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HEMAGGLUTININ-BINDING PEPTIDE AND PROPHYLACTIC/THERAPEUTIC AGENT FOR INFLUENZA VIRUS INFECTION WHICH CONTAINS SAME

Foreign code F180009378
File No. (S2016-1047-N0)
Posted date Apr 19, 2018
Country WIPO
International application number 2017JP030158
International publication number WO 2018038168
Date of international filing Aug 23, 2017
Date of international publication Mar 1, 2018
Priority data
  • P2016-164971 (Aug 25, 2016) JP
Title HEMAGGLUTININ-BINDING PEPTIDE AND PROPHYLACTIC/THERAPEUTIC AGENT FOR INFLUENZA VIRUS INFECTION WHICH CONTAINS SAME
Abstract A hemagglutinin-binding peptide is a tetravalent peptide, in which a peptide motif represented by SEQ ID NO: 1 is bound, directly or with a spacer interposed therebetween, to each of four amino groups located at terminals of a molecule core structure formed by binding three lysine (Lys) residues to one another.
Outline of related art and contending technology BACKGROUND ART
A influenza virus, has strong infectivity, including Japan in the world each year causing epidemic season. On the other hand, as seen in year 2009 with a new appearance or influenza virus, H5N1, H7N7 of a high-pathogenic avian influenza virus infectivity of the acquisition of the feared to humans and, in a global pandemics fatal one that is not even the inaccurate.
However, are currently used in general osetamibiru (trade name: (registered trademark) Tamiflu), zanamivirin (trade name: Relenza (registered trademark) ) such as neuraminidase inhibitors to rapidly (neuraminidase; NA) and the spreading resistance in the, urgent to establish a new influenza of the therapeutic agent has been obtained.
A surface of the particles of the influenza virus type, virus hemagglutinin involved in binding to the target cells (hemagglutinin; 'HA' and is sometimes less), and the nascent virus particles detached from the infected cells associated with one of membrane-bound glycoprotein NA 2 is known to exist.
Further, the HA, after the virus attached to the target cells, and the target cell membrane cause fusion of the viral membrane, cytoplasmic virus genes responsible for the release and also serves to, play an essential role in growth cycle of the virus is known. In addition, a number of HA is an influenza vaccine antigen.
From the above, as a target HA discovery suggests the importance of what is, at present, a targeted therapeutic agent HA still is not available on the market.
HA is a structure in which a virus on the membrane and the amount 3, HA1 molecules present on the host cell membrane glycoproteins and glycolipids of the 1 molecule to recognize and bind sialic acid. Therefore, a total amount of HA3 3 molecules may bind sialic acid. At this time, 1:1 3:3 is compared with the binding of the binding, binding affinity may be increased to several thousand times are known, this phenomenon is' effect of clusters' is called. For this reason, the conventional low molecular weight of the compound library screening, techniques such as phage in principle cannot be applied only to 1:1 interaction, the effect of the HA cluster and to function, its receptor binding site as the target to identify an inhibitor is very difficult in principle. In fact, there is no acquisition of a low molecular weight compound is, the cyclic peptide library phage (Patent Document 1) or (Patent Document 2) acquired by the HA-binding peptides are reported in the example, cluster HA directly based on the effect of receptor-binding site is an example of the isolated inhibitory peptide as a target has not been reported.
On the other hand, the inventors of the present invention, up to this point, the cluster based upon the effects of a molecule that inhibits the strong interaction screening a library method as a technique developed by the multi-value type (Patent Document 3). Polyhydric-peptide libraries, the core structure 4 is coupled to the random value of 4 for a structure in which the present invention, the effect of the cluster itself. In addition, the function and effect of this cluster to the development of the inhibitory molecule for a variety of molecules are successful (for example, JP-4-6).
Further, the inventors of the present invention, a library method is applied to a multi-value type, polyhydric-type peptide synthesized on a sheet level of several hundred established technique (Patent Document 7).
Scope of claims (In Japanese)[請求項1]
3つのリジン(Lys)が結合して形成された分子核構造の端部に位置する4つのアミノ基の各々に、配列番号1のペプチドモチーフが、直接またはスペーサーを介して結合している4価ペプチドであることを特徴とするヘマグルチニン結合ペプチド。
[請求項2]
配列番号1のペプチドモチーフのN末端側に位置するアルギニン(Arg)が、非天然異性体(D-Arg)に置換されていることを特徴とする請求項1のヘマグルチニン結合ペプチド。
[請求項3]
請求項1または2のヘマグルチニン結合ペプチドを含有することを特徴とするインフルエンザウイルス感染症の予防・治療薬。
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • THE DOSHISHA
  • Inventor
  • NISHIKAWA Kiyotaka
  • TAKAHASHI Miho
  • OHMI Junpei
  • YAMASHITA Makoto
  • HONGO Katsura
  • NATORI Yasuhiro
  • CHING-YI Tseng
IPC(International Patent Classification)
Specified countries National States: AE AG AL AM AO AT AU AZ BA BB BG BH BN BR BW BY BZ CA CH CL CN CO CR CU CZ DE DJ DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JO JP KE KG KH KN KP KR KW KZ LA LC LK LR LS LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PA PE PG PH PL PT QA RO RS RU RW SA SC SD SE SG SK SL SM ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN ZA ZM ZW
ARIPO: BW GH GM KE LR LS MW MZ NA RW SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ RU TJ TM
EPO: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW KM ML MR NE SN ST TD TG

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