Strippers from outer space: recombinant PNGase F.

Nature has evolved molecules called glycoproteins that are proteins carrying sugar chains (“glycans”). Glycans can make proteins more soluble, they can shield them from the environment, they can be used as calling cards to enable protein-protein recognition; in Eukaryotes, a glucose-on/glucose-off quality control system uses glycans to monitor glycoproteins folding. In general, glycans contribute to Read More …

Gram-scale synthesis of furopyridines

Access to large amounts of core building blocks is essential in drug discovery programs. It enables rapid synthesis of a series which can then give structure activity relationships (SAR) of the drugs and their target. SAR data allows medicinal chemists to determine the group(s) in a structure evoke a change in activity, whether positive or Read More …

Defining Epigenetic Drivers of Medulloblastoma – 01 – Introduction

Defining Epigenetic Drivers of Medulloblastoma – Introduction  Medulloblastoma is a cancer that arises from neural progenitor cells in the brain.  This cancer most commonly occurs in young children ages 1-4, and is the most common type of childhood brain cancer.  Although many cases of medulloblastoma show good prognosis, there are some sub-types of this cancer Read More …

Selectivity against, and action of, TNIK kinase in relation to ALK2.

Sorry I’ve not written for a while. I had some annual leave to use up and then I’ve been helping out with a residential EMBO course that was being co-organised by one of the group leaders in my department. The course was an introduction to a wide variety of biochemical and biophysical techniques. I was Read More …

Production and Purification of Huntingtin interaction partners continued

As the summer continues to progress, so does my project. After the last round of purification, detailed in my previous blog post, I am ready for another round. During this purification, I will be working with SH3G3 and PACN1. PACN1 is responsible for cytoskeletal remodeling through regulation of several other proteins, as well as neuronal Read More …

Protein-Protein Docking for PROTAC discovery

As explained in my previous post [https://openlabnotebooks.org/2714-2/], my goal is to test whether structure-based approaches can guide the design of PROTACs. As a first step, I am evaluating whether protein-protein docking tools can accurately predict the interface between an E3 ligase and its target, a question recently explore by Drummond and Williams.1 This step is Read More …

CaMKK2 Inibitors: Quinoline Analogs

In my last post, I reported a new synthetic route to our quinoline series, Scheme 1. The goal was to overcome prior synthetic challenges and to allow for rapid synthesis of many different analogs over a short period of time. Scheme 1: New synthetic route for generating quinoline analogs I have as a result generated large Read More …

First Round of Huntingtin Interaction Partner Protein Production

To start off my project at the SGC, my supervisor, Dr. Rachel Harding, and I produced and purified three proteins. These proteins were RAB1A, RAB1B, and MECP2. Both RAB1A and RAB1B have functions in the initiation of autophagy, which is a cellular system that helps clean out old debris and malfunctioning parts. MECP2 is a Read More …

Virtual Screening with Molecular Forecaster

You may recall I was in Montreal for the last three months doing an internship with Molecular Forecaster Inc. (MFI), a computational chemistry company. I’m back in Toronto from my internship, ready to jump back into my research, but first I’ll summarize the virtual screening work I did at MFI for USP5. In a previous Read More …