GUANINE NUCLEOSIDES--POTENTIAL NEW THERAPEUTIC USES
Project Number1R29CA062051-01
Contact PI/Project LeaderCOHEN, JUSTIN D
Awardee OrganizationUNIVERSITY OF COLORADO DENVER
Description
Abstract Text
Inhibition of DNA synthesis by a deoxynucleoside or a deoxynucleoside
analogue can kill cells ("direct toxicity") and can also enhance the
toxicity of alkylating agents ("sensitization"). Not surprisingly, the
extent of direct toxicity correlates closely with the degree of
sensitization. This proposal addresses T cell neoplasms which are
unusually sensitive to direct toxicity by deoxyguanosine and uniquely and
exquisitely sensitive to its analogue 9-beta-D-arabinofuranosylguanine
("araG"). One objective of this proposal is to use this unique
sensitivity to selectively sensitize T cell neoplasms compared to normal
hematopoietic progenitor cells responsible for dose-limiting clinical
toxicity. Such T cell selective sensitization has clear potential
applications in clinical treatment as well as in ex vivo purging of
neoplastic T cells from bone marrow. A second objective is to determine
the mechanisms of sensitization with the long term intention of
extrapolating these mechanistic concepts to closely analogous
sensitization approaches.
In preliminary studies araG and deoxyguanosine did potently enhance
alkylator toxicity producing 5 to 8 fold dose modifying effects in human
T cell neoplasms but not in B cells. In sharp contrast, guanosine was non-
toxic and strongly protected against alkylator toxicity in human T cell
lines - despite depleting dCTP and dTTP pools to the same extent as did
equimolar deoxyguanosine. Guanosine's surprising effect and the very
different effect of araG may relate to metabolism of araG almost
exclusively via the deoxycytidine kinase ("dCK") pathway and to metabolism
of guanosine via the purine nucleoside phophorylase ("PNP") pathway.
Deoxyguanosine, metabolized via both pathways, might sensitize T cell
neoplasms (high dCK:PNP ratio) while simultaneously protecting non-T cells
(low dCK:PNP). Using measures of nucleoside metabolism, DNA injury and
repair, and new techniques for specifically identifying which aspects of
DNA synthesis are being impaired, this proposal will test l) whether
deoxyguanosine, araG or guanosine preferentially sensitize or protect
human T cell malignancies relative to non-T cells including normal marrow
progenitor cells, 2) whether deoxyguanosine can sensitize or protect
depending on its metabolism via the dCK or PNP pathways, 3) whether
guanosine protects by increasing guanylate ribonucleotides which then
block cell cycle progression permitting greater repair of alkylator-
injured DNA before cells initiate replicative synthesis, and 4) whether
deoxyguanosine and araG cause direct toxicity and sensitization not only
by depleting dCTP and dTTP but also by high dGTP and araGTP inhibiting DNA
polymerases alpha, delta or epsilon.
No Sub Projects information available for 1R29CA062051-01
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