News
2015
A new class act: front cover highlights cannabinoid receptor work
A paper on work identifying a new class of selective cannabinoid receptor 2 (CB2R) agonists was chosen for the front cover image by Bioorganic and Medicinal Chemistry. The featured paper describes new CB2R activating molecules which have promise for further in vitro and in vivo studies, leading to the new development of drug candidates with potential for the treatment of a range of inflammatory diseases, including atherosclerosis and arthritis. Access online.
Revealing a new drug development strategy
A recent paper in the Journal of Medicinal Chemistry introduces an emerging new paradigm 'Stemistry' for the search and development of new agents targeting resident stem cells involved in repair processes in the tissues they exist. Access online.
No news items this month
Muscular Dystrophy UK research team visit
We were delighted to welcome the CEO, Robert Meadowcroft, and representatives of Muscular Dystrophy UK to the CRL, early this month, to provide them with an update on the work being done on the utrophin modulation programme. Meetings were held throughout the day and a presentation given by Aini Vuorinen on her recent work on newly identified compounds that modulate the up-regulation of utrophin. To read more about the visit, take a look at the news item on the Muscular Dystrophy UK website by clicking here.
Presentation at the 10th Annual Drug Discovery Chemistry Conference
Amy Varney was invited to give an oral presentation at the Drug Discovery Chemistry Conference in San Diego, CA. following the submission of her poster entitled 'Methylation and Cancer: Inhibiting the PRMTs and looking for new epigenetic markers'. The conference, in it's tenth year invited medicinal chemists from Pharma and Biotech to enjoy presentations and posters featured in six key themes (Protein-Protein Interactions; Inflammation Inhibitors; Kinase Inhibitor Chemistry; Macrocyclics and Constrained Peptides; Fragment-based Drug Discovery; and Epigenetic Inhibitor Discovery, where Amy's work was featured).
Welcome Dr. Nicky Willis
We are pleased to welcome Dr. Nicky Willis to the group. He'll be working on a Summit Therapeutics-funded project optimising utrophin modulators for Duchenne Muscular Dystrophy therapy. Nicky joins us following a post-doctoral project at GlaxoSmithKline, in collaboration with Prof. Graham Sandford (University of Durham).
Publication: second generation compound with exciting potential for the treatment of DMD
A new Human Molecular Genetics paper highlights some exciting results of the second generation compound, SMT 022357, shown to have utrophin modulation activity for the potential treatment of Duchenne Muscular Dystrophy. The compound, through an established mouse model, has exhibited improved physiochemical properties and a more robust metabolism profile than the original compound. These results support the continued development of the compound for the treatment of the lethal, muscle-wasting disease. Access online.
Welcome Dr. Laurence Silpa
We are pleased to announce that Dr. Laurence Silpa will be joining the group on 15th June to work on an EU Innovative Medicines Initiative (IMI) funded project, part of the Oxford-led StemBANCC consortium. Building on the work of Gu Liu, Laurence's project will focus on small molecule manipulation of induced pluripotent stem cells.
Welcome Bruno Marinic
In collaboration with Prof. David Sattelle (UCL) and Prof. Kathryn Else (University of Manchester), Bruno will be working on an anti-parasitic agent project during his summer vacation placement starting on 1st July, for 5 weeks.
Congratulations!
Well done to Marcus, Josh, Robyn and Jessica who have recently completed their Part II projects.
Prize: Robyn Zorab
Congratulations Robyn - after successfully completing her Part II, she was awarded the Examiners' Special Prize for Chemical Biology. The prize signifies the culmination of her hard work over the last year and so well done Robyn!
Welcome Jonathan Taylor
Jonathan joins us for his summer vacation placement starting 13th July, for seven weeks. He'll be working with Caitlin on the British Heart Foundation funded project to support the development of high throughput screening assays to identify small molecule activators of the resident progenitor cells of the human adult epicardium.
Welcome Daniel Sowood
In collaboration with Prof. David Sattelle (UCL) and Prof. Kathryn Else (University of Manchester), Daniel will be working on an anti-parasitic agent project during his summer vacation placement starting on 24th July, for 10 weeks.
Dr Kristína Csatayová
The department is very sad to announce that Dr Kristína Csatayová died on 26th July at the age of 32. Kristína secured her DPhil under the supervision of Professor Steve Davies last year, and was a postdoctoral research assistant to both Steve Davies and Angela Russell. She will be remembered for her outstanding contribution to chemistry and for being an exceptional scientist and human being. She will be greatly missed amongst her peers, friends and families. A donation to the Sobell House Hospice Charity (https://www.justgiving.com/Kristina-Csatayova) would be a wonderful way to support a cause that is important to her family and friends, and to honour Kristína who lost her life after a fierce battle with cancer.
