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The non-peptidomimetic cIAP1/2 and XIAP antagonist tolinapant promotes an anti-tumour immune response in T-cell lymphoma

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) [1], which is currently being tested in a first in human phase I-II clinical trial in patients with […]

Identification of potent small molecule allosteric inhibitors of SHP2

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 […]

Combined inhibition of SHP2 and ERK enhances anti-tumor effects in preclinical models

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 […]

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

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 […]