Hokkaido University

Shionogi Company Limited

Other

Hitachi-high-technologies Corporation

Toyo Boseki Kabushiki Kaisha

Sumitomo Bakelite Company Limited

Yamasa Corporation

Shin-Ichiro Nishimura

Yoshiaki Miura

Shinya Ito

Kisaburo Deguchi

Yoshito Numata

Shoichi Naito

Susumu Nishiguchi

Naoki Ohyabu

Kuriko Yamada

Izumi Ogata

Yasuhiro Takegawa

Takahiko Matsushita

Masao Fukushima

Tatsuya Takahashi

Toshitada Noguchi

Yoshihiko Maekawa

Hideyuki Shimaoka

Hiroki Abe

Junji Onoda

Tomoki Hamamoto

Akio Takimoto

Yasuro Shinohara

Atsushi Toda

Jun-ichi Furukawa

Midori Abe

Kiyoshi Okuyama

Taichi Ueda

Keiko Kawamoto

Yoko Kita

Mika Nakano

Masataka Fumoto

Wataru Takada

Kohta Igarashi

Kentaro Naruchi

Hiroshi Hinou

Noriko Nagahori

Maho Amano

Hirofumi Nagatome

Takaomi c/o Shionogi Innovation Center For Drug Discovery Ito

The present invention pertains to a complex including nanoparticles and, carried on the surface of the nanoparticles, a lysosomal enzyme inhibitor or kinase inhibitor shown by general formula (A) and a phospholipid mimetic substance shown by general formula (B).  In general formula (A), n1 is an integer of 2-30, n2 is an integer of 2-30, the -S- terminal is a nanoparticle-carrying site, and R10 is a suicide substrate site or a kinase inhibition site. In general formula (B), n3 is an integer in the range of 2-30, and the -S- terminal is a nanoparticle-carrying site. The present invention provides a versatile system capable of efficiently delivering a drug to endolysosomes and allowing the drug to function at a low concentration on lysosomal enzymes, and an anticancer agent in which this system is used.

Intracellular substance transport system and use thereof

Cancer-associated O-glycopeptide combination epitopes derived from the VNTR of MUC1 are disclosed. Autoantibodies present in human sera target the combination epitopes and are reduced or absent in cancer patients. The epitopes are useful as therapeutic and immunoprophylactic cancer vaccines. Monoclonal antibodies directed against the epitopes are also useful as immunotherapeutics for treatment and prevention of cancer. Diagnostic methods using the epitopes and antibodies are also disclosed.

Cancer-related glycopeptide epitopes, antibodies and methods of use

A sugar chain array containing a sugar chain immobilized thereon for detecting binding between an analyte and a sugar chain, and a sugar chain array having the sugar chain immobilized thereon that is capable of inhibiting non-specific adsorption and binding of an analyte without having to coat the array with an adsorption inhibitor. A specific sugar chain is immobilized on the array, and is useful for detecting binding between the sugar chain and an analyte, such as a pathogen of an infectious disease or an excretion thereof. In addition, in the array, when a base material is coated with a polymeric compound having a unit having a primary amino group, a unit for maintaining hydrophilicity, and a unit having a hydrophobic group, the sugar chain is immobilized efficiently and non-specific adsorption and binding of the analyte can be effectively inhibited.

Sugar chain array

Provided are a biomolecule-immobilized carrier obtained by immobilizing a biomolecule having a membrane-binding peptide containing a C terminal polypeptide of fucosyltransferase derived fromor a membrane-binding molecule having the membrane-binding peptide and various biomolecules and a method for immobilizing a biomolecule to a carrier, particularly a biomolecule-immobilized magnetic microparticle, a probe-immobilized carrier using the biomolecule and/or the membrane-binding molecule are/is used as a probe, and a separating agent for a biomolecule to which the biomolecule-immobilized magnetic microparticle is applied. A biomolecule having a membrane-binding peptide containing either an amino acid sequence represented by SEQ ID NO: 1 or an amino acid sequence encoded by a base sequence represented by SEQ ID NO: 2 and/or a membrane-binding molecule having the membrane-binding peptide and the biomolecule are/is attached to a carrier coated with an organic membrane containing a phospholipid.

Biomolecule-immobilized carrier and method for immobilizing biomolecule on carrier

An objective of the present invention is to provide a MUC1 antibody having high specificity to cancer cells. The objective has been achieved by the present inventors who found that a cancer-specific sugar chain can be specifically recognized in MUC1 and a cancer cell expressing MUC1 having such a cancer cell specific sugar chain can be recognized. The present invention provides an antibody, an antigen-binding fragment thereof or a MUC1-binding molecule, having, for example, 40-fold specificity or more for a cancer-associated structure of MUC1 as compared to that of a normal tissue-associated structure of MUC1.

