Protein Kinase Inhibitors from Microorganisms

Radhika, P.; Kumar, M. Murali Krishna; Nagasree, Kurre Purna

doi:10.1016/b978-0-444-63460-3.00008-0

Cited by 2 publications

(3 citation statements)

References 176 publications

(169 reference statements)

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“…from Streptomyces staurosporeus in 1977 [ 67 ]. Later on in 1986, the inhibitory activity of Staurosporine against PKC was revealed (IC 50 = 2.7 nM) [ 67 , 68 ]. This discovery opened the door widely toward new drug discovery trials targeting kinases in general.…”

Section: Protein Kinase Cmentioning

confidence: 99%

“…Staurosporine (compound 27 , Table 3 ) was first named as AM-2282; later on, many of its analogs were synthesized. Another series of PKC inhibitors was isolated from the culture of Nocardiopsis species; among them are K-252a (IC 50 = 18–25 nM; compound 28 , Table 3 ), K-252b (IC 50 = 20 nM; compound 29 , Table 3 ) and K-252c (IC 50 = 2.45 µM) [ 68–70 ]. Furthermore, in 1992, RK-1409 (7-oxo Staurosporine; compound 30 , Table 3 ) was isolated from Streptomyces platensis , subsp.…”

Section: Protein Kinase Cmentioning

confidence: 99%

“…Furthermore, in 1992, RK-1409 (7-oxo Staurosporine; compound 30 , Table 3 ) was isolated from Streptomyces platensis , subsp. Malvinus and showed significant PKC inhibitory activity (IC 50 ≈ 1 nM) [ 68–70 ]. Several other Staurosporine derivatives were reported to be isolated and reported in the literature but all with submicromolar PKC inhibitory concentrations [ 68–70 ].…”

Section: Protein Kinase Cmentioning

confidence: 99%

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Research Advances in Kinase Enzymes and Inhibitors for Cardiovascular Disease Treatment

et al. 2017

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The targeting of protein kinases has great future potential for the design of new drugs against cardiovascular diseases (CVDs). Enormous efforts have been made toward achieving this aim. Unfortunately, kinase inhibitors designed to treat CVDs have suffered from numerous limitations such as poor selectivity, bad permeability and toxicity. So, where are we now in terms of discovering effective kinase targeting drugs to treat CVDs? Various drug design techniques have been approached for this purpose since the discovery of the inhibitory activity of Staurosporine against protein kinase C in 1986. This review aims to provide context for the status of several emerging classes of direct kinase modulators to treat CVDs and discuss challenges that are preventing scientists from finding new kinase drugs to treat heart disease.

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Section: Protein Kinase Cmentioning

confidence: 99%

Section: Protein Kinase Cmentioning

confidence: 99%