St. Denis et al., “Fragment-based drug discovery: opportunities for organic synthesis”; RSC Medicinal Chemistry, 2021 https://pubs.rsc.org/en/content/articlelanding/2021/md/d0md00375a#!divAbstract
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Jahnke et al., “Fragment-to-Lead Medicinal Chemistry Publications in 2019”; Journal of Medicinal Chemistry, 2020 https://doi.org/10.1021/acs.jmedchem.0c01608
View Poster: The non-peptidomimetic cIAP1/2 and XIAP antagonist tolinapant promotes an anti-tumour immune response in T-cell lymphoma Summary Tolinapant (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 clinical trial in patients with […]
View Poster: Identification of potent small molecule allosteric inhibitors of SHP2 Summary SHP2 is a ubiquitously expressed protein tyrosine phosphatase required for growth factor signalling downstream of receptor tyrosine kinases (RTKs) and plays a role in regulating many cellular processes. Genetic knockdown and pharmacological inhibition of SHP2 inhibits proliferation of RTK-driven cancer cell lines and suppresses […]
View Poster: Combined inhibition of SHP2 and ERK enhances anti-tumor effects in preclinical models Summary MAPK signalling is frequently dysregulated in cancer. The pathway can Panel composition and the number of responding cell lines Examples of dose-response curves Anti-tumor activity of SHP2i, ASTX029 and combination in MIA PaCa-2 xenograft be targeted by inhibition of different […]
View Poster: The clinical candidate, ASTX029, is a novel, dual mechanism ERK1/2 Inhibitor and has potent activity in MAPK-activated cancer cell lines and in vivo tumor models Summary The MAPK signaling pathway is commonly upregulated in human cancers due to oncogenic mutations of upstream components such as BRAF or KRAS. MAPK pathway inhibition has been […]
Cadilla et al., “The exploration of aza-quinolines as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors with low brain exposure”; Bioorganic & Medicinal Chemistry, 2020 https://doi.org/10.1016/j.bmc.2020.115791
View Poster: 2020 AACR: Fragment-based drug discovery to identify small molecule allosteric inhibitors of SHP2
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 […]