View Poster: 2020 AACR: Fragment-based drug discovery to identify small molecule allosteric inhibitors of SHP2
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Downes et al., “Design and Synthesis of 56 Shape-Diverse 3D Fragments”; Chemistry: A European Journal, 2020 https://chemistry-europe.onlinelibrary.wiley.com/doi/pdfdirect/10.1002/chem.202001123
View Poster: ASTX660, a non-peptidomimetic antagonist of cIAP1/2 and XIAP, promotes an anti-tumor immune response in pre-clinical models of T-cell lymphoma Summary ASTX660 is a potent, non-peptidomimetic antagonist of the cellular and X-linked inhibitors of apoptosis proteins (cIAP1/2 and XIAP), which is currently being tested in a first in human phase I-II study in patients […]
View Poster: Different pharmacodynamic profiles of ERK1/2 inhibition can elicit comparable anti-tumor activity Summary The mitogen activated protein kinase (MAPK) pathway is frequently dysregulated in cancer, leading to activation of the downstream kinases ERK1/2 (ERK). Phosphorylation of ERK substrates such as p90RSK (RSK) leads to cancer cell proliferation. Clinical efficacy can be limited by toxicity, […]
View Poster: Discovering Small-Molecule Modulators of Autophagy for Neurodegeneration Summary Autophagy is a major protein degradation pathway with proven roles in protecting neurons against accumulation of aggregation-prone proteins and obsolete mitochondria. Genetics of human-disease and mouse-knockout studies highlight the connection between autophagy dysfunction and neurodegeneration, and therefore finding a way to augment autophagic-flux seems a […]
View Poster: A novel ERK1/2 inhibitor has potent activity in NRAS-mutant melanoma cancer models Summary NRAS mutations occuring 15- 20% of melanoma cancer patients. Currently there is no approved molecularly targeted therapy for NRAS mutant melanoma, an indication which is associated with aggressive clinical outcome and a poor prognosis. The NRAS mutation leads to constitutive […]
View Poster: Characterisation of a novel ERK1/2 inhibitor, which modulates the phosphorylation and catalytic activity of ERK1/2 Summary The MAPK pathway is commonly hyper-activated in human cancers due to the occurrence of oncogenic mutations in RAF and RAS, and multiple studies have demonstrated that MAPK pathway inhibition suppresses the growth of such cancer cells. MAPK […]
Erlanson et al., “Fragment-to-Lead Medicinal Chemistry Publications in 2018”; Journal of Medicinal Chemistry, 2020 https://pubs.acs.org/doi/10.1021/acs.jmedchem.9b01581
Coyle et al., “Applied Biophysical Methods in Fragment-Based Drug Discovery”; SLAS DISCOVERY, 2020 https://journals.sagepub.com/doi/full/10.1177/2472555220916168?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub%20%200pubmed
Osbourne et al., “Fragments: where are we now?”; Biochemical Society Transactions, 2020 https://portlandpress.com/biochemsoctrans/article-abstract/48/1/271/221949/Fragments-where-are-we-now?redirectedFrom=fulltext