PEPTIDE-BASED REGULATION OF GAP JUNCTIONS
    1.
    发明申请
    PEPTIDE-BASED REGULATION OF GAP JUNCTIONS 审中-公开
    基于肽基的GAP结构调节

    公开(公告)号:WO2009012224A2

    公开(公告)日:2009-01-22

    申请号:PCT/US2008069980

    申请日:2008-07-14

    IPC分类号: A61K38/10

    CPC分类号: A61K38/10

    摘要: The present invention relates to proteins and polypeptides that (i) have the formula A - [Wm - A]n where each A is independently a peptide of formula XXXXRXPXXXX where each X is independently any amino acid, R is arginine, and P is proline; each W is independently a linker; m is 1 or 2; and n is any number from 1 through 5; (ii) consist essentially of the formula XnRXPXm where each X is independently any amino acid, R is arginine, P is proline, n is any number from zero to fifteen, m is any number from zero to fifteen, and the sum of n and m is any number from eight to fifteen; (iii) have the formula A - An where each A is independently a peptide of formula XXXXRXPXXXX where each X is independently any amino acid, R is arginine, and P is proline; and n is any number from 1 through 5; or (iv) consist essentially of the formula XnRXPXm where each X is independently any amino acid, R is arginine, P is proline, n is any number from zero to seven, m is any number from zero to seven, and the sum of n and m is any number from zero to seven. Methods using these proteins and polypeptides to: identify the location of an RXP -binding domain of Cx43CT, modulate a Cx43 gap junction channel, screen for compounds that modulate Cx43CT, and measure Cx43CT-binding affinity of a compound that binds to Cx43CT, are also disclosed.

    摘要翻译: 本发明涉及(i)具有式A - [Wm-A] n的蛋白质和多肽,其中每个A独立地是式XXXXRXPXXXX的肽,其中每个X独立地是任何氨基酸,R是精氨酸,P是脯氨酸 ; 每个W独立地是一个连接体; m为1或2; n是从1到5的任何数字; (ii)基本上由式XnRXPXm组成,其中每个X独立地是任何氨基酸,R是精氨酸,P是脯氨酸,n是从零到十五的任何数,m是从零到十五的任何数,以及n和 m是从8到15的任何数字; (iii)具有式A-An,其中每个A独立地是式XXXXRXPXXXX的肽,其中每个X独立地是任何氨基酸,R是精氨酸,P是脯氨酸; n是从1到5的任何数字; 或(iv)基本上由式XnRXPXm组成,其中每个X独立地是任何氨基酸,R是精氨酸,P是脯氨酸,n是从0到7的任何数字,m是从0到7的任何数字,并且n的总和 m是从零到七的任何数字。 使用这些蛋白质和多肽的方法:鉴定Cx43CT的RXP结合结构域的位置,调节Cx43间隙连接通道,筛选调节Cx43CT的化合物和测量与Cx43CT结合的化合物的Cx43CT结合亲和力,也是 披露。

    IMPROVED SOLID-PHASE PEPTIDE SYNTHESIS AND AGENT FOR USE IN SUCH SYNTHESIS
    6.
    发明申请
    IMPROVED SOLID-PHASE PEPTIDE SYNTHESIS AND AGENT FOR USE IN SUCH SYNTHESIS 审中-公开
    改进的固相肽合成和用于此类合成的试剂

    公开(公告)号:WO1998011125A1

    公开(公告)日:1998-03-19

    申请号:PCT/DK1997000375

    申请日:1997-09-09

    IPC分类号: C07K01/04

    CPC分类号: C07K1/042 C07K1/04 Y02P20/55

    摘要: Peptides X-AA1-AA2...AAn-Y, wherein AA is an L- or D-amino acid residue, X is hydrogen or an amino protective group, Y is OH, NH2 or an amino acid sequence comprising from 3 to 9 amino acid residues and n is an integer greater than 2, are prepared by solid phase synthesis, preferably using Fmoc-chemistry, the improvement consisting in that the C-terminal part attached to the solid phase comprises a pre-sequence comprising from 3 to 9, preferably from 5 to 7, amino acid residues independently selected from native L-amino acids having a side chain functionality which is suitably protected during the coupling steps and having a propensity factor P alpha > 0.57 and a propensity factor P beta > 1.10, preferably Lys and/or Glu, or the corresponding D-amino acids and said pre-sequence is optionally cleaved from the formed peptide.

    摘要翻译: 肽X-AA1-AA2 ... AAn-Y,其中AA是L-或D-氨基酸残基,X是氢或氨基保护基,Y是OH,NH2或包含3至9的氨基酸序列 氨基酸残基和n是大于2的整数,通过固相合成制备,优选使用Fmoc化学,其改进在于连接到固相的C末端部分包含3至9个的前序列 ,优选5-7个氨基酸残基,其独立地选自具有侧链官能度的天然L-氨基酸,所述天然L-氨基酸在偶联步骤期间被适当地保护并且具有倾向因子Pα> 0.57和倾向因子Pβ> 1.10,优选地 Lys和/或Glu,或相应的D-氨基酸和所述前序列任选地从形成的肽切割。

    PEPTIDE-BASED REGULATION OF GAP JUNCTIONS
    9.
    发明申请

    公开(公告)号:WO2009012224A3

    公开(公告)日:2009-01-22

    申请号:PCT/US2008/069980

    申请日:2008-07-14

    IPC分类号: C07K14/00

    摘要: The present invention relates to proteins and polypeptides that (i) have the formula A - [Wm - A]n where each A is independently a peptide of formula XXXXRXPXXXX where each X is independently any amino acid, R is arginine, and P is proline; each W is independently a linker; m is 1 or 2; and n is any number from 1 through 5; (ii) consist essentially of the formula X n RXPX m where each X is independently any amino acid, R is arginine, P is proline, n is any number from zero to fifteen, m is any number from zero to fifteen, and the sum of n and m is any number from eight to fifteen; (iii) have the formula A - A n where each A is independently a peptide of formula XXXXRXPXXXX where each X is independently any amino acid, R is arginine, and P is proline; and n is any number from 1 through 5; or (iv) consist essentially of the formula X n RXPX m where each X is independently any amino acid, R is arginine, P is proline, n is any number from zero to seven, m is any number from zero to seven, and the sum of n and m is any number from zero to seven. Methods using these proteins and polypeptides to: identify the location of an RXP -binding domain of Cx43CT, modulate a Cx43 gap junction channel, screen for compounds that modulate Cx43CT, and measure Cx43CT-binding affinity of a compound that binds to Cx43CT, are also disclosed.