Title

The Road Less Traveled: a Bifunctional Molecular Approach to Cancer Medicine

Poster Number

11C

Lead Author Major

Biochemistry

Lead Author Status

Junior

Format

Poster Presentation

Faculty Mentor Name

Qinliang Zhao

Faculty Mentor Email

qzhao@pacific.edu

Faculty Mentor Department

Chemistry

Graduate Student Mentor Name

Chao Feng

Graduate Student Mentor Email

c_feng1@u.pacific.edu

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

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Apr 28th, 1:00 PM Apr 28th, 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.