Open Access. Powered by Scholars. Published by Universities.®

Biochemistry, Biophysics, and Structural Biology Commons

Open Access. Powered by Scholars. Published by Universities.®

Cancer Biology

UMass Center for Clinical and Translational Science Research Retreat

Articles 1 - 6 of 6

Full-Text Articles in Biochemistry, Biophysics, and Structural Biology

Structural Activity Relationship Study On Dual Plk1 /Brd4 Inhibitor, Bi- 2536, Hailemichael Yosief, Shuai Liu, Dennis L. Buckley, Justin M. Roberts, Alex M. Muthengi, Francesca M. Corsini, James E. Bradner, Wei Zhang May 2016

Structural Activity Relationship Study On Dual Plk1 /Brd4 Inhibitor, Bi- 2536, Hailemichael Yosief, Shuai Liu, Dennis L. Buckley, Justin M. Roberts, Alex M. Muthengi, Francesca M. Corsini, James E. Bradner, Wei Zhang

UMass Center for Clinical and Translational Science Research Retreat

Polo-like kinase 1 (PLK1) and BRD4 are two different therapeutic targets in cancer drug discovery. Recently it has been reported that PLK1 inhibitor, BI-2536, is also a potent inhibitor of BRD4. The simultaneous inhibition of PLK1 and BRD4 by a single drug molecule is interesting because this could lead to the development of effective therapeutic strategy for different types of disease conditions in which PLK1 and BRD4 are implicated. Structural activity relationship studies has been carried out on BI-2536 to generate analogs with enhanced dual inhibitory activity against BRD4 and PLK1 as well as to render the molecule selective to ...


Inhibition Of Colon Cancer By Polyphenols From Whole Cranberry, Catherine Neto, Anne Liberty, Sarah Frade, Anuradha Tata, Tracie Ferreira, Mingyue Song, Xian Wu, Hang Xiao May 2014

Inhibition Of Colon Cancer By Polyphenols From Whole Cranberry, Catherine Neto, Anne Liberty, Sarah Frade, Anuradha Tata, Tracie Ferreira, Mingyue Song, Xian Wu, Hang Xiao

UMass Center for Clinical and Translational Science Research Retreat

The ability of cranberry fruit extracts to inhibit colon carcinogenesis is under investigation using a combination of in vitro and in vivo methods. Compounds isolated from cranberry fruit (Vaccinium macrocarpon) including oligomeric polyphenols known as proanthocyanidins (PACs) decreased the proliferation of HCT116 and HT-29 colon cancer cells, induced apoptosis and reduced the formation of tumor colonies. Treatment of HCT116 colon cancer cells with cranberry polyphenols produced changes in expression of genes and proteins associated with the MAPK pathway, confirmed by microarray analysis, quantitative (Q)-PCR and Western blotting. Based on cranberry's effect in vitro, a feeding study was conducted ...


Inhibition Of Bromodomain Proteins In Treatment Of Diffuse Large B-Cell Lymphoma, Sally E. Trabucco, Rachel M. Gerstein, Andrew M. Evens, James E. Bradner, Leonard D. Shultz, Dale L. Greiner May 2014

Inhibition Of Bromodomain Proteins In Treatment Of Diffuse Large B-Cell Lymphoma, Sally E. Trabucco, Rachel M. Gerstein, Andrew M. Evens, James E. Bradner, Leonard D. Shultz, Dale L. Greiner

UMass Center for Clinical and Translational Science Research Retreat

Only ~50% of patients with diffuse large B-cell lymphoma (DLBCL), the most common and aggressive subtype of non-Hodgkin’s lymphoma, enter long-term remission after standard chemotherapy, and patients who do not respond to treatment have few options. Therefore, there is a critical need for effective and targeted therapeutics for DLBCL. Recent studies highlight the incidence of increased c-MYC protein in DLBCL and the correlation between high levels of c-MYC and poor survival prognosis of DLBCL patients, suggesting that c-MYC is a compelling therapeutic target for DLBCL therapy. The small molecule JQ1 suppresses c-MYC expression through inhibition of the BET family ...


Molecular Mechanisms Of Fsh Muscular Dystrophy Pathogenesis, Peter L. Jones, Takako I. Jones May 2013

Molecular Mechanisms Of Fsh Muscular Dystrophy Pathogenesis, Peter L. Jones, Takako I. Jones

UMass Center for Clinical and Translational Science Research Retreat

Discussion of a new research initiative at UMass Medical School focused on the pathogenesis of Facioscapulohumeral Muscular Dystrophy (FSHD) and efforts towards diagnostics and therapeutics. This presentation is part of the retreat mini-symposium entitled: Neuromuscular Diseases: Pathogenesis and the Road to Therapeutics.


Glyconanoparticle Uptake Profile In Lung Carcinoma Cells, Kalana W. Jayawardana, H. Surangi N. Jayawardena, Thareendra De Zoysa, Mingdi Yan May 2013

Glyconanoparticle Uptake Profile In Lung Carcinoma Cells, Kalana W. Jayawardana, H. Surangi N. Jayawardena, Thareendra De Zoysa, Mingdi Yan

UMass Center for Clinical and Translational Science Research Retreat

Non-small cell lung carcinoma (NSCLC) is responsible for nearly 85% of lung cancer, and early diagnosis and treatment of lung cancer can circumvent possible death. We focus on glyconanoparticles with a magnetic or a fluorescent core that act as multivalent glyco-scaffold to study cell surface interaction and internalization. The glyconanoparticles were synthesized by conjugating various carbohydrates on magnetic nanoparticles and fluorescent silica nanoparticles by a photocoupling technique developed in our laboratory. The size of nanoparticles used varies from 6 nm to 60 nm. The resulting glyconanoparticles were treated with human adenocarcinoma non-small lung epithelial cells (A549) and the primary small ...


Regulation Of Androgen Receptor Co-Regulators By Activation Of The Cxcl12/Cxcr4 Axis: A Microarray And Proteomics Approach, Sathish Kasina, Lesa Begley, Henriette Remmer, Jill A. Macoska May 2013

Regulation Of Androgen Receptor Co-Regulators By Activation Of The Cxcl12/Cxcr4 Axis: A Microarray And Proteomics Approach, Sathish Kasina, Lesa Begley, Henriette Remmer, Jill A. Macoska

UMass Center for Clinical and Translational Science Research Retreat

Background: Activation of the CXCL12/CXCR4 axis is known to stimulate androgen-independent activation of the androgen receptor (AR) in the LNCaP prostate cancer cell line. In the present study, the CXCL12-stimulated expression profile of androgen responsive genes (ARGs) and AR:co-regulator protein:protein interactions has been identified by microarray and proteomic analysis, respectively.

Methods: To directly identify proteins that interacted with the AR in response to CXCL12 stimulation, LNCaP cells treated with CXCL12 were subjected to a total proteomics analysis after co-immunoprecipitation (co-IP) with anti-AR antibody. AR- interacting proteins from co-IP were pre-fractionated by SDS-PAGE, in-gel trypsin digested, and analyzed ...