The Road Less Traveled: a Bifunctional Molecular Approach to Cancer Medicine
Poster Number
11C
Format
Poster Presentation
Faculty Mentor Name
Qinliang Zhao
Faculty Mentor Department
Chemistry
Graduate Student Mentor Name
Chao Feng
Graduate Student Mentor Department
Chemistry
Abstract/Artist Statement
For decades, scientists have believed that normal cells transform into cancer cells due to a single cell changing its genetic expression. There are many mechanisms that control gene expression. One important mechanism involves transferring acetyl groups on histone proteins to turn on and off genetic expressions. Histone deacetylase (HDAC) is an enzyme that removes acetyl groups from histone proteins, compacting the DNA strands and turning off its genetic expression. After extensive study on HDAC, scientists introduced a new cancer treatment using HDAC inhibitors, which act on different levels of genetic expression: binding with histone deacetylase to inhibit deacetylation, affecting transcription factors, and altering protein functions.
Here, HDAC inhibitors with a structural motif similar to current clinical inhibitors but also containing a coordination site to Pt metal were designed and synthesized. One of the ligand inhibitors has been characterized by mass spectrometry and nuclear magnetic resonance. With higher advantage over cisplatin, the proposed platinum complex will possess dual functions with the Pt core attacking DNA and inhibiting deacetylation in gene expression. Because of the common overexpression of HDAC in tumor cells, these designed bifunctional complexes may contain higher selectivity toward tumor cells than normal cells, thus conquering cancer cells with minimal side effects.
Location
DeRosa University Center, Ballroom
Start Date
28-4-2018 1:00 PM
End Date
28-4-2018 3:00 PM
The Road Less Traveled: a Bifunctional Molecular Approach to Cancer Medicine
DeRosa University Center, Ballroom
For decades, scientists have believed that normal cells transform into cancer cells due to a single cell changing its genetic expression. There are many mechanisms that control gene expression. One important mechanism involves transferring acetyl groups on histone proteins to turn on and off genetic expressions. Histone deacetylase (HDAC) is an enzyme that removes acetyl groups from histone proteins, compacting the DNA strands and turning off its genetic expression. After extensive study on HDAC, scientists introduced a new cancer treatment using HDAC inhibitors, which act on different levels of genetic expression: binding with histone deacetylase to inhibit deacetylation, affecting transcription factors, and altering protein functions.
Here, HDAC inhibitors with a structural motif similar to current clinical inhibitors but also containing a coordination site to Pt metal were designed and synthesized. One of the ligand inhibitors has been characterized by mass spectrometry and nuclear magnetic resonance. With higher advantage over cisplatin, the proposed platinum complex will possess dual functions with the Pt core attacking DNA and inhibiting deacetylation in gene expression. Because of the common overexpression of HDAC in tumor cells, these designed bifunctional complexes may contain higher selectivity toward tumor cells than normal cells, thus conquering cancer cells with minimal side effects.