Paul J Beswick
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Explore the profile of Paul J Beswick including associated specialties, affiliations and a list of published articles.
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15
Citations
112
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Recent Articles
1.
Harman M, Stanway S, Scott H, Demydchuk Y, Bezerra G, Pellegrino S, et al.
J Med Chem
. 2023 Jul;
66(14):9881-9893.
PMID: 37433017
Angiotensin-converting enzyme 2 (ACE2) is a metalloprotease that cleaves angiotensin II, a peptide substrate involved in the regulation of hypertension. Here, we identified a series of constrained bicyclic peptides, ,...
2.
Rigby M, Bennett G, Chen L, Mudd G, Harrison H, Beswick P, et al.
Mol Cancer Ther
. 2022 Sep;
21(12):1747-1756.
PMID: 36112771
Multiple tumor types overexpress Nectin-4 and the antibody-drug conjugate (ADC), enfortumab vedotin (EV) shows striking efficacy in clinical trials for metastatic urothelial cancer, which expresses high levels of Nectin-4, validating...
3.
Young R, Alderton W, Angell A, Beswick P, Brown D, Chambers C, et al.
Bioorg Med Chem Lett
. 2011 Apr;
21(10):3037-40.
PMID: 21482467
Heteroalicyclic carboxamidines were synthesised and evaluated as inhibitors of nitric oxide synthases. (2R)-2-Pyrrolidinecarboxamidine, in particular, was shown to be a highly potent in vitro (IC(50)=0.12 μM) and selective iNOS inhibitor...
4.
Abberley L, Bebius A, Beswick P, Billinton A, Collis K, Dean D, et al.
Bioorg Med Chem Lett
. 2010 Oct;
20(22):6370-4.
PMID: 20934331
A backup molecule to compound 2 was sought by targeting the most likely metabolically vulnerable site in this molecule. Compound 18 was subsequently identified as a potent P2X(7) antagonist with...
5.
Abdi M, Beswick P, Billinton A, Chambers L, Charlton A, Collins S, et al.
Bioorg Med Chem Lett
. 2010 Aug;
20(17):5080-4.
PMID: 20673717
A computational lead-hopping exercise identified compound 4 as a structurally distinct P2X(7) receptor antagonist. Structure-activity relationships (SAR) of a series of pyroglutamic acid amide analogues of 4 were investigated and...
6.
Gleave R, Walter D, Beswick P, Fonfria E, Michel A, Roman S, et al.
Bioorg Med Chem Lett
. 2010 Jul;
20(16):4951-4.
PMID: 20634071
A series of analogues of the pyrazole lead 1 were synthesized in which the heterocyclic core was replaced with an imidazole. A number of potent antagonists were identified and structure-activity...
7.
Beswick P, Billinton A, Chambers L, Dean D, Fonfria E, Gleave R, et al.
Bioorg Med Chem Lett
. 2010 Jun;
20(15):4653-6.
PMID: 20579878
Structure-activity relationships (SAR) of analogues of lead compound 1 were investigated and compound 16 was selected for further study in animal models of pain. Compound 16 was shown to be...
8.
Chambers L, Stevens A, Moses A, Michel A, Walter D, Davies D, et al.
Bioorg Med Chem Lett
. 2010 Apr;
20(10):3161-4.
PMID: 20399651
High-throughput screening identified compound 1 as a potent P2X(7) receptor antagonist suitable for lead optimisation. Structure-activity relationships (SAR) of a series of (1H-pyrazol-4-yl)acetamides were investigated and compound 32 was identified...
9.
Gleave R, Beswick P, Brown A, Giblin G, Goldsmith P, Haslam C, et al.
Bioorg Med Chem Lett
. 2009 Dec;
20(2):465-8.
PMID: 20005703
A series of 3-amino-6-aryl-pyridazines have been identified as CB(2) agonists with high efficacy and selectivity against the CB(1) receptor. Details of the investigation of structure-activity relationships (SAR) are disclosed, which...
10.
Gleave R, Beswick P, Brown A, Giblin G, Haslam C, Livermore D, et al.
Bioorg Med Chem Lett
. 2009 Oct;
19(23):6578-81.
PMID: 19864133
2-Amino-5-aryl-pyridines, exemplified by compound 1, had been identified as a synthetically tractable series of CB(2) agonists from a high-throughput screen of the GlaxoSmithKline compound collection. Described herein are the results...