1-Methoxy-agroclavine from Penicillium sp. WC75209, a novel inhibitor of the Lck tyrosine kinase.
A high-throughput screen was developed and implemented to identify inhibitors of the Lck tyrosine kinase. This report describes the identification of a specific inhibitor of this enzyme from the solid fermentation culture of the Penicillium sp., WC75209. The active compound was isolated and structurally characterized as 1-methoxy-5R, 10S-agroclavine, a new member of the ergot alkaloid family.
Padmanabha
R
R
Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT, USA.
Shu
Y Z
YZ
Cook
L S
LS
Veitch
J A
JA
Donovan
M
M
Lowe
S
S
Huang
S
S
Pirnik
D
D
Manly
S P
SP
D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D004873:Ergolines / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D019860:Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / Q000037:antagonists & inhibitors*; D008956:Models, Chemical; D010407:Penicillium / Q000737:chemistry; D013237:Stereoisomerism
C116603:1-methoxyagroclavine; D004791:Enzyme Inhibitors; D004873:Ergolines; D019860:Lymphocyte Specific Protein Tyrosine Kinase p56(lck)