Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:6.2.1.7 (BAL)
 1,977 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

To more rapidly prepare members of the 1,3-bis(acylamino)-2-butanone class of cysteine protease inhibitors, a solid-phase synthesis was developed. 1-Azido-3-amino-2,2-dimethoxybutane (4), which has the two amino groups differentiated and the ketone protected as a a ketal, served as a surrogate for the 1,3-diamino-2-butanone core. Amine (4) was coupled to the BAL-resin-linked carboxylic acids derived from alpha-amino acid esters. Evaluation of a small combinatorial array by measuring inhibition constants (Ki,appS) against cathepsins K, L, and B provided some structure-activity relationship trends with respect to selectivity and potency. Novel, potent inhibitors of cathepsins K and L were identified.
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PMID:Solid-phase synthesis of a combinatorial array of 1,3-bis(acylamino)-2-butanones, inhibitors of the cysteine proteases cathepsins K and L. 1074 10

A root extract of Valeriana jatamansi (code BAL-O) exhibited larvicidal and adulticidal activity against different mosquito species. The median lethal concentration (LC50) of BAL-O against larvae of Anopheles stephensi, Anopheles culicifacies, Aedes aegypti, Aedes albopictus, and Culex quinquefasciatus were 68.1, 42.8, 51.2, 53.8, and 80.6 mg/liter, respectively. The LC50 and the 90% lethal concentration against adult An. stephensi, An. culicifacies, Ae. aegypti, Ae. albopictus, and Cx. quinquefasciatus were 0.14, 0.16, 0.09, 0.08, and 0.17 and 0.24, 0.34, 0.25, 0.21, and 0.28 mg/cm2, respectively. The median knock-down time and 90% knock-down time of the fraction were 13, 13, 12, 13, and 18 and 24, 25, 21, 20, and 42 min against An. stephensi, An. culicifacies, Ae. aegypti, An. albopictus and Cx. quinquefasciatus, respectively, using 0.28 mg/cm2 impregnated papers. The median effective time and 90% effective time against An. stephensi at 4 degrees C were 46.6 and 8.7 days, and at 29 degrees C, 25.5 and 5.6 days, respectively. Gas chromatographic-mass spectrometric analysis of BAL-O showed 2-butanone,4-(2,6,6-trimethyl-2-cyclohexen-l-yl) (10.11%), patchouli alcohol (8.55%), cubenol (5.97%), caryophyllene oxide (5.46%), cadinol (5.23%), and aristolene (5.19%).
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PMID:Insecticidal activity of Valeriana jatamansi (Valerianaceae) against mosquitoes. 1866 42

Deltex-3-like (DTX3L), an E3 ligase, is a member of the Deltex (DTX) family and is also called B-lymphoma and BAL-associated protein (BBAP). Previously, we established RFP/RET-transgenic mice, in which systemic hyperpigmented skin, benign melanocytic tumor(s) and melanoma(s) develop stepwise. Here we showed that levels of Dtx3l/DTX3L in spontaneous melanoma in RFP/RET-transgenic mice and human melanoma cell lines were significantly higher than those in benign melanocytic cells and primarily cultured normal human epithelial melanocytes, respectively. Immunohistochemical analysis of human tissues showed that more than 80% of the melanomas highly expressed DTX3L. Activity of FAK/PI3K/AKT signaling, but not that of MEK/ERK signaling, was decreased in Dtx3l/DTX3L-depleted murine and human melanoma cells. In summary, we demonstrated not only increased DTX3L level in melanoma cells but also DTX3L-mediated regulation of invasion and metastasis in melanoma through FAK/PI3K/AKT but not MEK/ERK signaling. Our analysis in human BRAFV600E inhibitor-resistant melanoma cells showed about 80% decreased invasion in the DTX3L-depleted cells compared to that in the DTX3L-intact cells. Thus, DTX3L is clinically a potential therapeutic target as well as a potential biomarker for melanoma.
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PMID:Deltex-3-like (DTX3L) stimulates metastasis of melanoma through FAK/PI3K/AKT but not MEK/ERK pathway. 2603 50