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    COMPOUNDS MODIFYING APOPTOSIS
    2.
    发明申请
    COMPOUNDS MODIFYING APOPTOSIS 审中-公开
    化合物修饰药物

    公开(公告)号：WO2006128455A2

    公开(公告)日：2006-12-07

    申请号：PCT/DK2006/000280

    申请日：2006-05-23

    申请人： CARLSBERG A/S ,  THASTRUP, Ole ,  NORRILD, Jens

    发明人： THASTRUP, Ole ,  NORRILD, Jens

    CPC分类号： C07K5/1008 ,  C07K1/047 ,  C07K5/0806

    摘要： The present invention relates to compounds capable of inhibiting binding of the Smac protein to Inhibitors of apoptosis (IAPs). Such compounds are preferably capable of inhibiting IAP and thus may promote apoptosis or sensitize cells for apoptosis. The compounds may be used in the treatment of proliferative diseases, such as cancer.

    摘要翻译： 本发明涉及能够抑制Smac蛋白与凋亡抑制剂（IAP）结合的化合物。 这些化合物优选能够抑制IAP，从而可以促进细胞凋亡或使细胞增殖以进行细胞凋亡。 该化合物可用于治疗增殖性疾病，例如癌症。

    FLUOROGENIC PEPTIDES AND THEIR USE IN THE DETERMINATION OF ENZYMATIC ACTIVITIES
    5.
    发明申请
    FLUOROGENIC PEPTIDES AND THEIR USE IN THE DETERMINATION OF ENZYMATIC ACTIVITIES 审中-公开
    荧光素酶及其在酶活性测定中的应用

    公开(公告)号：WO1991016336A1

    公开(公告)日：1991-10-31

    申请号：PCT/DK1991000102

    申请日：1991-04-16

    申请人： CARLSBERG A/S ,  MELDAL, Morten ,  BREDDAM, Klaus

    发明人： CARLSBERG A/S

    IPC分类号： C07K05/00

    CPC分类号： C07K7/06 ,  C07K5/1016 ,  C12Q1/37 ,  Y02P20/55

    摘要： A fluorogenic peptide exhibiting intramolecular quenching having the general formula F-A-Q-Y1 or Y2-Q-A-F wherein Q is a fluorescence quenching substituted amino acid residue (I) wherein R1, R2, R3, R4 and R5 are independently selected from hydrogen, hydroxy, alkyl, alkoxy, amino, nitro, amido, halogen, aryl or aralkyl, with the proviso that at least one of R1 to R5 is hydroxy and at least one is nitro, wherein X is a spacing group which may be absent or selected from any combination of -CO-NH-, -CO-O-, -S-, -S-S-, -O-, -NH- or -C6H4-, and n and m are integers from 0 to 10, F is a fluorescent group having a maximum emission within the absorption band for the quenching residue Q, A is a spacing entity selected from amino acid residues and peptide residues and may include a non-peptide molecular entity, e.g. a mono- or oligosaccharie being linked to the fluorescent group F via an amide bond or ester bond, Y1 is OH, NH2, an amino acid residue, a peptide residue which is preferably attachable to a solid phase or a C-terminal protective group, Y2 is H, an amino acid residue, a peptide residue or an N-terminal protective group. Preferred peptides are those, wherein Q is 3-nitro-tyrosine, i.e. F1-A1-Tyr(NO2)-Y1 wherein F1 is a fluorescent group having a maximum emission of from 400 to 460 nm, preferably anthraniloyl, A1 is an amino acid residue or a peptide residue, preferably having 2 to 15 amino acids, and linked to the group F via a peptide bond, and Y1 is as defined above. The peptides are useful as substrates for determination of enzymatic activities in a sample, e.g. biological systems by incubating with the sample under conditions favourable to enzymatic activities, and determining and comparing the fluorescence emitted before and after the incubation. The peptides may advantageously be prepared by parallel multi-column solid phase synthesis.

    摘要翻译： 显示分子内猝灭的荧光肽，其通式为FAQ-Y1或Y2-QAF，其中Q为荧光猝灭取代的氨基酸残基（I），其中R 1，R 2，R 3，R 4和R 5独立地选自氢，羟基，烷基， 烷氧基，氨基，硝基，酰胺基，卤素，芳基或芳烷基，条件是R 1至R 5中的至少一个为羟基，并且至少一个为硝基，其中X为间隔基团，其可以不存在或选自 -CO-NH-，-CO-O-，-S-，-SS-，-O-，-NH-或-C6H4-，n和m为0〜10的整数，F为具有 在猝灭残基Q的吸收带内的最大发射是A，选自氨基酸残基和肽残基的间隔实体，并且可以包括非肽分子实体，例如 单糖或寡糖通过酰胺键或酯键与荧光基团F连接，Y 1是OH，NH 2，氨基酸残基，优选可附着于固相或C末端保护基的肽残基， Y2是H，氨基酸残基，肽残基或N-末端保护基。 优选的肽是其中Q是3-硝基 - 酪氨酸的那些，即F1-A1-Tyr（NO2）-Y1，其中F1是具有400-460nm的最大发射的荧光基团，优选地是氨基甲酰基，A1是氨基酸 残基或肽残基，优选具有2至15个氨基酸，并通过肽键与基团F连接，并且Y1如上所定义。 肽可用作测定样品中酶活性的底物，例如， 生物系统通过在有利于酶活性的条件下与样品一起孵育，并且确定和比较孵育前后发射的荧光。 肽可以有利地通过平行多柱固相合成来制备。

    ASSAYS FOR DETECTING GLUCOSIDASE ACTIVITY
    9.
    发明申请
    ASSAYS FOR DETECTING GLUCOSIDASE ACTIVITY 审中-公开
    检测葡糖苷酶活性的测定

    公开(公告)号：WO2013185771A1

    公开(公告)日：2013-12-19

    申请号：PCT/DK2013/050183

    申请日：2013-06-07

    申请人： CARLSBERG A/S, CARLSBERG FORSKNINGSCENTER

    发明人： BØJSTRUP, Marie ,  CHRISTENSEN, Caspar Elo ,  HINDSGAUL, Ole

    IPC分类号： C12Q1/00 ,  G01N33/50

    CPC分类号： C12Q1/34 ,  C12Q1/40 ,  G01N33/582 ,  G01N2333/944

    摘要： The present invention relates to a method of detecting α-(1→6)-glucosidase activity in a sample. The method is for example useful for determining the limit dextrinase activity in a sample. The method involves use of an oligosaccharide substrate of the formula X- (glucoside) n -*(glucoside) m -Z-Y, where X is a blocking group, -* is a α-(1→6)-glucosidic linkage and Y is a detectable label. Upon cleavage of the α-(1→6)-glucosidic linkage, the detectable labelis released and thus the α-(1→6)-glucosidase activity can be determined. The invention also relates to the oligosaccharide substrate per se.

    摘要翻译： 本发明涉及检测样品中α-（1-> 6） - 葡萄糖苷酶活性的方法。 该方法例如用于确定样品中限制性糊精酶活性。 该方法包括使用式X-（葡萄糖苷）n-*（葡萄糖苷）m -ZY的寡糖底物，其中X是封闭基团， - *是α-（1-> 6） - 葡萄糖苷键，Y 是可检测的标签。 当α-（1-> 6） - 葡萄糖苷键断裂时，可检测到的标记物被释放，因此可以测定α-（1-> 6） - 葡糖苷酶活性。 本发明还涉及寡糖底物本身。