Discovery of CDZ173 (Leniolisib), representing a structurally novel class of PI3K delta-selective inhibitors

…, AB Smith, GJ Hollingworth, J Blanz… - ACS medicinal …, 2017 - ACS Publications
The predominant expression of phosphoinositide 3-kinase δ (PI3Kδ) in leukocytes and its
critical role in B and T cell functions led to the hypothesis that selective inhibitors of this isoform …

Functional properties of the high-affinity TRPV1 (VR1) vanilloid receptor antagonist (4-hydroxy-5-iodo-3-methoxyphenylacetate ester) iodo-resiniferatoxin

…, GJ Hollingworth, S Teague, J Webb… - … of Pharmacology and …, 2002 - ASPET
We have synthesized iodinated resiniferatoxin bearing a 4-hydroxy-5-iodo-3-methoxyphenylacetate
ester (I-RTX) and have characterized its activity on rat and human TRPV1 (VR1) …

Discovery and pharmacological characterization of novel quinazoline-based PI3K delta-selective inhibitors

…, AB Smith, C Hebach, GJ Hollingworth… - ACS Medicinal …, 2016 - ACS Publications
Inhibition of the lipid kinase PI3Kδ is a promising principle to treat B and T cell driven inflammatory
diseases. Using a scaffold deconstruction–reconstruction strategy, we identified 4-aryl …

Discovery of new binders for DCAF1, an emerging ligase target in the targeted protein degradation field

…, C Pissot-Soldermann, GJ Hollingworth… - ACS Medicinal …, 2023 - ACS Publications
In this study, we describe the rapid identification of potent binders for the WD40 repeat
domain (WDR) of DCAF1. This was achieved by two rounds of iterative focused screening of a …

Divalent Naphthalene Diimide Ligands Display High Selectivity for the Human Telomeric G‐quadruplex in K+ Buffer

STG Street, DN Chin, GJ Hollingworth… - … A European Journal, 2017 - Wiley Online Library
Selective G‐quadruplex ligands offer great promise for the development of anti‐cancer
therapies. A novel series of divalent cationic naphthalene diimide ligands that selectively bind to …

2-Aryl indole NK1 receptor antagonists: Optimisation of indole substitution

…, K Dinnell, JM Elliott, GJ Hollingworth… - Bioorganic & medicinal …, 2001 - Elsevier
The synthesis and biological evaluation of a series of 2-aryl indoles with high affinity for the
human neurokinin-1 (hNK1) receptor are reported, concentrating on optimisation of the …

2-Aryl indole NK1 receptor antagonists: optimisation of the 2-aryl ring and the indole nitrogen substituent

…, MJ Dhar, JM Elliott, GJ Hollingworth… - Bioorganic & medicinal …, 2001 - Elsevier
… Author links open overlay panel Kevin Dinnell a , Gary G Chicchi d , Madhumeeta J Dhar
c , Jason M Elliott a , Gregory J Hollingworth a , Marc M Kurtz d , Mark P Ridgill a , Wayne …

Transient targeting of phosphoinositide 3-kinase acts as a roadblock in mast cells' route to allergy

…, C Burkhart, E Hirsch, GJ Hollingworth… - Journal of allergy and …, 2013 - Elsevier
Background Tissue mast cell numbers are dynamically regulated by recruitment of
progenitors from the vasculature. It is unclear whether progenitors are recruited during allergic …

Preparation and palladium-catalysed cross-coupling reactions of 3-and 4-tributylstannylfuran-2 (5H)-ones

GJ Hollingworth, G Perkins, J Sweeney - Journal of the Chemical …, 1996 - pubs.rsc.org
Hollingworth, Gemma Perkins and Joseph Sweeney *,t … J 16 15 … Coupling constants (J)
are quoted in Hz. Reactions involving chemicals or intermediates sensitive to air and/or …

[HTML][HTML] Structure-activity relationship studies on divalent naphthalene diimide G quadruplex ligands with anticancer and antiparasitic activity

…, J Ramos-Soriano, YJ Jiang, GJ Hollingworth… - Bioorganic & Medicinal …, 2022 - Elsevier
Naphthalene diimide (NDI) is a central scaffold that has been commonly used in the design
of G-quadruplex (G4) ligands. Previous work revealed notable anticancer activity of a …