AbstractThe tetrasaccharide heparan sulfate (HS) mimetic PG545, a clinical anti-cancer candidate, is an inhibitor of the HS-degrading enzyme heparanase. The kinetics of heparanase inhibition by PG545 and three structural analogues were investigated to understand their modes of inhibition. The cholestanol aglycon of PG545 significantly increased affinity for heparanase and also modified the inhibition mode. For the tetrasaccharides, competitive inhibition was modified to parabolic competition by the addition of the cholestanol aglycon. For the trisaccharides, partial competitive inhibition was modified to parabolic competition. A schematic model to explain these findings is presented
Heparan sulfate proteoglycans are integral components of the extracellular matrix that surrounds all...
Heparanase has been viewed as a promising anti-cancer drug target for almost two decades, but no ant...
Heparanase is an endo-β-glucuronidase that cleaves at a limited number of internal sites the glycosa...
AbstractThe tetrasaccharide heparan sulfate (HS) mimetic PG545, a clinical anti-cancer candidate, is...
Heparanase is a promising anticancer target because of its involvement in cancer invasion and metast...
PG545 is a clinically relevant heparan sulfate (HS) mimetic which, in addition to possessing anti-an...
<div><p>PG545 is a clinically relevant heparan sulfate (HS) mimetic which, in addition to possessing...
Heparan sulfate proteoglycans (HSPGs) mediate essential interactions throughout the extracellular ma...
BACKGROUND: PG545 is a heparan sulfate (HS) mimetic that inhibits tumour angiogenesis by sequesterin...
Heparan sulfate (HS) is a highly sulfated polysaccharide that serves many biological functions, incl...
Heparanase is the unique and specific functional endoglycosidase capable of cleaving heparan sulfate...
Heparanase is the unique and specific functional endoglycosidase capable of cleaving heparan sulfate...
In recent years, heparanase has attracted considerable attention as a promising target for innovativ...
Pixatimod (PG545), a heparan sulfate (HS) mimetic and anticancer agent currently in clinical trials,...
Heparan sulfate mimetics, which we have called the PG500 series, have been developed to target the i...
Heparan sulfate proteoglycans are integral components of the extracellular matrix that surrounds all...
Heparanase has been viewed as a promising anti-cancer drug target for almost two decades, but no ant...
Heparanase is an endo-β-glucuronidase that cleaves at a limited number of internal sites the glycosa...
AbstractThe tetrasaccharide heparan sulfate (HS) mimetic PG545, a clinical anti-cancer candidate, is...
Heparanase is a promising anticancer target because of its involvement in cancer invasion and metast...
PG545 is a clinically relevant heparan sulfate (HS) mimetic which, in addition to possessing anti-an...
<div><p>PG545 is a clinically relevant heparan sulfate (HS) mimetic which, in addition to possessing...
Heparan sulfate proteoglycans (HSPGs) mediate essential interactions throughout the extracellular ma...
BACKGROUND: PG545 is a heparan sulfate (HS) mimetic that inhibits tumour angiogenesis by sequesterin...
Heparan sulfate (HS) is a highly sulfated polysaccharide that serves many biological functions, incl...
Heparanase is the unique and specific functional endoglycosidase capable of cleaving heparan sulfate...
Heparanase is the unique and specific functional endoglycosidase capable of cleaving heparan sulfate...
In recent years, heparanase has attracted considerable attention as a promising target for innovativ...
Pixatimod (PG545), a heparan sulfate (HS) mimetic and anticancer agent currently in clinical trials,...
Heparan sulfate mimetics, which we have called the PG500 series, have been developed to target the i...
Heparan sulfate proteoglycans are integral components of the extracellular matrix that surrounds all...
Heparanase has been viewed as a promising anti-cancer drug target for almost two decades, but no ant...
Heparanase is an endo-β-glucuronidase that cleaves at a limited number of internal sites the glycosa...