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Books > Science & Mathematics > Biology, life sciences > Biochemistry
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Non-peptide Inhibitors of Proprotein Convertase Subtilisin Kexins (PCSKs) - An Overall Review of Existing and New Data (Paperback)
Loot Price: R1,129
Discovery Miles 11 290
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Non-peptide Inhibitors of Proprotein Convertase Subtilisin Kexins (PCSKs) - An Overall Review of Existing and New Data (Paperback)
Series: Colloquium Series on Protein Activation and Cancer
Expected to ship within 10 - 15 working days
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The Ca+2-dependent mammalian Proprotein Convertase Subtilisin
Kexins (PCSKs) or Proprotein/ Prohormone Convertases (PCs) are a
family of endoproteases that play critical roles not only in normal
development and metabolism but also in various physiological and
pathological conditions. These were initiated by the proteolytic
processing of large inactive proproteins into their shorter
bioactive mature forms by the PCSK enzymes. These events take place
in a highly selective, orchestrated, and stepwise manner. Among the
various proprotein substrates of PCSK enzymes, particularly
important are the precursor growth factors that include proPDGF-A,
B, proIGF-1, 2 and proVEGF-C because of their strong implications
in neoplasia initiation, progression, and metastasis. As a result
of these findings, PCSK enzymes, particularly furin or PCSK3,
became a major target for possible interventions of cancer via the
use of their selective inhibitors. Significant progress has been
accomplished in the development of peptide and protein-based PCSK
inhibitors. However, non-peptide PCSK9 inhibitors are more
preferable because of their drug-like and other characteristics. So
far, a few non-peptide inhibitors of PCSK enzymes of various types
of chemical structures have been described in the literature. These
include (i) Carbocyclic compounds of diterpene and streptamine
class. (ii) Nitrogen (N)-based heterocyclic compounds of various
types and chemical structures such as (a) pyrrolidine bis
piperazines, (b) Cu/Zn chelating terpyridine derivatives; (iii)
Oxygen (O)-based Heterocyclic compounds of varying types of
chemical structures such as (a) Flavonoids, (b) Coumarins of simple
and dimeric types, (c) Quinonoids, (d) Iridoids; (iv) Aromatic
compounds such as (a) Aryl guanidino and amidino derivatives, (b)
Naphthyl fluorescein derivative, and (c) Phenyl Arsonic acids; and
(v) C2-symmetrical aromatic azo-compounds. When measured against a
small peptidyl-MCA fluorogenic substrate, these inhibitors
displayed IC50 values ranging from nM to ?M. A number of these
inhibitors exhibited significant anti-PCSK activity when tested in
ex vivo or cell culture conditions. This article provides an
overall review of all non-peptide PCSK inhibitors so far reported
in the literature along with those we identified recently for the
first time and not yet published. The potential implications of
these molecules as biochemical, therapeutical, or clinical agents
will also be discussed.
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