Month: April 2021

Fused tetrahydroquinolines (THQ): potential PAINS compounds in a recent HTS for moesin-CD44 pathway inhibitors

Posted onAuthorJoel Annor GyamfiLeave a comment

Joel K. Annor-Gyamfi, Felix Nwogbo, Kun Qian, Yuhong Du, Kenneth H. Pearce Jr, Opher Gileadi, Haian Fu, Stephen V. Frye and Alison D. Axtman https://doi.org/10.5281/zenodo.4685122 Alzheimer’s disease (AD) is the most common cause of dementia worldwide but very few therapeutic options exist despite multiple high-profile but failed clinical trials. And as the population of the Read More …

Distinguishing between catalytic and non-catalytic pockets in the ligandable human genome: InterPro analysis

Posted onAuthorEvianne RoversLeave a comment

As describe in my previous post, my goal is to discover non-catalytic druggable pockets in human enzymes. These pockets could potentially be exploited for the design of ProxPharm compounds (chimeric compounds that bring two proteins in close proximity to elicit an effect of one protein on the other1). An essential aspect for the design of Read More …

The Preparation of Allosteric SYK Inhibitor X1 and Investigation of a Covalent Inhibition Mechanism

Posted onAuthorFrances PotjewydLeave a comment

Frances M. Potjewyd and Vittorio Katis http://doi.org/10.5281/zenodo.4670214 Spleen Tyrosine Kinase (SYK) has a reported role in AD pathology and was identified as a target for the TREAT-AD (Target Enablement to Accelerate Therapy Development for Alzheimer’s Disease) program.1–3 We are focusing drug discovery efforts on the inhibition of SYK and more specifically, inhibition of the interaction Read More …