Rachel Harding, a researcher at SGC Toronto, appears on Global News discussing her open science experiment. She's welcomed the world to view her research progress in real-time by placing her lab notes online and explaining her results on her blog Lab Scribbles.
Fremont, CA – February 29, 2016 – DiscoverX Corporation, the leading supplier of innovative cell-based assays and services for drug discovery and development, today announced its partnership with the Structural Genomics Consortium (SGC), a public-private organization established in 2003, to develop selective and potent chemical probes for the unexplored human kinome and to promote open sharing of these probes with the scientific community.
TORONTO, February 26, 2016 — University of Toronto researcher Rachel Harding will be the first known biomedical researcher to welcome the world to review her lab notes in real time. The post-doctoral fellow with U of T’s Structural Genomics Consortium (SGC) is also explaining her findings to the general public through her blog. She hopes her open approach will accelerate research into Huntington’s disease.
This month, we talk to Dr Wen Hwa Lee, Strategic Alliances Manager at the Structural Genomics Consortium (SGC), part of the Nuffield Department of Clinical Medicine, about how the SGC is revolutionising the way we think about drug discovery.
We have recently heard a lot about open innovation in drug discovery and biomedicine – with the Structural Genomics Consortium (SGC) being one of the shining examples, mentioned in industry and strategic reports (including RAND, Deloitte and the recent Dowling Report) – can you tell us a bit more about it?
Myeloma UK and the Structural Genomics Consortium (SGC) have entered into an open-access research partnership to discover and characterise novel drug targets for myeloma using structural biology and chemical proteomics.
In this first partnership of its kind in Europe, Myeloma UK and the SGC have explicitly agreed not to file for patents on any of the collaborative research and to make all reagents and knowledge available without restriction to the wider research community, including pharmaceutical, biotech, and academic research groups.
University of Toronto and McGill University scientists are leading an international partnership to discover new and improved drug treatments for tuberculosis, malaria and neglected tropical diseases -- thanks to a contribution from Merck Canada Inc., as well as an additional $5 million supplement to a grant from the Bill & Melinda Gates Foundation. The new funding brings the total investment from the Bill & Melinda Gates Foundation to nearly US $12 million since 2012.
OAKVILLE, ON, Dec. 4, 2015 /CNW/ - Takeda Pharmaceutical Company Limited (Takeda) today announced it has renewed its partnership with the Structural Genomics Consortium (SGC) to fund collective drug research aimed at bringing new, more effective medicines to patients faster. Takeda has invested an additional CAD$7.5 million, adding to its initial investment in 2012 of CAD$5 million.
MONTREAL, Nov. 18, 2015 /CNW/ - AbbVie today announced its continued commitment to the Structural Genomics Consortium (SGC) by providing a cash sponsorship of CDA$7.5 million towards open access research leading to the discovery of new medicines. Today`s announcement coincides with meetings with Ontario and Quebec-based research leaders and AbbVie global research and development business development professionals to assess continued investment.
This probe is available from Sigma and Cayman Chemical.
| Probe | Negative control | |
 |
|  |
GSK864 |
| GSK990 |
GlaxoSmithKline has developed GSK864 [1], a potent and selective inhibitor of mutant IDH1, and has made this available as an SGC chemical probe. GSK864 inhibits IDH1 mutants R132C/R132H/R132G with IC50 values of 9/15/17 nM, respectively, and is moderately selective over wild-type IDH1 and IDH2 mutants/wild-type. Treatment of R132C IDH1 mutant HT-1080 cells for 24 hours with GSK864 results in a dose-dependent reduction of 2-hydroxyglutarate (2-HG), which is not observed with GSK990, a structurally similar compound which is inactive as an IDH1 inhibitor. GSK864 has been shown to be selective in vitro for IDH1 over other classes of proteins (7TMs, ion channels, kinases) and chemoproteomic studies with GSK321, an analog of GSK864, confirm selective binding of IDH1 by this chemical series. GSK864 has a pharmacokinetic profile suitable for in vivo studies.
Chemoproteomics: the selectivity of GSK864 for IDH1 was illustrated by conducting a chemoproteomics experiment with a closely related analog, GSK321 [1]. GSK321 was functionalized so that it could be immobilized to NHS-activated Sepharose beads which were then incubated with a lysate (protein concentration 5 mg/mL) from HT-1080 cells. The experimental plan included using GSK990 and vehicle as control bait. The proteins were eluted from the beads and then subjected to in-gel digestion and labelling with TMT reagents. LC/MS/MS identified over 300 proteins of which only one, IDH1 had IC50 < 200 nM.
| Probe | Negative control | |
|
| |
GSK864 |
| GSK990 |
| Physical and chemical properties for GSK864 | |
| Molecular weight | 560.3 |
| Molecular formula | C30H33FN6O4 |
| MollogP | 3.162 |
| PSA | 98.62 |
| No. of chiral centres | 1 |
| No. of rotatable bonds | 10 |
| No. of hydrogen bond acceptors | 8 |
| No. of hydrogen bond donors | 4 |
| Physical and chemical properties for GSK990 (Negative Control) | |
| Molecular weight | 429.2 |
| Molecular formula | C23H23N7O2 |
| IUPAC name | (7-((1H-imidazol-4-yl)-methyl)-9-((3-methyl-phenylamino)-formyl)-3,7,8-triaza-bicyclo[4.3.0]nona-1(6),8-dien-3-yl)-(1H-pyrrol-2-yl)-methanone |
| MollogP | 1.316 |
| PSA | 85.96 |
| No. of chiral centres | 0 |
| No. of rotatable bonds | 7 |
| No. of hydrogen bond acceptors | 6 |
| No. of hydrogen bond donors | 3 |
|
| Physical and chemical properties for GSK990 (Negative Control) | |
| Molecular weight | 501.2 |
| Molecular formula | C28H28FN5O3 |
| IUPAC name | (7-(4-fluoro-benzyl)-9-((3-(1-hydroxy-ethyl)-phenylamino)-formyl)-5-methyl-3,7,8-triaza-bicyclo[4.3.0]nona-1(6),8-dien-3-yl)-(1H-pyrrol-2-yl)-methanone |
| MollogP | 3.285 |
| PSA | 79.77 |
| No. of chiral centres | 2 |
| No. of rotatable bonds | 8 |
| No. of hydrogen bond acceptors | 6 |
| No. of hydrogen bond donors | 3 |
Through a novel open source approach the molecule has been made freely available to the cancer research community to help discover new therapeutic strategies for cancer patients sooner.