Title

Synthesis, Characterization and Reactivities of New HDAC Inhibitors

Poster Number

12B

Lead Author Major

Biochemistry

Lead Author Status

Junior

Second Author Major

Bioengineering

Second Author Status

Junior

Format

Poster Presentation

Faculty Mentor Name

Qinliang Zhao

Faculty Mentor Email

qzhao@pacific.edu

Faculty Mentor Department

Chemistry

Additional Faculty Mentor Name

Xin Guo

Additional Faculty Mentor Email

xguo@pacific.edu

Additional Faculty Mentor Department

Pharmaceutics and Medicinal Chemistry

Graduate Student Mentor Name

Chao Feng

Graduate Student Mentor Email

c_feng1@u.pacific.edu

Graduate Student Mentor Department

Chemistry

Additional Mentors

Yingbo Huang, y_huang10@u.pacific.edu Department of Pharmaceutics and Medicinal Chemistry.

Abstract/Artist Statement

The advancement of tumors and growing resistance to existing anticancer drugs required the constant need for new drugs and/or therapies. Histone deacetylase (HDAC) is found to be overexpressed in some cancer cells, which condenses the chromatin structure of tumor suppressor genes, cell-cycle inhibitor genes and apoptosis inducer genes. Our innovative approach to these problems is to develop bifunctional platinum complexes stabilized by newly designed HDAC inhibitors. Each inhibitor comprises of a main scaffold, a zinc-binding group, a protein recognition cap and also a coordination site to metal ions. The HDAC inhibitors were synthesized, purified, and have been characterized by MS and NMR analysis. Platinum ions were anchored at the coordination site of the inhibitors, resulting in the desired metal complexes. Cell viability studies of the inhibitors and selected bifunctional compounds demonstrated the critical and unique role of each component in the inhibitor and metal complexes.

Location

DeRosa University Center Ballroom

Start Date

27-4-2018 12:30 PM

End Date

27-4-2018 2:30 PM

This document is currently not available here.

Share

COinS
 
Apr 27th, 12:30 PM Apr 27th, 2:30 PM

Synthesis, Characterization and Reactivities of New HDAC Inhibitors

DeRosa University Center Ballroom

The advancement of tumors and growing resistance to existing anticancer drugs required the constant need for new drugs and/or therapies. Histone deacetylase (HDAC) is found to be overexpressed in some cancer cells, which condenses the chromatin structure of tumor suppressor genes, cell-cycle inhibitor genes and apoptosis inducer genes. Our innovative approach to these problems is to develop bifunctional platinum complexes stabilized by newly designed HDAC inhibitors. Each inhibitor comprises of a main scaffold, a zinc-binding group, a protein recognition cap and also a coordination site to metal ions. The HDAC inhibitors were synthesized, purified, and have been characterized by MS and NMR analysis. Platinum ions were anchored at the coordination site of the inhibitors, resulting in the desired metal complexes. Cell viability studies of the inhibitors and selected bifunctional compounds demonstrated the critical and unique role of each component in the inhibitor and metal complexes.