BACKGROUND: This research was undertaken in order to investigate the inhibitory potential of the Jamaican ball moss, Tillandsia recurvata against several kinases. The inhibition of these kinases has emerged as a potential solution to restoring the tight regulation of normal cellular growth, the loss of which leads to cancer cell formation. MATERIALS AND METHODS: Kinase inhibition was investigated using competition binding (to the ATP sites) assays, which have been previously established and authenticated. RESULTS: Four hundred and fifty one kinases were tested against the Jamaican ball moss extract and a dose-response was tested on 40 kinases, which were inhibited by more than 35% compared to the control. Out of the 40 kinases, the Jamaican ball moss selectively inhibited 5 (CSNK2A2, MEK5, GAK, FLT and DRAK1) and obtained Kd(50)s were below 20 μg/ml. CONCLUSION: Since MEK5 and GAK kinases have been associated with aggressive prostate cancer, the inhibitory properties of the ball moss against them, coupled with its previously found bioactivity towards the PC-3 cell line, makes it promising in the arena of drug discovery towards prostate cancer.
BACKGROUND: This research was undertaken in order to investigate the inhibitory potential of the Jamaican ball moss, Tillandsia recurvata against several kinases. The inhibition of these kinases has emerged as a potential solution to restoring the tight regulation of normal cellular growth, the loss of which leads to cancer cell formation. MATERIALS AND METHODS: Kinase inhibition was investigated using competition binding (to the ATP sites) assays, which have been previously established and authenticated. RESULTS: Four hundred and fifty one kinases were tested against the Jamaican ball moss extract and a dose-response was tested on 40 kinases, which were inhibited by more than 35% compared to the control. Out of the 40 kinases, the Jamaican ball moss selectively inhibited 5 (CSNK2A2, MEK5, GAK, FLT and DRAK1) and obtained Kd(50)s were below 20 μg/ml. CONCLUSION: Since MEK5 and GAK kinases have been associated with aggressive prostate cancer, the inhibitory properties of the ball moss against them, coupled with its previously found bioactivity towards the PC-3 cell line, makes it promising in the arena of drug discovery towards prostate cancer.
Authors: Tommaso Stefani; Antonio Romo-Mancillas; Juan J J Carrizales-Castillo; Eder Arredondo-Espinoza; Karla Ramírez-Estrada; Victor M Alcantar-Rosales; Leticia González-Maya; Jessica Nayelli Sánchez-Carranza; Isaías Balderas-Renterías; María Del Rayo Camacho-Corona Journal: Molecules Date: 2021-02-19 Impact factor: 4.411