Adrian J Highton
Overview
Explore the profile of Adrian J Highton including associated specialties, affiliations and a list of published articles.
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Articles
5
Citations
44
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0
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Recent Articles
1.
McNae I, Kinkead J, Malik D, Yen L, Walker M, Swain C, et al.
Nat Commun
. 2021 Feb;
12(1):1052.
PMID: 33594070
The parasitic protist Trypanosoma brucei is the causative agent of Human African Trypanosomiasis, also known as sleeping sickness. The parasite enters the blood via the bite of the tsetse fly...
2.
Mackman R, Steadman V, Dean D, Jansa P, Poullennec K, Appleby T, et al.
J Med Chem
. 2018 Aug;
61(21):9473-9499.
PMID: 30074795
Cyclophilins are a family of peptidyl-prolyl isomerases that are implicated in a wide range of diseases including hepatitis C. Our aim was to discover through total synthesis an orally bioavailable,...
3.
Crawford J, Kenny P, Bowyer J, Cook C, Finlayson J, Heyes C, et al.
J Med Chem
. 2012 Sep;
55(20):8827-37.
PMID: 22984809
Rational structure-based design has yielded highly potent inhibitors of cathepsin K (Cat K) with excellent physical properties, selectivity profiles, and pharmacokinetics. Compounds with a 3,4-(CH₃O)₂Ph motif, such as 31, were...
4.
Dossetter A, Bowyer J, Cook C, Crawford J, Finlayson J, Heron N, et al.
Bioorg Med Chem Lett
. 2012 Aug;
22(17):5563-8.
PMID: 22858142
The discovery of nitrile compound 4, a potent inhibitor of Cathepsin K (Cat K) with good bioavailability in dog is described. The compound was used to demonstrate target engagement and...
5.
Dossetter A, Beeley H, Bowyer J, Cook C, Crawford J, Finlayson J, et al.
J Med Chem
. 2012 Jun;
55(14):6363-74.
PMID: 22742641
Directed screening of nitrile compounds revealed 3 as a highly potent cathepsin K inhibitor but with cathepsin S activity and very poor stability to microsomes. Synthesis of compounds with reduced...