1-Methoxy-agroclavine from Penicillium sp. WC75209, a novel inhibitor of the Lck tyrosine kinase

R Padmanabha; Y Z Shu; L S Cook; J A Veitch; M Donovan; S Lowe; S Huang; D Pirnik; S P Manly

doi:10.1016/s0960-894x(98)00072-9

1-Methoxy-agroclavine from Penicillium sp. WC75209, a novel inhibitor of the Lck tyrosine kinase

Bioorg Med Chem Lett. 1998 Mar 17;8(6):569-74. doi: 10.1016/s0960-894x(98)00072-9.

Authors

R Padmanabha¹, Y Z Shu, L S Cook, J A Veitch, M Donovan, S Lowe, S Huang, D Pirnik, S P Manly

Affiliation

¹ Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT, USA.

PMID: 9871562
DOI: 10.1016/s0960-894x(98)00072-9

Abstract

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.

MeSH terms

Enzyme Inhibitors / chemistry
Enzyme Inhibitors / isolation & purification*
Enzyme Inhibitors / pharmacology*
Ergolines / chemistry
Ergolines / isolation & purification*
Ergolines / pharmacology*
Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / antagonists & inhibitors*
Models, Chemical
Penicillium / chemistry
Stereoisomerism

Substances

1-methoxyagroclavine
Enzyme Inhibitors
Ergolines
Lymphocyte Specific Protein Tyrosine Kinase p56(lck)