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ú chain and to
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(15) All tables listed in this paper contain IC50’s that are the average
of triplicate measurements. In all cases, ZAP-70 and Syk refer
to the tandem SH2 ZAP-70 and Syk.
(26) Table 1 lists the IC50’s for the ú-1-ITAM peptide against ZAP-
70 and Syk. A number of large peptide sequences have also been
tested against ZAP-70 and Syk. Some of these include: Ac-DVD-
pYTGLSTRNQET-pYETLK-NH2, Ac-KEL-pYTELLTLLEKL-
pYETLK-NH2, Ac-DAV-pYTGLNTRNQET-pYETLK-NH2, and
Ac-DGV-pYTGLAAAAAAA-pYETLK-NH2. Very little selectivity
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(18) Table 1 lists the standard tetrapeptide Ac-pYEEI-NH2 ligand
for Src. A large number of tetrapeptide sequences have also been
found to be almost as effective. For a discussion on peptide
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S.; Crosby, R.; Alligood, K.; Green, M.; Kimery, M.; Wagner, C.;
Kinder, D.; Charifson, P.; Hassel, A. M.; Willard, D.; Luther,
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(31) Compounds 14a -14f were prepared using a reaction sequence
similar to that shown in Scheme
1 except that BOC-Tyr-
(PO3Bzl2)-OH was used instead of Ac-Tyr(PO3Bzl2)-OH. Upon
TFA treatment, the phosphate group was unmasked and the
BOC group was removed. The resulting amino phosphate
derivative was then acylated with the desired acid chloride (see
Experimental Section).
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J M990229T