MUC1 antibody

An object of the present invention is to provide an antibody which does not bind to a normal cell, and is specific for a cancer cell. The object was solved by the finding by the present inventors that an antibody obtained by immunizing an animal using a 2,3ST glycopeptide as an antigen unexpectedly recognizes a sugar chain specific for a cancer specifically and remarkably, and consequently, can recognize and kill a cancer cell expressing MUC1 having such a cancer cell-specific sugar chain. The present invention provides, for example, an antibody, an antigen-binding fragment thereof or a MUC1-binding molecule, in which specificity for a cancer-associated structure of MUC1 is 100-fold or more as compared with that for a normal tissue-associated structure of MUC1.

Anti-MUC1 antibody

The present invention is directed to, for example, an oligosaccharide having at an end thereof a 4-position halogenated galactose residue represented by formula (I): (wherein X represents a halogen atom, and R represents a monosaccharide, an oligosaccharide, or a carrier), a transferase inhibitor containing the oligosaccharide, and a method for inhibiting sugar chain elongation reaction in the presence of glycosyltransferase, the method including employing the inhibitor. The invention also provides a method for producing a 4-position halogenated galactose sugar nucleotide represented by formula (II): (wherein each of Rto Rrepresents a hydroxyl group, an acetyl group, a halogen atom, or a hydrogen atom; X represents a halogen atom; and M represents a hydrogen ion or a metal ion), wherein the method employs bacterium-derived galactokinase and bacterium-derived hexose-1-phosphate uridylyltransferase. The invention is also directed to a sugar chain containing 4-position halogenated galactose envisaged to be employed as drugs and other materials, and to applications of the compound.

Sugar chain containing 4-position halogenated galactose and application thereof

A means for pre-treatment in glycomic analysis of a glycoprotein is provided by the present invention. A salt of the general formula (I): wherein Z, X, R, R, M, m and n are the same as described in DESCRIPTION,is useful as a protein solubilizer, and an oligosaccharide is efficiently released from a sample if reductive alkylation and/or digestion by a proteinase are carried out under the presence of the said solubilizer at the first step in the glycomic analysis of glycoprotein derived from a living body.

Method of serum pre-treatment for glycomic analysis

To provide a method for enhancing analysis sensitivity of bio-related molecules in mass spectrometry. To provide a method for rapidly and conveniently analyzing biological acid molecules using the method of enhanced analysis sensitivity in mass spectrometry. A method of preparing a bio-related molecule to be subjected to mass spectrometry, in which at least a part of acid group(s) is esterified, comprising reacting a bio-related molecule comprising an acid group(s) with a triazene compound to esterify at least a part of said acid group(s). A method of analyzing bio-related molecules comprising reacting a bio-related molecule comprising an acid group(s) with a triazene compound to esterify said acid group(s), and then subjecting said bio-related molecule having an esterified acid group(s) to mass spectrometry.

Method of esterifying bio-related molecule for mass spectrometry and method of mass spectrometry of obtained esterified derivative

A polymer compound having a monosaccharide or an oligosaccharide residue, or an amino acid or peptide residue bound to a monosaccharide or an oligosaccharide residue bound to a side chain of a water-soluble polymer through a linker containing a selectively cleavable bond, the water-soluble polymer containing 20 to 80 mol % of (meth)acrylic acid residue.

Water-soluble polymer compound having sugar chains

The invention intends to determine a presence ratio between mixed compounds which are difficult to separate from each other by a separation unit and cannot be discriminated by MS. In a mass spectrometer with an MSanalysis function for ionizing a sample eluted from a separation unit for separating the sample into individual components, fragmenting an ion of a desired mass number, and performing a mass analysis of fragment ions, the mass spectrometer includes a database storing correlation information between an isomer presence ratio and a particular ion intensity ratio in a mass spectrum per isomer. An isomer ratio can be clarified even for a mixed sample of isomers, such as enantiomers, which are difficult to separate from each other by the separation unit and cannot be discriminated by MS.

Mass spectrometer and method of analyzing isomers

The present invention provides a method for easily producing glycopeptides which are useful as a material for scientific studies, medicaments and foodstuffs. The glycopeptides can be produced by coupling a fluorinated glycoside of a monosaccharide or an oligosaccharide of the formula (I) with an amino acid or a peptide and then deprotecting the resultant glycopeptide by hydrogenation, and the sequential glycopeptide of the formula (IV) can be produced by polycondensation of a precursor glycopeptide.

Process for the preparation of regular glycopeptides

Processes for producing saccharide derivatives using solid ultrastrong acid

A method for producing glycoconjugate, which comprises the steps of:

Method for producing glycoconjugates

Growing community of inventors

Sapporo, Japan

Shin-Ichiro Nishimura