Duncan S. Holmes

GlaxoSmithKline R&D
Stevenage, ENG, United Kingdom

Last Updated: 09/26/2026

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Found 23 publications

Optimization of Potent and Selective Cyclohexyl Acid ERAP1 Inhibitors Using Structure- and Property-Based Drug Design.

Optimization of Potent and Selective Cyclohexyl Acid ERAP1 Inhibitors Using Structure- and Property-Based Drug Design.

Journal: ACS medicinal chemistry letters

Published: August 08, 2024

GSK137, a potent small-molecule BCL6 inhibitor with in vivo activity, suppresses antibody responses in mice.

GSK137, a potent small-molecule BCL6 inhibitor with in vivo activity, suppresses antibody responses in mice.

Journal: The Journal of biological chemistry

Published: January 12, 2021

The development of highly potent and selective small molecule correctors of Z α1-antitrypsin misfolding.

The development of highly potent and selective small molecule correctors of Z α1-antitrypsin misfolding.

Journal: Bioorganic & medicinal chemistry letters

Published: December 02, 2020

A Potent and Selective Kallikrein-5 Inhibitor Delivers High Pharmacological Activity in Skin from Patients with Netherton Syndrome.

A Potent and Selective Kallikrein-5 Inhibitor Delivers High Pharmacological Activity in Skin from Patients with Netherton Syndrome.

Journal: The Journal of investigative dermatology

Published: October 14, 2020

Structure-based optimisation of orally active & reversible MetAP-2 inhibitors maintaining a tight 'molecular budget'.

Structure-based optimisation of orally active & reversible MetAP-2 inhibitors maintaining a tight 'molecular budget'.

Journal: Bioorganic & medicinal chemistry letters

Published: May 28, 2020

Targeting the Regulatory Site of ER Aminopeptidase 1 Leads to the Discovery of a Natural Product Modulator of Antigen Presentation.

Targeting the Regulatory Site of ER Aminopeptidase 1 Leads to the Discovery of a Natural Product Modulator of Antigen Presentation.

Journal: Journal of medicinal chemistry

Published: February 29, 2020

Corrigendum to 'Design and development of a series of borocycles as selective, covalent kallikrein 5 inhibitors' [Bioorg. Med. Chem. Lett. 29 (2019) 126675].

Corrigendum to 'Design and development of a series of borocycles as selective, covalent kallikrein 5 inhibitors' [Bioorg. Med. Chem. Lett. 29 (2019) 126675].

Journal: Bioorganic & medicinal chemistry letters

Published: December 21, 2019

Design and development of a series of borocycles as selective, covalent kallikrein 5 inhibitors.

Design and development of a series of borocycles as selective, covalent kallikrein 5 inhibitors.

Journal: Bioorganic & medicinal chemistry letters

Published: July 23, 2019

Identification, preclinical profile, and clinical proof of concept of an orally bioavailable pro-drug of miridesap.

Identification, preclinical profile, and clinical proof of concept of an orally bioavailable pro-drug of miridesap.

Journal: British journal of pharmacology

Published: July 09, 2019

Structure guided drug design to develop kallikrein 5 inhibitors to treat Netherton syndrome.

Structure guided drug design to develop kallikrein 5 inhibitors to treat Netherton syndrome.

Journal: Bioorganic & medicinal chemistry letters

Published: February 18, 2019

Evaluation of a crystallographic surrogate for kallikrein 5 in the discovery of novel inhibitors for Netherton syndrome.

Evaluation of a crystallographic surrogate for kallikrein 5 in the discovery of novel inhibitors for Netherton syndrome.

Journal: Acta crystallographica. Section F, Structural biology communications

Published: January 14, 2019

Kallikrein 5 inhibitors identified through structure based drug design in search for a treatment for Netherton Syndrome.

Kallikrein 5 inhibitors identified through structure based drug design in search for a treatment for Netherton Syndrome.

Journal: Bioorganic & medicinal chemistry letters

Published: December 11, 2018

Showing 1-12 of 23

Last Updated: 09/26/2026