“The Rhodadyn™ compounds represent a completely new chemical scaffold upon which we have designed and engineered a dynamin inhibitor. They represent novel chemistry”.
Bristol, UK, Sydney and Newcastle, Australia (PRWEB UK) 4 April 2012
Abcam, together with The University of Newcastle and the Children's Medical Research Institute, have today announced the expansion of their range of small molecule dynamin inhibitors for research. These are novel tools for investigating clathrin-mediated endocytosis and synaptic vesicle recycling and are available in the Abcam Biochemicals range. The agreement was facilitated by Bio-Link Australia, a life sciences commercialisation company.
The laboratories of Professor Adam McCluskey (University of Newcastle) and Professor Phil Robinson (Children's Medical Research Institute) have developed a potent, cell permeable inhibitor of dynamin, Rhodadyn C10™, which potently inhibits clathrin-mediated endocytosis via dynamin inhibition. The Rhodadyn C10™ dynamin inhibitor was recently published in ACS Medicinal Chemistry Letters, by a collaboration involving scientists from the University of Newcastle, Children’s Medical Research Institute, Leibniz Institut für Molekulare Pharmakologie and Freie Universität Berlin in a paper entitled “The Rhodadyns™, a new class of small molecule inhibitors of dynamin GTPase activity” (Robertson et al., ACS Medicinal Chemistry Letters, 2012, 3, DOI: 10.1021/ml200284s).
In addition to clathrin-mediated endocytosis, the dynamin II isoform has also been implicated in some forms of clathrin-independent membrane trafficking, facilitates a number of cellular processes such as cell migration, and is important in mitosis at the cytokinesis stage as well as metastasis. The Dynamin I isoform regulates neurotransmission through the maintenance of synaptic vesicle recycling, ensuring retrieval of vesicles for refilling and reuse at the synapse.
The Rhodadyn C10™ dynamin inhibitor complements a range of other dynamin inhibitors available in the Abcam Biochemicals range from March 2011, which are designed to selectively target different domains of dynamin. Together they provide research tools for understanding cellular vesicle trafficking. All dynamin inhibitors reported to date block the function of both dynamin I and dynamin II with approximately similar potency.
Professor McCluskey said “The Rhodadyn™ compounds represent a completely new chemical scaffold upon which we have designed and engineered a dynamin inhibitor. They represent novel chemistry”.
Professor Robinson remarked "For cell biologists to demonstrate a process is dynamin-dependent, it is important to utilise more than one dynamin inhibitor from different chemical classes, as well as their inactive analogues. This reduces the likelihood of confounding off-target effects. The availability of the Rhodadyn C10™ compound and its inactive control add value to the growing palette of dynamin inhibitors, providing researchers with much greater options".
Steve Roome PhD, General Manager for Abcam Biochemicals, comments "The introduction of these potent dynamin inhibitors is a great addition to our dynamin tool box. They will allow researchers to study the role of endocytosis in multiple cell types and in neurotransmission with the hope of uncovering additional therapeutic avenues in neurological disease including epilepsy, Alzheimer’s and schizophrenia.”
Highly potent cell permeable dynamin I GTPase activity inhibitor (IC50 = 7.1 μM). Blocks clathrin-mediated endocytosis of transferrin when applied for 30 minutes to U2OS cells in culture (IC50 = 7.0 μM).
Negative control for the Rhodadyn C10™ compound. Demonstrates no significant inhibition of dynamin I in vitro GTPase activity up to 300 μM and has no effect on clathrin-mediated endocytosis of transferrin when applied for 30 minutes to U2OS cells in culture.
Rhodadyn C10™ and Rhodadyn B10™ are sold under exclusive license from Children’s Medical Research Institute and Newcastle Innovation Ltd. Rhodadyn™, Rhodadyn C10TM and Rhodadyn B10™ are trademarks of Children’s Medical Research Institute and Newcastle Innovation Ltd.
About the Children's Medical Research Institute
Established in 1958 by Sir Lorimer Dods' goal to advance and enhance health care for the benefit of the community. Today, CMRI is committed to excellence in biomedical science, engaging in fundamental research into the causes, prevention, early diagnosis and relief or cure of disease in children. CMRI scientists aim to understand the basic inner workings of our cells and to find better ways to prevent and treat diseases which rob children of their chance at a long and healthy life. Many diseases that affect children, such as cancer and epilepsy, have the same origins in adults.
About The University of Newcastle
Established in 1965, the University of Newcastle in regional NSW is the most research intensive university outside of an Australian capital city. Ranked ninth among Australia's universities for research, Newcastle's reputation is for innovation, excellence and research with impact. http://www.newcastle.edu.au
About Bio-Link Australia
Bio-Link Australia Pty Ltd. is a life sciences commercialisation company which facilitates partnerships in the biopharma and diagnostic industries. Bio-Link has offices in Sydney and Melbourne, Australia, and clients including leading Australian and international medical research institutions and biotechnology companies.
Abcam is a producer and distributor of high quality research-grade antibodies and associated protein research tools. Since it was founded in 1998 by Dr. Jonathan Milner, Abcam has enjoyed rapid growth and is widely accredited as a leading company in its industry. Headquartered in Cambridge (UK), Abcam has subsidiary offices in Bristol (UK), Cambridge, MA. (USA), Eugene, OR. (USA), Tokyo (Japan) and Hong Kong (China), allowing them to serve a global customer base. Abcam employs over 325 staff across its operating companies.
Abcam revolutionized the buying of antibodies via its website and their online catalogue consists of tens of thousands of products, supported by hundreds of thousands of pages of accompanying data. The catalogue includes a growing range of non-antibody products such as proteins, peptides, lysates, immunoassays and other kits and biochemicals. Products are available for life science research and distributed to academic and commercial users. A highly developed e-commerce platform, which includes regional websites for the Chinese and Japanese markets, allows customers to access up-to-date and detailed technical product data sheets at the
Company's website http://www.abcam.com
Professor Adam McCluskey
University of Newcastle
Phone: +612 4921 6486
Email: Adam.McCluskey (at) newcastle (dot) edu (dot) au
Professor Phil Robinson
Children's Medical Research Institute
Phone: +612 8865 2800
Email: probinson (at) cmri (dot) org (dot) au
Dr Christian Toouli
Phone: +612 9571 8815
Email: c.toouli (at) bio-link (dot) com
Dr Steve Roome
Phone: +44 (0)117 982 9988
Email: steve.roome (dot) abcam (dot) com