Structure activity relationships of αv integrin antagonists for pulmonary fibrosis by variation in aryl substituents
Antagonism of alphav beta6 is emerging as a potential treatment of idiopathic pulmonary fibrosis based on strong target validation. Starting from an alphav beta3 antagonist lead and through simple variation in the nature and position of aryl substituent, the discovery of compounds with improved alp...
| Main Authors: | Adams, James, Anderson, Edward C., Blackham, Emma E., Chiu, Yin Wa Ryan, Clarke, Thomas, Eccles, Natasha, Gill, Luke A., Haye, Joshua J., Haywood, Harvey T., Hoenig, Christian R., Russell, Hannah L., Smedley, Christopher, Tipping, William J., Tongue, Tom, Wood, Charlotte C., Yeung, Jason, Rowedder, James E., Fray, Michael J., Mcinally, Thomas, Macdonald, Simon J.F. |
|---|---|
| Format: | Article |
| Published: |
American Chemical Society
2014
|
| Subjects: | |
| Online Access: | https://eprints.nottingham.ac.uk/29558/ |
Similar Items
Impact of the calcium form of β-hydroxy-β-methylbutyrate upon human skeletal muscle protein metabolism
by: Wilkinson, Daniel J., et al.
Published: (2017)
by: Wilkinson, Daniel J., et al.
Published: (2017)
The molecular basis of Gs protein efficacy at the b2- adrenoceptor
by: Harwood, Clare
Published: (2022)
by: Harwood, Clare
Published: (2022)
Defining the mechanism of galectin-3-mediated TGF-β1 activation and its role in lung fibrosis
by: Calver, J.F.
Published: (2023)
by: Calver, J.F.
Published: (2023)
Effect of encapsulation of D-limonene on the moisture adsorption property of ß-cyclodextrin
by: Fang, Zhongxiang, et al.
Published: (2013)
by: Fang, Zhongxiang, et al.
Published: (2013)
Investigations into β2-adrenoceptor pharmacology: kinetic analysis, mechanotransduction and allosteric modulation
by: Cullum, Sean A.
Published: (2024)
by: Cullum, Sean A.
Published: (2024)
Novel selective β1-adrenoceptor antagonists for concomitant cardiovascular and respiratory disease
by: Baker, Jillian G., et al.
Published: (2017)
by: Baker, Jillian G., et al.
Published: (2017)
Adsorption kinetics and thermodynamics of water-insoluble crosslinked β-cyclodextrin polymer for phenol in aqueous solution
by: Huang, Hui, et al.
Published: (2013)
by: Huang, Hui, et al.
Published: (2013)
Predictors of severe exacerbations, poor asthma control, and β-agonist overuse for patients with asthma
by: Patel, Mitesh, et al.
Published: (2014)
by: Patel, Mitesh, et al.
Published: (2014)
Active search for computer-aided drug design
by: Oglic, Dino, et al.
Published: (2018)
by: Oglic, Dino, et al.
Published: (2018)
Generation of human monoclonal antibodies: the development of methods to identify and isolate neutralising antibodies targeted to Ebolavirus from peripheral blood
by: Bailey, Graham D.
Published: (2017)
by: Bailey, Graham D.
Published: (2017)
Mechanisms of resistance to β-lactam antibiotics in Bacteroides species
by: Edwards, Richard
Published: (1995)
by: Edwards, Richard
Published: (1995)
Fabrication, characterization and evaluation of β-elemene nanoparticles for anti-cancer treatment
by: Zhao, Xi
Published: (2020)
by: Zhao, Xi
Published: (2020)
Impact of stirring speed on B-lactoglobulin fibril formation
by: Ng, Shy Kai, et al.
Published: (2016)
by: Ng, Shy Kai, et al.
Published: (2016)
Mathematical Models of Pro-remodelling Growth Factor Activation in Asthmatic Airways
by: Pybus, Hannah J.
Published: (2020)
by: Pybus, Hannah J.
Published: (2020)
Antioxidant properties of novel dimers derived from natural β‑elemene through inhibiting H2O2‑induced apoptosis
by: Chen, Jichao, et al.
Published: (2017)
by: Chen, Jichao, et al.
