"Bioactive Food Peptides in Health and Disease" highlights recent developments on bioactive food peptides for the promotion of human health and the prevention/management of chronic diseases. The book provides a comprehensive revision of bioactive peptides obtained from both animal and plant food sources. Aspects related to their bioactivity, mechanism of action, and bioavailability are extensively described along the different chapters.
THE EXTENT AND TIMING OF PLANT GROWTH are controlled by the coordinated actions of positive and negative regulators. Some of the most obvious examples of regulated nongrowth are seed and bud dormancy, adaptive features that delay growth until environmental conditions are favorable. For many years, plant physiologists suspected that the phenomena of seed and bud dormancy were caused by inhibitory compounds, and they attempted to extract and isolate such compounds from a variety of plant tissues, especially dormant buds.
We have previously reported that sulfoquinovosylmonoacylglycerol
(SQMG) is a potent inhibitor of mammalian DNA polymerases. DNA
polymeraseb(pol b) is one of the most important enzymes protecting the
cell against DNA damage by base excision repair. In this study, we charac-terized the inhibitory action of SQMG against rat pol b. SQMG competed
with both the substrate and the template-primer for binding to polb.
Amino-(3,4-dihydroxyphenyl)methyl phosphonic acid, the
phosphonic analogof 3,4-dihydroxyphenylglycine, hadbeen
previously reported as a potent inhibitor of tyrosinase. The
mechanism of the apparent enzyme inhibition by this com-pound has now been established. Amino-(3,4-dihydroxy-phenyl)methyl phosphonic acid turned out to be a substrate
and was oxidized too-quinone, which evolved to a final
product identified as 3,4-dihydroxybenzaldehyde, the same
as for 3,4-dihydroxyphenylglycine.
The study and therapeutic modulation of purinergic signaling is hindered
by a lack of specific inhibitors for NTP diphosphohydrolases (NTPDases),
which are the terminating enzymes for these processes. In addition, little is
known of the NTPDase protein structural elements that affect enzymatic
activity and which could be used as targets for inhibitor design.
Other Diseases The power and versatility of gene transfer approaches are such that there are few serious disease entities for which gene transfer therapies are not under development. Besides those already discussed, other areas of interest include gene therapies for HIV and for neurodegenerative disorders.
The protein arginine methyltransferase (PRMT) family of enzymes cata-lyzes the transfer of methyl groups from S-adenosylmethionine to the gua-nidino nitrogen atom of peptidylarginine to form monomethylarginine or
dimethylarginine. We created several less polar analogs of the specific
PRMT inhibitor arginine methylation inhibitor-1, and one such compound
was found to have improved PRMT inhibitory activity over the parent
Highly active, small-molecule furin inhibitors are attractive drug candidates
to fend off bacterial exotoxins and viral infection. Based on the 22-residue,
active Lys fragment of the mung bean trypsin inhibitor, a series of furin
inhibitors were designed and synthesized, and their inhibitory activity
towards furin and kexin was evaluated using enzyme kinetic analysis.
HIV-1 protease is an important target for treatment of
AIDS, and efficient drugs have been developed. However,
the resistance and negative side effects of the current drugs
has necessitated the development of new compounds with
different binding patterns. In this study, nine C-terminally
duplicated HIV-1 protease inhibitors were cocrystallised
with the enzyme, the crystal structures analysed at 1.8–2.3 A˚
resolution, and the inhibitory activity of the compounds
characterized inorder toevaluate the effects of the individual