Targeting glycolysis: a fragment based approach towards bifunctional inhibitors of hLDH-5.
hLDH-5 has emerged as a promising target for anti-glycolytic cancer chemotherapy. Here we report a first generation of bifunctional inhibitors, which show promising activity against hLDH-5.
Moorhouse
Adam D
AD
School of Chemistry, University of Nottingham, University Park, Nottingham, NG7 2RD, UK.
Spiteri
Christian
C
Sharma
Pallavi
P
Zloh
Mire
M
Moses
John E
JE
D000480:Alkynes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D020134:Catalytic Domain / Q000187:drug effects; D057930:Click Chemistry; D018360:Crystallography, X-Ray; D006019:Glycolysis; D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors / Q000378:metabolism; D007770:L-Lactate Dehydrogenase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000080864:Lactate Dehydrogenase 5; D008024:Ligands; D008958:Models, Molecular; D015394:Molecular Structure; D009243:NAD / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D010072:Oxamic Acid / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
D000480:Alkynes; D007527:Isoenzymes; D008024:Ligands; D014230:Triazoles; D009243:NAD; D007770:L-Lactate Dehydrogenase; D000080864:Lactate Dehydrogenase 5; D010072:Oxamic Acid