Search Results - "Collie, Iain T"
-
1
Tool inhibitors and assays to interrogate the biology of the TRAF2 and NCK interacting kinase
Published in Bioorganic & medicinal chemistry letters (01-08-2019)“…[Display omitted] The TRAF2 and NCK interacting kinase (TNIK) has been proposed to play a role in cytoskeletal organization and synaptic plasticity and has…”
Get full text
Journal Article -
2
One Scaffold, Three Binding Modes: Novel and Selective Pteridine Reductase 1 Inhibitors Derived from Fragment Hits Discovered by Virtual Screening
Published in Journal of medicinal chemistry (23-07-2009)“…The enzyme pteridine reductase 1 (PTR1) is a potential target for new compounds to treat human African trypanosomiasis. A virtual screening campaign for…”
Get full text
Journal Article -
3
Development of a Series of Pyrrolopyridone MAT2A Inhibitors
Published in Journal of medicinal chemistry (28-03-2024)“…The optimization of an allosteric fragment, discovered by differential scanning fluorimetry, to an in vivo MAT2a tool inhibitor is discussed. The…”
Get full text
Journal Article -
4
HTS and hit finding in academia – from chemical genomics to drug discovery
Published in Drug discovery today (01-12-2009)“…The liaison between academia and the pharmaceutical industry was originally served primarily through the scientific literature and limited, specific…”
Get full text
Journal Article -
5
Development of a 2,4-Diaminothiazole Series for the Treatment of Human African Trypanosomiasis Highlights the Importance of Static–Cidal Screening of Analogues
Published in Journal of medicinal chemistry (13-07-2023)“…While treatment options for human African trypanosomiasis (HAT) have improved significantly, there is still a need for new drugs with eradication now a…”
Get full text
Journal Article -
6
The First Potent and Selective Inhibitors of the Glycine Transporter Type 2
Published in Journal of medicinal chemistry (16-08-2001)Get full text
Journal Article -
7
Discovery of Indoline-2-carboxamide Derivatives as a New Class of Brain-Penetrant Inhibitors of Trypanosoma brucei
Published in Journal of medicinal chemistry (08-10-2015)“…There is an urgent need for new, brain penetrant small molecules that target the central nervous system second stage of human African trypanosomiasis (HAT). We…”
Get full text
Journal Article -
8
Development of Small-Molecule Trypanosoma brucei N-Myristoyltransferase Inhibitors: Discovery and Optimisation of a Novel Binding Mode
Published in ChemMedChem (01-11-2015)“…The enzyme N‐myristoyltransferase (NMT) from Trypanosoma brucei has been validated both chemically and biologically as a potential drug target for human…”
Get full text
Journal Article -
9
Identification of Inhibitors of the Leishmania cdc2-Related Protein Kinase CRK3
Published in ChemMedChem (09-12-2011)“…New drugs are urgently needed for the treatment of tropical parasitic diseases such as leishmaniasis and human African trypanosomiasis (HAT). This work…”
Get full text
Journal Article -
10
A Novel Allosteric Inhibitor of the Uridine Diphosphate N‑Acetylglucosamine Pyrophosphorylase from Trypanosoma brucei
Published in ACS chemical biology (20-09-2013)“…Uridine diphosphate N-acetylglucosamine pyrophosphorylase (UAP) catalyzes the final reaction in the biosynthesis of UDP-GlcNAc, an essential metabolite in many…”
Get full text
Journal Article -
11
Quinol derivatives as potential trypanocidal agents
Published in Bioorganic & medicinal chemistry (15-02-2012)“…Quinols have been developed as a class of potential anti-cancer compounds. They are thought to act as double Michael acceptors, forming two covalent bonds to…”
Get full text
Journal Article -
12
Design, Synthesis and Biological Evaluation of Novel Inhibitors of Trypanosoma brucei Pteridine Reductase 1
Published in ChemMedChem (07-02-2011)“…Genetic studies indicate that the enzyme pteridine reductase 1 (PTR1) is essential for the survival of the protozoan parasite Trypanosoma brucei. Herein, we…”
Get full text
Journal Article -
13
Cover Picture: Development of Small-Molecule Trypanosoma brucei N-Myristoyltransferase Inhibitors: Discovery and Optimisation of a Novel Binding Mode (ChemMedChem 11/2015)
Published in ChemMedChem (01-11-2015)“…The front cover picture shows the enzyme N‐myristoyltransferase from the pathogen Trypanosoma brucei. Next to this is an image of the parasite. Also shown are…”
Get full text
Journal Article -
14
Optimisation of the Anti-Trypanosoma brucei Activity of the Opioid Agonist U50488
Published in ChemMedChem (04-10-2011)“…Screening of the Sigma–Aldrich Library of Pharmacologically Active Compounds (LOPAC) against cultured Trypanosoma brucei, the causative agent of African…”
Get full text
Journal Article -
15
Cover Picture: Synthesis and Evaluation of Indatraline-Based Inhibitors for Trypanothione Reductase / Design, Synthesis and Biological Evaluation of Novel Inhibitors of Trypanosoma brucei Pteridine Reductase 1 / Modified 5′-Trityl Nucleosides as Inhibitors of Plasmodium falciparum dUTPase (ChemMedChem 2/2011)
Published in ChemMedChem (07-02-2011)Get full text
Journal Article