70677-94-0Relevant articles and documents
Design, synthesis and X-ray crystallographic study of new nonsecosteroidal vitamin D receptor ligands
Demizu, Yosuke,Takahashi, Takeo,Kaneko, Fumiya,Sato, Yukiko,Okuda, Haruhiro,Ochiai, Eiji,Horie, Kyohei,Takagi, Ken-Ichiro,Kakuda, Shinji,Takimoto-Kamimura, Midori,Kurihara, Masaaki
scheme or table, p. 6104 - 6107 (2011/11/06)
We designed and synthesized nonsecosteroidal vitamin D receptor (VDR) ligands that formed H-bonds with six amino acid residues (Tyr143, Ser233, Arg270, Ser274, His301 and His393) of the VDR ligand-binding domain. The ligand YR335 exhibited potent transcriptional activity, which was comparable to those of 1α,25-dihydroxyvitamin D3 and YR301. The crystal structure of the complex formed between YR335 and the VDR ligand-binding domain was solved, which revealed that YR335 formed H-bonds with the six amino acid residues mentioned above.
Allyl sulfides are privileged substrates in aqueous cross-metathesis: Application to site-selective protein modification
Lin, Yuya A.,Chalker, Justin M.,Floyd, Nicola,Bernardes, Goncalo J. L.,Davis, Benjamin G.
supporting information; experimental part, p. 9642 - 9643 (2009/02/04)
Allyl sulfides undergo efficient cross-metathesis in aqueous media with Hoveyda-Grubbs second generation catalyst 1. The high reactivity of allyl sulfides in cross-metathesis was exploited in the first examples of cross-metathesis on a protein surface. S-Allylcysteine was incorporated chemically into the protein, providing the requisite allyl sulfide handle. Preliminary efforts to genetically incorporate S-allylcysteine into proteins are also reported. Copyright
An expeditious synthesis of pentosidine, an advanced glycation end product
Yokokawa, Fumiaki,Sugiyama, Hideyuki,Shioiri, Takayuki,Katagiri, Noriko,Oda, Osamu,Ogawa, Hiroshi
, p. 4759 - 4766 (2007/10/03)
The chemical synthesis of pentosidine (1), an advanced glycation end product, was achieved via the asymmetric alkylation of the chiral schiff base derived from (+)-2-hydroxy-3-pinanone ((+)-HyPN) and glycine tert-butyl ester, the mercury salt mediated intramolecular guanylation, and the regioselective alkylation of imidazo[4,5-b]pyridine ring. This reliable synthetic achievement will promise availability of pentosidine (1) in quantities.
