alexa Screening For P53-MDM2 Small Molecule Inhibitors: Cancer Therapeutic Target | 72465
ISSN: 0974-276X

Journal of Proteomics & Bioinformatics
Open Access

Like us on:
OMICS International organises 3000+ Global Conferenceseries Events every year across USA, Europe & Asia with support from 1000 more scientific Societies and Publishes 700+ Open Access Journals which contains over 50000 eminent personalities, reputed scientists as editorial board members.

Open Access Journals gaining more Readers and Citations

700 Journals and 15,000,000 Readers Each Journal is getting 25,000+ Readers

This Readership is 10 times more when compared to other Subscription Journals (Source: Google Analytics)

9th International Conference on Structural Biology
September 18-20, 2017 Zurich, Switzerland

Ameena M Ali, Jack Atmaj, Matthew R Groves, Neochoritis, C G, Daniel G Rivera, Tad Holak and Alexander Domling
Faculty of Science and Engineering, Drug Design Department, Groningen University, Netherlands
Telesispharma B.V, Groningen, Netherlands
Faculty of Chemistry, University of Havana, Cuba
Faculty of Biochemistry, Biophysics and Biotechnology, Jagiellonian University, Poland
Posters & Accepted Abstracts: J Proteomics Bioinform
DOI: 10.4172/0974-276X-C1-101
Abstract
Statement of the Problem: p53 is the key tumor suppressor protein and the guardian of the genome. Mutation or deletion in TP53 gene, which encode p53 protein, is the main trigger for >50% of human cancer due to the protein’s central role in cell cycle checkpoints. This lead to over-expression of MDM2 and down regulation of mutated P53 in parallel. MDM2 (Mouse Double Minute 2, also named Hdm2 in humans) is an oncoprotein that negatively regulates the apoptotic function of p53 via transactivation inhibition in two manners: either by direct protein- protein interaction (PPI) or by targeting P53 to proteasome degradation through its E3 ligase activity. The purpose of this study is to design and optimize small molecules that block the PPI between P53 and MDM2 as a novel non-genotoxic target for anticancer drugs. Methodology & Theoretical Orientation: MDM2 protein was first expressed in inclusion bodies, refolded and then purified. Highly pure MDM2 was used for optimized compounds screening and analyzing their binding to MDM2. To achieve this goal protein was co-crystallized with the optimized compounds and their binding modes will be characterized by X-ray crystallography. Moreover, the binding kinetics of the same compounds was estimated using fluorescence polarization (FP) and microscale thermophoresis (MST). Findings: Some of the screened compounds showed a high binding affinity toward MDM2 with Kd values down to nano-molar values. Conclusion & Significance: We anticipate that our studies will result in further improvements in the affinity of the inhibitors targeting the MDM2
Biography

Ameena M Ali is a PhD student in Drug Design Department at Groningen University since 2015. She conducts her structural biology and crystallography research under the supervision of Prof. Alexander Dömling and Dr. Matthew Groves. She became the main Researcher in MDM2: P53 (PPI) inhibitor discovery and screening in 2016. She was honored with a Master’s degree in Medical Biotechnology from the Arabian Gulf University, Kingdom of Bahrain in 2012, while she received her Bachelor’s degree in 2003 from Qatar University in Biological and Environmental Sciences with excellence. Most of her research work focused on diseases and treatment strategy development for critical diseases such as, point mutations in LDL gene, Diabetes Mellitus and Cancer.

image PDF   |   image HTML
 

Relevant Topics

Peer Reviewed Journals
 
Make the best use of Scientific Research and information from our 700 + peer reviewed, Open Access Journals
International Conferences 2018-19
 
Meet Inspiring Speakers and Experts at our 3000+ Global Annual Meetings

Contact Us

Agri & Aquaculture Journals

Dr. Krish

[email protected]

1-702-714-7001Extn: 9040

Biochemistry Journals

Datta A

[email protected]

1-702-714-7001Extn: 9037

Business & Management Journals

Ronald

[email protected]

1-702-714-7001Extn: 9042

Chemistry Journals

Gabriel Shaw

[email protected]

1-702-714-7001Extn: 9040

Clinical Journals

Datta A

[email protected]

1-702-714-7001Extn: 9037

Engineering Journals

James Franklin

[email protected]

1-702-714-7001Extn: 9042

Food & Nutrition Journals

Katie Wilson

[email protected]

1-702-714-7001Extn: 9042

General Science

Andrea Jason

[email protected]

1-702-714-7001Extn: 9043

Genetics & Molecular Biology Journals

Anna Melissa

[email protected]

1-702-714-7001Extn: 9006

Immunology & Microbiology Journals

David Gorantl

[email protected]

1-702-714-7001Extn: 9014

Materials Science Journals

Rachle Green

[email protected]

1-702-714-7001Extn: 9039

Nursing & Health Care Journals

Stephanie Skinner

[email protected]

1-702-714-7001Extn: 9039

Medical Journals

Nimmi Anna

[email protected]

1-702-714-7001Extn: 9038

Neuroscience & Psychology Journals

Nathan T

[email protected]

1-702-714-7001Extn: 9041

Pharmaceutical Sciences Journals

Ann Jose

[email protected]

1-702-714-7001Extn: 9007

Social & Political Science Journals

Steve Harry

[email protected]

1-702-714-7001Extn: 9042

 
© 2008- 2018 OMICS International - Open Access Publisher. Best viewed in Mozilla Firefox | Google Chrome | Above IE 7.0 version