Additional peptidyl diazomethyl ketones, including biotinyl derivatives, which affinity-label calpain and related cysteinyl proteinases.
Calpain, the calcium-activated cysteinyl proteinase, can be irreversibly inactivated by peptidyl diazomethyl ketones in which the peptide portion contains a penultimate leucine residue. Some new derivatives of this type have been synthesized and examined for their rates of inactivation of chicken gizzard and human platelet calpain. Two derivatives containing a C-terminal biotin residue, Biot-Aca-Leu-TyrCHN2 and Biot-Aca-Leu-Leu-TyrCHN2, have also been prepared in the expectation that their application to the study of the function of calpain and related proteases will prove fruitful.
Wikstrom
P
P
Friedrich Miescher-Institut, Basel, Switzerland.
Anagli
J
J
Angliker
H
H
Shaw
E
E
D000345:Affinity Labels / Q000737:chemistry / Q000378:metabolism*; D000595:Amino Acid Sequence; D000818:Animals; D001710:Biotin; D001792:Blood Platelets / Q000201:enzymology; D002154:Calpain / Q000037:antagonists & inhibitors* / Q000378:metabolism; D002645:Chickens; D003546:Cysteine Endopeptidases / Q000378:metabolism; D015853:Cysteine Proteinase Inhibitors / Q000378:metabolism*; D003978:Diazomethane / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism; D005895:Gizzard, Avian / Q000201:enzymology; D006801:Humans; D007659:Ketones / Q000737:chemistry / Q000378:metabolism*; D008969:Molecular Sequence Data
D000345:Affinity Labels; D015853:Cysteine Proteinase Inhibitors; D007659:Ketones; C021232:peptidyl diazomethyl ketones; D003978:Diazomethane; D001710:Biotin; D002154:Calpain; D003546:Cysteine Endopeptidases