D. Holmes

发表

4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy.

P. Bamborough, W. Rumsey, C. Chung, 2012, Bioorganic & medicinal chemistry letters.

In search of a small molecule agonist of the relaxin receptor RXFP1 for the treatment of liver fibrosis

J. Fallowfield, J. Iredale, D. Mossakowska, 2017, Scientific Reports.

Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.

I. McLay, Helen T Horsley, D. Coe, 2010, Journal of medicinal chemistry.

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

A. Hovnanian, J. Liddle, Kathrine J. Smith, 2019, Acta crystallographica. Section F, Structural biology communications.

Structural and mechanistic basis of differentiated inhibitors of the acute pancreatitis target kynurenine-3-monooxygenase

C. Chung, D. Mole, J. Liddle, 2017, Nature Communications.

Targeting the regulatory site of ER aminopeptidase 1 leads to the discovery of a natural product modulator of antigen presentation.

Jonathan M. Lea, J. Liddle, P. Rowland, 2020, Journal of medicinal chemistry.

4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors.

P. Bamborough, J. Liddle, M. Morse, 2009, Bioorganic & medicinal chemistry letters.

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

J. Irving, Zhengrong Zhu, D. Lomas, 2021, Bioorganic & medicinal chemistry letters.

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

A. Hovnanian, J. Liddle, Kathrine J. Smith, 2019, Bioorganic & medicinal chemistry letters.

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

A. Hovnanian, J. Liddle, Kathrine J. Smith, 2019, Bioorganic & medicinal chemistry letters.

The discovery of quinoline based single-ligand human H1 and H3 receptor antagonists.

S. Hodgson, D. Holmes, P. Procopiou, 2016, Bioorganic & medicinal chemistry letters.

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

D. Holmes, L. Liefaard, M. Bamford, 2019, British journal of pharmacology.

Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.

S. Dowell, E. Demont, J. Witherington, 2016, Journal of medicinal chemistry.

The discovery of potent and selective kynurenine 3-monooxygenase inhibitors for the treatment of acute pancreatitis.

M. Hann, D. Mole, J. Liddle, 2017, Bioorganic & medicinal chemistry letters.

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

A. Hovnanian, J. Liddle, P. Thomas, 2019, Bioorganic & medicinal chemistry letters.

Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.

S. Dowell, K. Philpott, T. Heightman, 2011, Journal of medicinal chemistry.

Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H1 receptor antagonists for use in allergic rhinitis.

K. Clark, S. Hodgson, D. Holmes, 2017, Bioorganic & medicinal chemistry letters.

Design of Phthalazinone Amide Histamine H1 Receptor Antagonists for Use in Rhinitis.

K. Clark, S. Hodgson, D. Holmes, 2017, ACS medicinal chemistry letters.

A potent and selective Kallikrein-5 inhibitor delivers high pharmacological activity in Netherton Syndrome patient skin.

M. Lennon, A. Hovnanian, D. Grillot, 2021, The Journal of investigative dermatology.

Kynurenine–3–monooxygenase inhibition prevents multiple organ failure in rodent models of acute pancreatitis

J. Iredale, S. Howie, J. Hughes, 2015, Nature Medicine.

Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity.

Paul Bamborough, Penny A. Smee, P. Bamborough, 2008, Bioorganic & medicinal chemistry letters.

The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.

Kenneth L. Clark, Duncan S. Holmes, Michael Kranz, 2011, Journal of medicinal chemistry.

Synthesis and structure-activity relationships of a series of penicillin-derived HIV proteinase inhibitors containing a stereochemically unique peptide isostere.

J. Kitchin, R. Bethell, N. Cammack, 1993, Journal of medicinal chemistry.

Synthesis and biological activity of conformationally constrained sialyl Lewis X analogues with reduced carbohydrate character

D. Holmes, M. Bamford, R. Priest, 1996 .

Synthesis of a novel analogue of sialyl Lewis X

D. Holmes, M. Bamford, P. Ward, 1995 .

Chemoselective Glycosylations. 2. Differences in Size of Anomeric Leaving Groups Can Be Exploited in Chemoselective Glycosylations.

G. Boons, D. Holmes, R. Geurtsen, 1997, The Journal of organic chemistry.

Novel dimeric penicillin derived inhibitors of HIV-1 proteinase: interaction with the catalytic aspartates

J. Kitchin, R. Storer, D. Holmes, 1993 .

An Improved Method for the Synthesis of Gdp-Hexanolamine Derivatives, key Reagents for the Purification and Characterisation of Carbohydrate Processing Enzymes

D. Holmes, M. Bamford, E. Draeger, 1996 .

Synthesis of Putative Intermediates on the Monensin Biosynthetic Pathway and Incorporation Experiments with the Monensin-Producing Organism

John A. Robinson, S. T. Russell, D. Holmes, 1990 .

