Sygnature Discovery

SEPTEMBER 12, 2024

Cryo-EM Expert microscopists in house and access to high end microscopes for screening and high resolution data collection (Glacios, Tecnai, Titan Krios). Fragment Based Drug Discovery Crystallographic fragment screening using a high solubility curated fragment library devoid of soluble aggregates.

Fragment Screening 52

Fragment Screening RNA Protein Production DNA 52

Molecular Design

JANUARY 12, 2021

> It’s been ages since my last COVID-19 post (How not to repurpose a 'drug') and I’ll kick blogging off for 2021 with a follow up to an even older post (SARS-CoV-2 main protease. Crowdsourcing, peptidomimetics and fragments). Pfizer began a phase I study of the SARS-CoV-2 main protease inhibitor PF-00835321 (K i = 0.27

Fragment Screening 52

Fragment Screening Treatment Nurses Doctors 52

Molecular Design

MAY 26, 2020

A crystallographic fragment screen has been run against SARS-CoV-2 and a number of electrophilic fragments were screened using mass spectroscopy. These two screens serve as a launch pad for the COVID Moonshot which looks interesting (although I’d suggest easing off a bit on the propaganda).

Fragment Screening 52

Fragment Screening Drugs 52

Dark Matter Blog

APRIL 4, 2023

The bulk of my nearly three decades of experience up to that point was with drugging protein targets using a variety of modalities, but principally small molecules. It’s all well and good to say, “we should drug RNA,” but which RNA? Prior to 2015, I had a casual relationship, at best, with targeting RNA. Welcome to the RNA world.

Small Molecule 52

Small Molecule RNA Fragment Screening DNA 52

Molecular Design

JULY 18, 2020

Satchel Paige (1906-1982) The COVID Moonshot and OSC19 are examples of what are sometimes called crowdsourced or open source approaches to drug discovery. Open source drug discovery originated with OSDD in India and it should be noted that the approach has also been pioneered for malaria by OSM.

Biochemical Assays 52

Biochemical Assays Fragment Screening Pharmacokinetics Drugs 52

Sygnature Discovery

JUNE 17, 2024

At Sygnature Discovery, we see biophysics as a core component of drug discovery projects, which can generate data throughout the pipeline. Comprehensive Assay Development for Diverse Applications Our team here at Sygnature Discovery, comprised of expert biophysicists, is highly experienced in a variety of target classes and drug modalities.

Biophysical Assays 52

Biophysical Assays Screening Hits Assay Development Fragment Screening 52

Sygnature Discovery

APRIL 26, 2022

Integrated protein production in drug discovery Peak Proteins’s core technologies include protein expression and purification, alongside protein crystallography, structure determination and mass spectrometry services. During this period the two companies working together have supported a number of integrated drug discovery programmes.

Fragment Screening 40

Fragment Screening Protein Production Protein Expression Production 40

Sygnature Discovery

JUNE 17, 2024

At Sygnature Discovery, we utilise various biophysical technologies to create assays for diverse targets, integral to every stage of the drug discovery process, from hit identification to candidate selection. Covalent drugs may have advantages over non-covalent molecules, such as greater potency and duration of action.

Small Molecule 52

Small Molecule Fragment Screening DNA Science 52

PerkinElmer

JUNE 3, 2022

Inhibiting SARS-CoV-2 Proteases Currently, limited therapeutic options are available to those who are infected with SARS-CoV-2 and attempts to repurpose approved drugs have shown minimal success so far. The second virtual screen focused on optimization of a hit from a previous crystallographic fragment screen.

Fragment Screening 52

Fragment Screening Clinical Trials Vaccine Pharmacokinetics 52

Molecular Design

AUGUST 2, 2020

Paramin panorama Crystallographic fragment screens have been run recently against the main protease (at Diamond ) and the Nsp3 macrodomain (at UCSF and Diamond ) of SARS-Cov-2 and I thought that it might be of interest to take a closer look at why we screen fragments.

Fragment Screening 40

Fragment Screening Computational Chemistry Engineering Drugs 40

Covalent Modifiers

DECEMBER 3, 2024

Screening covalent fragments against purified protein targets reduces the demands on the mass spectrometer with respect to absolute throughput, detection limit, and dynamic range. The system enables primary screening of ∼10,000 covalent fragments per day in pooled format.

Fragment Screening 147

Fragment Screening Compound Screening Small Molecule Drugs 147

Covalent Modifiers

DECEMBER 27, 2024

2024 , e202419736 [link] Protein kinases are important drug targets, yet specific inhibitors have been developed for only a fraction of the more than 500 human kinases. Previously, covalent fragment screens yielded potent and selective compounds for individual kinases such as ERK1/2 but have not been applied to the broader kinome.

Fragment Screening 162

Fragment Screening Drugs 162