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    • 4. 发明申请
    • Fluorescent ligands for GPCR arrays
    • GPCR阵列的荧光配体
    • US20050009205A1
    • 2005-01-13
    • US10741213
    • 2003-12-19
    • Ye FangYulong HongJinlin Peng
    • Ye FangYulong HongJinlin Peng
    • C07K7/08C07K14/63G01N33/543
    • G01N33/582C07K7/083C07K14/63G01N33/6845G01N33/74G01N2333/63G01N2333/726
    • A fluorescent ligand includes a material having a binding affinity in the range of about 0.01 to about 25 nM, or about 0.1 to about 10 nM; a specificity to its cognate receptor in the range of about 50 to about 99%, or about 65 to about 99%; a cross-activity to other receptors of 0 to about 20%, or 0 to about 10%; a net charge per ligand of about −3 to about +5, or more preferably, about −2 to about +2 or most preferably for small compound ligands about −1 to about +2. The ligand may also have a hydrophobicity in the range of about 3 to about 55 minutes eluting time (as measured under specified eluting conditions). In some embodiments, the ligand including fluorescently labeled motilin 1-16 labeled with Bodipy-TMR, rhodamine or Cy5-. Other embodiments include fluorescently labeled Cy5-naltrexone, Cy5-neurotensin 2-13, N-terminal labeled neurotensin 2-13 or lys-labeled labeled neurotensin 2-13.
    • 荧光配体包括具有约0.01至约25nM,或约0.1至约10nM范围内的结合亲和力的材料; 在约50至约99%,或约65至约99%的范围内对其同源受体的特异性; 与其他受体的交叉活性为0至约20%,或0至约10%; 每个配体的净电荷为约-3至约+5,或更优选约-2至约+2,或最优选约为-1至约+2的小化合物配体。 配体还可以具有约3至约55分钟洗脱时间(在规定的洗脱条件下测量)的疏水性。 在一些实施方案中,配体包括用Bodipy-TMR,罗丹明或Cy5-标记的荧光标记的胃动素1-16。 其他实施方案包括荧光标记的Cy5-纳曲酮,Cy5-神经丝氨酸2-13,N-末端标记的神经丝氨酸蛋白酶2-13或lys-标记的标记的神经丝氨酸素2-13。
    • 8. 发明申请
    • PEPTIDE HAVING AN EXTENDING ACTION FOR HALF-LIFE OF OBJECT PEPTIDE IN PLASMA
    • 具有等离子体对象肽半衰期的延伸作用的肽
    • US20100305031A1
    • 2010-12-02
    • US12675961
    • 2009-05-22
    • Naomi WakabayashiSato Seiji
    • Naomi WakabayashiSato Seiji
    • A61K38/08C07K7/06C07K7/08C07K14/00C07K14/435A61K38/10A61K38/16A61P9/00A61P19/02A61P3/10
    • C07K14/00A61K47/62C07K14/58C07K14/63C07K16/26C07K2319/31
    • A peptide of the following (I) or (II). (I) a peptide represented by the formula B, A-B, B-C or A-B-C in which A, B and C each is represented by the following (1), (2) and (3) and, when it is bonded to other object peptide, it is able to extent the half-life in plasma as compared with the object peptide where the physiological activity of the object peptide is still retained. (II) a peptide comprising a reversed sequence of the peptide of (I); a sequence which is represented by A-B in (I) and A or B is reversed; a sequence which is represented by B-C in (I) and B or C is reversed; or a sequence which is represented by A-B-C in (I) and A, B, C, A and B, B and C or A and C is reserved. (1) A is a peptide comprising 1 to 14 of any amino acid(s) (2) B is a peptide represented by the formula 1: (Wk-Xl-Y-Zm-Wn)-(Wo-Xp-Y-Zq-Wr)s (In the formula 1, W is a basic amino acid; X and Z are any amino acids; Y is an acidic amino acid; k is 1 or 2; l is an integer of 4≧l≧0; m is an integer of 2≧m≧0; 4≧l+m≧0; n is 1 or 2; o is 1 or 2; p is an integer of 4≧p≧0; q is an integer of 2≧q≧0; 4≧p+q≧0; r is 1 or 2; and s is 0 or 1.) (3) C is a peptide comprising 2 to 14 of any amino acids.
    • 下列(I)或(II)的肽。 (I)由式B,AB,BC或ABC表示的肽,其中A,B和C各自由以下(1),(2)和(3)表示,并且当其结合到其它目标肽 与目标肽的生理活性仍然保留的目标肽相比,能够调节血浆中的半衰期。 (II)包含(I)的肽的逆序列的肽; (I)和A或B中的A-B表示的序列相反; 由(I)中的B-C和B或C表示的序列相反; 或由A,B,C,A和B,B和C或A和C中的A-B-C表示的序列被保留。 (1)A是包含1至14个任意氨基酸的肽(2)B是由式1表示的肽:(Wk-X1-Y-Zm-Wn) - (Wo-Xp-Y- Zq-Wr)s(式1中,W为碱性氨基酸,X为Z为任意氨基酸,Y为酸性氨基酸,k为1或2,l为4≥1≥0的整数。 m是2≥m≥0的整数;4≥1+m≥0; n是1或2; o是1或2; p是4≥P≥0的整数; q是2≥q的整数 ≥0;4≥p+q≥0; r为1或2; s为0或1.)(3)C为任意氨基酸2〜14个的肽。