Mercian Corporation

Eisai R&d Management Co., Ltd.

Sanraku Incorporated

Eisai Company, Limited

Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai

Naoto Kawamura

Tomohiro Sameshima

Takashi Nakashima

Rokuro Okamoto

Satoshi Yamamoto

Hiroshi Tone

Susumu Takeda

Takashi Sakai

Motoko Matsufuji

Kazuhiko Okamura

Akifumi Okuda

Kiyoshi Okamoto

Mitsuo Nagai

Yoshihiko Kotake

Jun Niijima

Toshio Tsuchida

Masashi Yoshida

Kazuyuki Dobashi

Yoshiharu Mizui

Toshimitsu Uenaka

Takao Yamori

Masanori Fujita

Naoki Asai

Akira Arisawa

Tomonari Yamada

Keisuke Komeda

Koji Norihisa

Kumiko Kishi

Ikuo Kojima

Masao Iwata

Tomio Takeuchi

Masaaki Ishizuka

Kunio Isshiki

Hiroyuki Inoue

Tetsuya Someno

Hiroyuki Kumagai

Katsura Kaneko

Taira Kato

Tsutomu Inoue

Yasushi Okumura

The present invention provides a novel method of producing the 12-membered ring macrolide compound 11107D having an antitumor activity by biological transformation. Starting material which is the 12-membered ring macrolide compound 11107B represented by the formula (I) is incubated in the presence of a strain belonging to the genus, the genusor the family Micromonosporaceae (for example,sp. AB-1704 strain (FERM BP-8551)), each of which has the ability of transforming the 12-membered ring macrolide compound 11107B into a 11107D substance represented by the formula (II), or a preparation of its cultured myceha and oxygen, and then 11107D substance which is a target material is collected from the treating solution. 

Method of producing macrolide compound

The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution ofsp. Mer. 11107 or a variant thereof, a pharmacologically acceptable salt thereof or a hydrate of them, and a process for producing it. 

Bioactive substance

A compound represented by formula (I); a process for producing a compound (substance F-1490) of formula (I), wherein X represents &#x2014;O&#x2014; and R represents a hydroxyl group, by using a microorganism belonging to the genus; and asp. F-1490 strain (FERM BP-8287) capable of producing the substance F-1490; and an osteoclast differentiation inhibitory agent containing as an active ingredient the compound represented by formula (I): wherein X represents &#x2014;O&#x2014; or &#x2014;CH&#x2014;, and R represents a hydroxyl group when X represents &#x2014;O&#x2014;, or a hydrogen atom when X represents &#x2014;CH&#x2014;.

Osteoclast differentiation inhibitors

The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution ofsp. Mer. 11107 or a variant thereof, a pharmacologically acceptable salt thereof or a hydrate of them, and a process for producing it

Physiologically active substances

A DNA fragment or a restriction enzyme-digested DNA fragment, the DNA fragment containing a gene, acyA, encoding a 3-acylation enzyme for macrolide antibiotics, characterized by being derived from a strain belonging to the genus Streptomyces, having a size of about 1.8 kb or about 3.2 kb, and having a DNA base sequence shown in a restriction enzyme map shown in FIG. 1(A) or FIG. 1(B), respectively, in the attached drawing. 3-Acylated macrolide antibiotics can be produced advantageously using macrolide antibiotics-producing bacteria transformed with vector plasmids having inserted therein the DNA fragment.

Genes encoding a 3-acylation enzyme for macrolide antibiotics

A DNA fragment containing acyB gene coding for an enzyme capable of acylating the 4'-position of a macrolide antibiotic, said DNA fragment being derived from a microorganism of the genus Streptomyces, having a size of about 3.1 kb and being characterized by the restriction endonuclease map shown in FIG. 1 , and a DNA restriction fragment resulting from digestion with a restriction endonuclease; a recombinant DNA plasmid containing this DNA fragment; a microorganism transformed with this recombinant plasmid; and a process for producing a 4'-acylated macrolide antibiotic by using the transformant.

DNA coding for enzyme capable of acylating the 4'-position of macrolide

This invention provides a blood typing training kit comprising a red blood cell model and an antiserum model with no use of human blood in experiments for blood agglutination and in learning of blood typing, the red blood cell model being an easily available granule which can be suspended in water such as agarose bead, Sepharose, cellulose, Sephadex, cellulofine, alginate, tamarind polysaccharide, gelatin, xanthan gum, etc. or the saccharide- or protein-bound form thereof and the antiserum model being lectin, boric acid-containing liquid or immunoglobulin G.

Bloodless blood typing training kit

Growing community of inventors

Kanagawa, Japan

Naoto Kawamura