TY - JOUR
T1 - Effect of two series of isoindolines over HDAC8 activity and expression
AU - Trejo Muñoz, Cynthia R.
AU - Jiménez, Elvia Mera
AU - Pinto-Almazán, Rodolfo
AU - Gandarilla, José Alfredo Díaz
AU - Correa-Basurto, José
AU - Trujillo-Ferrara, José G.
AU - Guerra-Araiza, Christian
AU - Rohana, Patricia Talamás
AU - Percino, Teresa Mancilla
N1 - Funding Information:
Acknowledgments The authors are grateful to CONACYT for scholarship No. 215133 to CRTM, SIP-COFAA/IPN, CONACYT (132353), and ICyTDF for financial support, to Brenda Trejo for language help corrections.
PY - 2014/6
Y1 - 2014/6
N2 - This work describes the effect of two series of isoindolines 1(a-g) and 2(a-g) on histone deacetylase 8 (HDAC8) activity by theoretical study (docking method) and experimental assays using a commercial kit, as well as the effect of isoindolines on HDAC8 expression on HeLa cells. The theoretical study show interactions of the isoindolines with two HDAC8 deep pockets; these binding sites were compared to those of HDAC8 inhibitor, Trichostatin A. It was demonstrated experimentally that tested compounds can act as HDAC8 inhibitors. The expression of HDAC8 by Western blot analysis, remain unchanged in HeLa cells treated with the isoindolines with the exception of compound 2b which seems to increase HDAC8 expression. In conclusion, isoindolines act as HDAC8 inhibitors because they do not decrease the protein expression.
AB - This work describes the effect of two series of isoindolines 1(a-g) and 2(a-g) on histone deacetylase 8 (HDAC8) activity by theoretical study (docking method) and experimental assays using a commercial kit, as well as the effect of isoindolines on HDAC8 expression on HeLa cells. The theoretical study show interactions of the isoindolines with two HDAC8 deep pockets; these binding sites were compared to those of HDAC8 inhibitor, Trichostatin A. It was demonstrated experimentally that tested compounds can act as HDAC8 inhibitors. The expression of HDAC8 by Western blot analysis, remain unchanged in HeLa cells treated with the isoindolines with the exception of compound 2b which seems to increase HDAC8 expression. In conclusion, isoindolines act as HDAC8 inhibitors because they do not decrease the protein expression.
KW - Cancer
KW - Docking
KW - HDAC8 inhibitors
KW - HeLa cells
KW - Isoindolines
UR - http://www.scopus.com/inward/record.url?scp=84898925995&partnerID=8YFLogxK
U2 - 10.1007/s00044-013-0903-y
DO - 10.1007/s00044-013-0903-y
M3 - Artículo
SN - 1054-2523
VL - 23
SP - 3227
EP - 3234
JO - Medicinal Chemistry Research
JF - Medicinal Chemistry Research
IS - 6
ER -