Thesis submission - James Egleton
Well done to James who has submitted his thesis this month.
Moving on to pastures new - Gu Liu
Gu Liu has left the group to join Accenture - although sad to see her leave, we wish her the best of luck in her new role.
Welcome Minjun Yang
Minjun joins us for his summer vacation sponsored placement starting 1st August, for eight weeks. Minjun is working, in collaboration with David Greaves of the BHF Centre of Research Excellence, on small molecule modulators of chemotaxis.
Welcome Karen Heathcote
Karen has joined our group for four weeks, from 3rd August, to work on small molecule modulators of utrophin for Duchenne Muscular Dystrophy therapy, a project in collaboration with Professor Dame Kay E. Davies (Department of Physiology, Anatomy and Genetics, University of Oxford) and Summit Therapeutics plc.
Welcome Maria Chatzopoulou
Maria has joined the AJR group to work on small molecule modulators of utrophin for Duchenne Muscular Dystrophy therapy, a project in collaboration with Professor Dame Kay E. Davies (Department of Physiology, Anatomy and Genetics, University of Oxford) and Summit Therapeutics plc.
Summit Therapeutics plc announces Phase 1b clinical trial success
On 17th August, Summit Therapeutics revealed that their primary objective for the Phase 1b Modified Diet clinical trial of SMT C1100 for the treatment of Duchenne Muscular Dystrophy (DMD) had been achieved. The compound has received orphan drug designation in the US and Europe and will be progressed to Phase 2 open-label trial in 4Q2015. To read more about this story, click here. See also www.summitplc.com.
Presentation: AJR at the American Chemical Society (ACS) 250th meeting - Boston
AJR gave a presentation entitled 'Discovery of small molecule utrophin modulators for the therapy of Duchenne Muscular Dystrophy (DMD)' on Sunday 16th August at the celebratory 250th ACS meeting: Innovation - from Discovery to Application.
Presentation: Graham Wynne at RSC-SCI Medicinal Chemistry symposium
Graham presented a talk entitled 'Discovery of compounds which modulate utrophin expression for the treatment of Duchenne Muscular Dystrophy' at the 18th SCI/RSC Medicinal Chemistry conference in Cambridge on 16th September.
Welcome Part II students
Welcome to our new Part IIs: Samantha Cloake, Ryan Davies, Anna Olerinyova and Jessica Reynolds.
Welcome Christopher Lindsay and Daniel Lucy
Welcome to the AJR group, Chris and Daniel who are beginning their British Heart Foundation (BHF) Centre of Research Excellence DPhil in Medicinal Chemistry for Cardiovascular Disease on 1st October.
Thesis submission - Amy Varney
Congratulations to Amy who has submitted her thesis this month.
Publication: Augmentation of creatine in the heart
A paper has been published in Mini-reviews in Medicinal Chemistry discussing the evidence in support of creatine elevation and the pharmacological approaches currently available. Access online...
Publication: The Derivation of Primary Human Epicardium-Derived Cells
Congratulations to Caitlin on her new Current Protocols in Stem Cell Biology paper this month describing techniques to establish and maintain human epicardium explant cultures from patient-derived right atrial appendage biopsies and methods to probe the resultant outgrowth of human epicardium-derived cells (hEPDCs). Access online...
Multi-year £3.3M extension of strategic alliance with Summit Therapeutics plc
Summit Therapeutics plc has announced a multi-year extension of its exclusive strategic alliance with the research teams of Prof Angela Russell, Prof Steve Davies and Prof Dame Kay Davies (DPAG) until November 2019, with an option to extend it for a further 12 months, to support and accelerate development of future generation utrophin modulators for the treatment of the progressive muscle wasting disorder, DMD. Summit Therapeutics will continue to sponsor a drug discovery and development programme in the University of Oxford research laboratories to identify and develop oral utrophin modulators for the treatment of DMD. This research programme, originally running to November 2016, will now continue until November 2019 with a option to extend it for a further 12 months. As part of the extension, Summit Therapeutics will increase the funding to £0.83 million a year starting in November 2015.
Congratulations Dr Egleton!
Well done to James who successfully passed his DPhil viva on 26th November.
Well done Dr Varney!
Congratulations to Amy who successfully passed her DPhil viva on 4th December.
Summit Therapeutics plc announces first research milestone achieved in strategic alliance
The company has announced that two series of novel utrophin modulators have been nominated to progress into lead optimisation studies, achieving the first research milestone as part of the strategic alliance. The partnership aims to develop utrophin modulators for the treatment of patients for the progressive muscle-wasting disease Duchenne Muscular Dystrophy (DMD).