A potent tyrosine kinase inhibitor, lavendustin A [1], has been isolated from a butyl acetate extract of Streptomyces griseolavendus culture filtrate. It inhibits epidermal growth factor receptor-associated tyrosine kinase with an IC50 of 4.4 ng/ml, which is about 50 times more inhibitory than erbstatin. It does not inhibit protein kinase A or C. Its structure, determined by spectral data and total synthesis, is novel, having a tertiary amine in the center with substituted benzyl and phenyl groups. Lavendustin A competes with ATP and is noncompetitive with the peptide. Its structure-activity relationship is discussed.
The performance of the Lung Imaging Fluorescence Endoscope (LIFE) system was compared with conventional bronchoscopy in 158 patients: 68 patients with invasive cancer, 42 patients
with abnormal sputum cytology findings (12 early cancer and 26 dysplasia), 17 cases with
resected lung cancer and 31 smokers with symptoms. The respective results of conventional
bronchoscopy and LIFE for detection of dysplasia were; sensitivity 52% and 90% (biopsy
basis), 62% and 92% (patient basis). Fluorescence bronchoscopy may be an important
adjunct to conventional bronchoscopy to improve the localization of subtle lesions of
bronchus.
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