Alex Phillipou
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Explore the profile of Alex Phillipou including associated specialties, affiliations and a list of published articles.
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10
Citations
63
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Recent Articles
1.
Hryczanek R, Hackett A, Rowland P, Chung C, Convery M, Holmes D, et al.
ACS Med Chem Lett
. 2024 Dec;
15(12):2107-2114.
PMID: 39691536
Endoplasmic reticulum aminopeptidase 1 (ERAP1) cleaves the -terminal amino acids of peptides, which can then bind onto major histocompatibility class I (MHC-I) molecules for presentation onto the cell surface, driving...
2.
Bradley E, Fusani L, Chung C, Craggs P, Demont E, Humphreys P, et al.
J Med Chem
. 2023 Nov;
66(23):15728-15749.
PMID: 37967462
Small-molecule-mediated disruption of the protein-protein interactions between acetylated histone tails and the tandem bromodomains of the bromodomain and extra-terminal (BET) family of proteins is an important mechanism of action for...
3.
Bamborough P, Chung C, Goodwin N, Mitchell D, Neipp C, Phillipou A, et al.
ACS Med Chem Lett
. 2023 Sep;
14(9):1231-1236.
PMID: 37736196
The 1,3-dihydro-2-benzo[]azepin-2-ones are potent and ligand-efficient pan-BET bromodomain inhibitors. Here we describe the extension of this template to exploit a bivalent mode of action, binding simultaneously to both bromodomains. Initially...
4.
Fallon D, Phillipou A, Schofield C, House D, Tomkinson N, Bush J
Biochem J
. 2023 Jul;
480(15):1183-1197.
PMID: 37401534
The development and optimisation of a photoaffinity labelling (PAL) displacement assay is presented, where a highly efficient PAL probe was used to report on the relative binding affinities of compounds...
5.
Clegg M, Theodoulou N, Bamborough P, Chung C, Craggs P, Demont E, et al.
ACS Med Chem Lett
. 2021 Aug;
12(8):1308-1317.
PMID: 34413961
Bromodomain containing proteins and the acetyl-lysine binding bromodomains contained therein are increasingly attractive targets for the development of novel epigenetic therapeutics. To help validate this target class and unravel the...
6.
Fallon D, Lehmann S, Chung C, Phillipou A, Eberl C, Fantom K, et al.
Chemistry
. 2021 Jul;
27(71):17880-17888.
PMID: 34328642
We present a one-step Ugi reaction protocol for the expedient synthesis of photoaffinity probes for live-cell MS-based proteomics. The reaction couples an amine affinity function with commonly used photoreactive groups,...
7.
Seal J, Atkinson S, Bamborough P, Bassil A, Chung C, Foley J, et al.
J Med Chem
. 2021 Jul;
64(15):10772-10805.
PMID: 34255512
The profound efficacy of pan-BET inhibitors is well documented, but these epigenetic agents have shown pharmacology-driven toxicity in oncology clinical trials. The opportunity to identify inhibitors with an improved safety...
8.
Rianjongdee F, Atkinson S, Chung C, Grandi P, Gray J, Kaushansky L, et al.
J Med Chem
. 2021 Jul;
64(15):10806-10833.
PMID: 34251219
Second-generation bromodomain and extra terminal (BET) inhibitors, which selectively target one of the two bromodomains in the BET proteins, have begun to emerge in the literature. These inhibitors aim to...
9.
Watson R, Bamborough P, Barnett H, Chung C, Davis R, Gordon L, et al.
J Med Chem
. 2020 Jul;
63(17):9045-9069.
PMID: 32691589
Pan-bromodomain and extra terminal (BET) inhibitors interact equipotently with all eight bromodomains of the BET family of proteins. They have shown profound efficacy in vitro and in vivo in oncology...
10.
Liddle J, Hutchinson J, Kitchen S, Rowland P, Neu M, Cecconie T, et al.
J Med Chem
. 2020 Feb;
63(6):3348-3358.
PMID: 32109056
ER aminopeptidase 1 (ERAP1) is an intracellular enzyme that generates antigenic peptides and is an emerging target for cancer immunotherapy and the control of autoimmunity. ERAP1 inhibitors described previously target...