Therapeutics Development
Overview
The Vancouver Prostate Centre’s comprehensive Therapeutics Development core, consisting of Pharmacology and Drug Design units, helps clients to identify novel drug candidates using methods of computational drug design and cheminformatics, followed by hit-to-lead optimization combined with comprehensive experimental evaluation of pharmacological activity. Our expert team is experienced in both computational and experimental aspects of conventional drug discovery and can seamlessly integrate their services with The Vancouver Prostate Centre’s other units to provide all the necessary components of focused translational research.
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Therapeutics Development Overview / Expertise and Services
Expertise and Services
Expertise
Our expert team of scientists and technicians work in a state-of-the-art facility and balance work in research and development, which integrates seamlessly with the genome analysis, pathology and functional genomics services, as well as the clinical trials unit, to realize a comprehensive and focused translational research centre. The Therapeutic Development core includes the Gobind Khorana Protein Engineering Core.
Services
- Drug target identification and characterization
- Computational drug discovery (virtual screening, combinatorial library construction, structure-activity modeling)
- Computer-aided hit-to-lead optimization (ADME and Toxicity prediction, bioavailability and selectivity optimization)
- GC and LC-MS assays for a variety of chemistries in biological matrices for GLP studies
- Biomarker assay development
- Single agent studies and combination studies
- Pharmacodynamic and biomarker analysis of novel drugs in human clinical trials
Therapeutics Development Overview / Gobind Khorana Protein Engineering Core
Gobind Khorana Protein Engineering Core
The Gobind Khorana Protein Engineering Core was established after a successful application to the Canadian Foundation for Innovation (CFI) and British Columbia Knowledge Development Fund (BCKDF), to create an Accelerated Drug Discovery Using Clinical Translation (ADDUCT) program, and is generously supported by a grant from the Aqueduct Foundation on behalf of an anonymous donor.
This gift represents the donor's commitment to a tradition of innovation in science in BC as a long-term investment in the people of British Columbia. The donor had great respect for the late Gobind Khorana and chose to name this research platform in his honour.
Professor Har Gobind Khorana (1922 – 2011) was an Indian-born biochemist who was responsible for constructing the first synthetic gene. Despite his humble background, his aptitude and brilliance shone early on. After receiving his Doctorate, Khorana studied proteins and nucleic acids at the University of Cambridge. In 1952, he was recruited by UBC and created an outstanding research program in Vancouver. He later moved to the US to work, gaining international reputation and later won the Nobel Prize in Physiology or Medicine in 1968, along with a myriad of other awards until his death in 2011. He is revered as fiercely loyal, a deep thinker and most importantly, a visionary pioneer in his field.
This Core provides expertise and infrastructure to provide researchers protein engineering support in areas such as cancer target expression and purification, biophysical characterization of samples (structure, dynamics, stability and interactions), and drug screening and validation.
In order to validate and optimize cancer therapeutics, the core provides the following support to the scientific community:
- Protein expression and purification
- Molecular biology and biochemistry expertise to design, clone and express cancer targets alone or in complex with stabilizing partners
- Bacterial and mammalian expression
- Production of high-quality samples for biophysical and/or structural studies
- Biophysical characterization of protein integrity
- Analysis of protein quality, proper folding and stability
- Determination of the presence of protein aggregation and the percentage of protein monodispersity
- Drug validation
- Testing of binding affinity of small molecule inhibitors designed to disrupt the activity of cancer targets
- Potency ranking of small molecule inhibitors designed to disrupt the activity of cancer targets
Structural characterization of proteins and protein complexes
Should the identified cancer targets lack important structural information or require structural resolution in complex with the inhibitor in order to further optimize the specificity, stability and potency of the molecules, the core provides support to research teams to perform their structural studies through contract research organizations (CRO) and academic collaborations at UBC’s Pt. Grey Campus in the UBC Imaging Labs. The UBC Imaging Labs have acquired some of their equipment as part of the ADDUCT program.
VGH & UBC Hospital Foundation and the Vancouver Prostate Centre are incredibly grateful to the donor and the Aqueduct Foundation for their philanthropic leadership to accelerate research to turn new discoveries into clinical practice.
Key equipment in the Gobind Khorana Protein Engineering Core (PDF)
Projects currently utilizing the expertise of the Gobind Khorana Protein Engineering Core (PDF)
Recent publications from the Gobind Khorana Protein Engineering Core (PDF)
Last updated: October 7, 2020
Therapeutics Development Overview / Therapeutics Development Contacts
Therapeutics Development Contacts
Dr. Artem Cherkasov
Head, Chemoinformatic Drug Design
604-875-4111 ext. 69628
Click here to contact Dr. Cherlasov
View bio for Dr. Artem Cherkasov
Dr. Nada Lallous
Senior Research Scientist
604-875-4111 ext. 63430
Click here to contact Dr. Lallous
View bio for Dr. Nada Lallous