Optimisation of viability assay for DIPG patient-derived cell lines

Background: Evaluation of the efficacy of M4K compounds in DIPG patient-derived cell lines is essential before any promising compounds can be further tested in mouse xenograft models. This approach can aid in narrowing down clinical compound candidates and reduce the time, resources and animal sacrifice needed downstream. A robust and efficient readout for the changes Read More …

Synthesis of promiscuous ALK2 inhibitors-continuation-2

Continuing with our goal to synthesize three compounds as ALK2 inhibitors, let’s refer back to Scheme 2 in the previous post on this topic, compounds 6, 8 and 9 were synthesized in good yields (65-90%), however compound 10 could not be obtained.   Different conditions were tested to induce the cyclization of the bromo-pyrazine-2-carboxamide 9 Read More …

SETDB1 Protein and Its Role in Cancer Progression

The molecular blueprint of the living organisms, deoxyribonucleic acid (DNA), is often wrapped with a family of proteins, called histones, in mammalian cells. The functions of histones are vast, including the protection of DNA, and most importantly, the regulation of gene expression. However, the details of gene regulation function of histones are not clearly understood, Read More …

Project Overview: Huntingtin and its interaction partners

  Huntington’s disease (HD) is a progressive neurological disorder caused by a mutation in the HTT gene which encodes for the huntingtin protein. The current understanding of the function of HTT is limited, and there are only a few sources that indicate that it likely plays a critical role in several intracellular processes such as Read More …