Total Synthesis of A Putative Triene Intermediate in Monensin Biosynthesis, Activated as a Caprylcysteamine Thiol Ester.

John A. Robinson, S. T. Russell, D. Holmes, 1988 .

HOMEOMORPHIC ISOMERISM IN A PEPTIDIC MACROBICYCLE

N. Rees, D. Turner, D. Holmes, 1996 .

Selection of a specifically blocked mutant of Streptomyces cinnamonensis: isolation and synthesis of 26-deoxymonensin A.

D. Cane, J. Robinson, D. Holmes, 1989, The Journal of antibiotics.

An Electron Spin Resonance Study of Gamma-Irradiated 5,6-Dihydropyrimidines

D. Holmes, L. Piette, 1968 .

The Bioconversion of (3RS,E)‐ and (3RS,Z)‐Nerolidol into Oxygenated Products by Streptomyces cinnamonensis. Possible Implications for the Biosynthesis of the Polyether Antibiotic Monensin A??

John A. Robinson, D. Holmes, D. Ashworth, 1990 .

4-acyl-1-(4-aminoalkoxyphenyl)-2-ketopiperazines as a novel class of non-brain-penetrant histamine H3 receptor antagonists.

Christopher Browning, Helen Connor, David M. Wilson, 2007, Journal of medicinal chemistry.

Chemoselective glycosylations (part 1): Differences in size of anomeric leaving groups can be exploited in chemoselective glycosylations

G. Boons, D. Holmes, R. Geurtsen, 1995 .

Chemoselective Glycosylations. Part 1. Differences in Size of Anomeric Leaving Groups can be Exploited in Chemoselective Glycosylations.

G. Boons, D. Holmes, R. Geurtsen, 1995 .

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

P. Thomas, Jonathan D Goodacre, Lena Shukla, 2020, Bioorganic & medicinal chemistry letters.

p38alpha mitogen-activated protein kinase inhibitors: optimization of a series of biphenylamides to give a molecule suitable for clinical progression.

J. B. Buckton, Penny A. Smee, P. Bamborough, 2009, Journal of medicinal chemistry.

Discovery of a rapidly metabolized, long-acting β(2) adrenergic receptor agonist with a short onset time incorporating a sulfone group suitable for once-daily dosing.

K. Biggadike, D. Holmes, P. Procopiou, 2014, Journal of medicinal chemistry.

Development of a Series of Kynurenine 3-Monooxygenase Inhibitors Leading to a Clinical Candidate for the Treatment of Acute Pancreatitis.

Xiaozhong Zheng, D. Mole, D. Clapham, 2017, Journal of medicinal chemistry.

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

J. Schofield, M. Convery, Xiping Zhang, 2021, The Journal of biological chemistry.

Discovery of a Selective S1P1 Receptor Agonist Efficacious at Low Oral Dose and Devoid of Effects on Heart Rate.

S. Dowell, E. Demont, J. Witherington, 2011, ACS medicinal chemistry letters.

Mimics of the sialyl Lewis X tetrasaccharide. Replacement of the N-acetylglucosamine sugar with simple C2-symmetric 1,2-diols.

D. Holmes, M. Bamford, R. Priest, 1996, Bioorganic & medicinal chemistry.

Generation and Characterization of Monoclonal Antibodies to Human Type-5 Tartrate-Resistant Acid Phosphatase : Development of a Specific Immunoassay of the lsoenzyme in Serum

Stephen, Juliet, Timothy, 2004 .

Quinolines as a novel structural class of potent and selective PDE4 inhibitors. Optimisation for inhaled administration.

Tony W Dean, Michael D. Woodrow, D. Somers, 2009, Bioorganic & medicinal chemistry letters.

Synthesis and structure-activity relationships of a series of penicillin-derived HIV proteinase inhibitors: heterocyclic ring systems containing P1' and P2' substituents.

J. Kitchin, R. Bethell, N. Cammack, 1994, Journal of medicinal chemistry.

Development of a small molecule that corrects misfolding and increases secretion of Z α1-antitrypsin

J. Irving, Zhengrong Zhu, D. Lomas, 2020, bioRxiv.

Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity.

P. Bamborough, R. Angell, A. Walker, 2008, Bioorganic & medicinal chemistry letters.

In search of a small molecule agonist of the relaxin receptor RXFP1 for the treatment of liver fibrosis

J. Fallowfield, J. Iredale, D. Mossakowska, 2017, Scientific Reports.