center for Life Science Technologies

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To let you know about our research, this area contains 4 types of information about CLST; “Article”, “Videos”, “Event” and “Study”.
At “Article”, you can read articles on interviews and lectures, and you can enjoy the videos about CLST at “Videos”. If you want to meet and talk directly with the researcher, “Visit” give you some information of such events. You can find more difficult contents to know about our research deeply at “Study”.
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Labs & Technologies

Drug Discovery Chemistry Platform Unit

Compound profile optimization toward preclinical candidate identification

Unit Leader
Hiroo Koyama  Ph.D.

2-1 Hirosawa, Wako, Saitama 351-0198, Japan
Tel: 048-467-4206

3_16_koyama.png

Research Area

Medicinal chemistry advances the drug discovery stage

The main focus of our unit is to identify small molecule drug candidates suitable for animal safety studies and subsequent human clinical trials by medicinal chemistry. Our dedicated laboratory scientists conduct chemical synthesis for multi-dimensional compound optimization on potency to target protein, PK/PD and off-target activity profiles through SAR (Structure-Activity Relationship) development. By capitalizing on RIKEN's available expertise in protein synthesis, X-ray crystallography and computational chemistry, we strive to expedite the drug discovery process by rational drug design.

Main Publications List

1

Glycosphingolipid Ligands for Invariant Natural Killer T cells as Immunostimulants

Tashiro T, Mori K.
Studies in Natural Products Chemistry, 42, 1-31 (2014).
2

糖鎖の新機能開発・応用ハンドブック,

田代卓哉、谷口克
NKT,, (2014).
3

Synthesis and biological activity of hydroxylated analogs of RCAI-80

Shiozaki M, Tashiro T, Koshino H, Shigeura T, Watarai H, Taniguchi M, Mori K.
Tetrahedron, 69(46), 9710-9725 (2013).
4

RCAI-61 and related 6'-modified analogs of KRN7000: their synthesis and bioactivity for mouse lymphocytes to produce interferon-γ in vivo.

Tashiro T, Nakagawa R, Shigeura T, Watarai H, Taniguchi M, Mori K.
Bioorg Med Chem, 21(11), 3066-30779 (2013).
5

RCAI-133, an N-methylated analogue of KRN7000, activates mouse natural killer T cells to produce Th2-biased cytokines

Tashiro T, Shigeura T, Shiozaki M, Watarai H, Taniguchi M, Mori K.
Med Chem Comm, 4, 949-955 (2013).
6

Synthesis and biological activity of hydroxylated analogues of KRN7000 (α-galactosylceramide).

Shiozaki M, Tashiro T, Koshino H, Shigeura T, Watarai H, Taniguchi M, Mori K.
Carbohydr Res, 370, 46-66 (2013).
7

Pathogenic mutation of ALK2 inhibits induced pluripotent stem cell reprogramming and maintenance: mechanisms of reprogramming and strategy for drug identification.

Hamasaki M, Hashizume Y, Yamada Y, Katayama T, Hohjoh H, Fusaki N, Nakashima Y, Furuya H, Haga N, Takami Y, Era T.
Stem Cells, 30(11), 2437-2449 (2012).
9

PAI-1阻害薬.

橋爪良信,小原 要,稲田 進,加賀山彰,景山浩充,鯉渕 靖,吉田茂美,後藤俊男
血管医学, 12, 345-350 (2011).
10

Plasminogen activator inhibitor-1阻害薬.

橋爪良信,新保斎,菊地克史,後藤俊男,目黒寛司,宮田敏男
カレントテラピー, 29, 532-535 (2011).

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