Cyclica and Structural Genomics Consortium co-crystallize DCAF1, a key component in proteasomal degradation, with a novel ligand to support targeted therapeutics discovery
11 November, 2021
Cyclica, the partner of choice for data-driven drug discovery, and the Structural Genomics Consortium (SGC), a global public-private partnership dedicated to open science, have collaborated on a project in support of Target 2035, an initiative to discover probe molecules in support of developing medicines for all.
New look for Target 2035
SGC’s Target 2035 initiative just launched a new website with a fresh look and feel. Users will be able to access information about the project, upcoming webinars, and general updates. Check the Target 2035 Twitter and Linked In accounts for the latest news.
What is Target 2035
Inhibiting a key enzyme that controls a large network of proteins important in cell division and growth paves the way for a new class of drugs that could stop glioblastoma, a deadly brain cancer, from growing.
Researchers at Princess Margaret Cancer Centre, the Hospital for Sick Children (SickKids) and University of Toronto, showed that chemically inhibiting the enzyme PRMT5 can suppress the growth of glioblastoma cells.
On September 8th, 2020, the Royal Society of Canada (RSC) elected Dr. Cheryl Arrowsmith, SGC-Toronto's Chief Scientist, as an RSC Fellow, the highest honour an individual can achieve in the Arts, Social Sciences and Sciences.
Leucine-rich repeat kinase 2 (LRRK2) is the most commonly mutated gene in familial Parkinson’s disease (PD) and is also linked to its idiopathic form. LRRK2 is proposed to function in membrane trafficking and co-localizes with microtubules. Despite LRRK2’s fundamental importance for understanding and treating PD, there is limited structural information on it.
SGC Director, Aled Edwards, speaks to The Future Economy on why Open Science is important in fighting COVID-19, and other related questions, in their series "The COVID-19 Rebound". You can see the full interview here: https://thefutureeconomy.ca/interviews/aled-edwards/
We determined the structure of the TASK-1 potassium ion channel. Mutations in TASK-1 are linked to pulmonary arterial hypertension.
TASK-1 has an unusual X-gate, consisting of two crossed helices. This type of gate is not present in related potassium channels and explains the low activity of TASK-1. We also crystallised TASK-1 in complex with inhibitors and found that they bind in the central cavity, trapped by the X-gate.
This work is a collaboration with Bayer AG and University of Marburg.
(Chapel Hill, N.C.— April 7, 2020) — Today, the Structural Genomics Consortium (SGC), the University of North Carolina at Chapel Hill and the Eshelman Institute for Innovation, announce the launch of the Rapidly Emerging Antiviral Drug Development Initiative (READDI), a global organization formed to discover and develop drugs to put “on the shelf” for clinical trial testing in anticipation of future viral pandemics.