絞り込み

16514

広告

“賛否両論の登山家”栗城史多さんとは何者だったのか | 文春オンライン

登山家の栗城史多さんがエベレストで亡くなった。これを書いている5月22日現在では、死因などについての詳しい情報が入ってきていないので、事故についてはなにもわから...

  1. [医学] LRRK2キナーゼの結核菌助長...
  2. 東急不動産が再エネ事業に本腰、全国で40...
  3. 高い場所にいる人ほど、リスクが高い決断を...
  4. 6月22日にプライベートセミナー開催 ビ...

ニュース一覧

Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide.

著者 Lopez-Girona A , Mendy D , Ito T , Miller K , Gandhi AK , Kang J , Karasawa S , Carmel G , Jackson P , Abbasian M , Mahmoudi A , Cathers B , Rychak E , Gaidarova S , Chen R , Schafer PH , Handa H , Daniel TO , Evans JF , Chopra R
Leukemia.2012 May 3 ; ():.
この記事をPubMed上で見るPubMedで表示
この記事をGoogle翻訳上で見る Google翻訳で開く

Celgene, San Diego, California, USA.

スターを付ける スターを付ける     (739view , 0users)

Full Text Sources

Miscellaneous

Other Literature Sources

Research Materials

DF15R (CVCL_Y430)

DF15 (CVCL_Y429)

Thalidomide and the immunomodulatory drug, lenalidomide, are therapeutically active in hematological malignancies. The ubiquitously expressed E3 ligase protein cereblon (CRBN) has been identified as the primary teratogenic target of thalidomide. Our studies demonstrate that thalidomide, lenalidomide and another immunomodulatory drug, pomalidomide, bound endogenous CRBN and recombinant CRBN-DNA damage binding protein-1 (DDB1) complexes. CRBN mediated antiproliferative activities of lenalidomide and pomalidomide in myeloma cells, as well as lenalidomide- and pomalidomide-induced cytokine production in T cells. Lenalidomide and pomalidomide inhibited autoubiquitination of CRBN in HEK293 T cells expressing thalidomide-binding competent wild-type CRBN, but not thalidomide-binding defective CRBN(YW/AA). Overexpression of CRBN wild-type protein, but not CRBN(YW/AA) mutant protein, in KMS12 myeloma cells, amplified pomalidomide-mediated reductions in c-myc and IRF4 expression and increases in p21(WAF-1) expression. Long-term selection for lenalidomide resistance in H929 myeloma cell lines was accompanied by a reduction in CRBN, while in DF15R myeloma cells resistant to both pomalidomide and lenalidomide, CRBN protein was undetectable. Our biophysical, biochemical and gene silencing studies show that CRBN is a proximate, therapeutically important molecular target of lenalidomide and pomalidomide.Leukemia accepted article preview online, 3 May 2012 doi:10.1038/leu.2012.119.
PMID: 22552008 [PubMed - as supplied by publisher]
印刷用ページを開く Endnote用テキストダウンロード