Published: (2017)
Novel hybrids of natural β-elemene bearing isopropanolamine
moieties: synthesis, enhanced anticancer profile, and improved aqueous solubility
by: Chen, Jichao, et al.
Published: (2017)
by: Chen, Jichao, et al.
Published: (2017)
Engineering novel S-glycosidase activity into extremo-adapted β-glucosidase by rational design
by: Almulhim, Nourah
Published: (2021)
by: Almulhim, Nourah
Published: (2021)
Molecular mechanisms controlling μ-opioid receptor activation
by: Batista Gondin, Arisbel
Published: (2019)
by: Batista Gondin, Arisbel
Published: (2019)
Suberanilohydroxamic acid prevents TGF-β1-induced COX-2 repression in human lung fibroblasts post-transcriptionally by TIA-1 downregulation
by: Pasini, Alice, et al.
Published: (2018)
by: Pasini, Alice, et al.
Published: (2018)
Similarity- and substructure-based development of β2-adrenergic receptor ligands based on unusual scaffolds
by: Schmidt, Denis, et al.
Published: (2017)
by: Schmidt, Denis, et al.
Published: (2017)
Targeted suppression of AR-V7 using PIP5K1α inhibitor overcomes enzalutamide resistance in prostate cancer cells
by: Sarwar, Martuza, et al.
Published: (2016)
by: Sarwar, Martuza, et al.
Published: (2016)
Modelling and experimental study on β-phase depletion behaviour of HVOF sprayed free-standing CoNiCrA1Y coatings during oxidation
by: Chen, H., et al.
Published: (2016)
by: Chen, H., et al.
Published: (2016)
Some aspects on modelling of the β-phase depletion behaviour under different oxide growth kinetics in HVOF CoNiCrAlY coatings
by: Chen, H., et al.
Published: (2017)
by: Chen, H., et al.
Published: (2017)
Identification, characterisation and functional analyses of novel beta-catenin associated protein, FLYWCH1
by: Muhammad, Belal Abdul-Rahman
Published: (2013)
by: Muhammad, Belal Abdul-Rahman
Published: (2013)
Determination of the ligand pharmacophore required for secondary conformation activation of the human β1-adrenoceptor
by: Pinto de Sousa, Emanuel
Published: (2020)
by: Pinto de Sousa, Emanuel
Published: (2020)
FLYWCH1, a novel transcription regulator with potential tumour suppressor activity
by: Almozyan, Sheema
Published: (2021)
by: Almozyan, Sheema
Published: (2021)
In vivo pharmacological evaluation of a novel dual-target inhibitor and methylprednisolone as Alzheimer’s disease treatments
by: Zhang, Bocheng
Published: (2023)
by: Zhang, Bocheng
Published: (2023)
Differential effects of short-term β agonist and growth hormone treatments on expression of myosin heavy chain IIB and associated metabolic genes in sheep muscle
by: Hemmings, K.M., et al.
Published: (2014)
by: Hemmings, K.M., et al.
Published: (2014)
Predicting in vivo cardiovascular properties of β-blockers from cellular assays: a quantative comparison of cellular and cardiovascular pharmacological responses
by: Baker, Jillian G., et al.
Published: (2011)
by: Baker, Jillian G., et al.
Published: (2011)
Genetically-controlled Vesicle-Associated Membrane Protein 1 expression may contribute to Alzheimer’s pathophysiology and susceptibility
by: Sevlever, Daniel, et al.
Published: (2015)
by: Sevlever, Daniel, et al.
Published: (2015)
Tumour compartment transcriptomics demonstrates the activation of inflammatory and odontogenic programmes in human adamantinomatous craniopharyngioma and identifies the MAPK/ERK pathway as a novel therapeutic target
by: Apps, John R., et al.
Published: (2018)
by: Apps, John R., et al.
Published: (2018)
Discovery of novel antitumor nitric oxide-donating b-elemene hybrids through inhibiting the PI3K/Akt pathway
by: Chen, Jichao, et al.
Published: (2017)
by: Chen, Jichao, et al.
Published: (2017)
An analytical approach to the β-phase coarsening behaviour in a thermally sprayed CoNiCrAlY bond coat alloy
by: Chen, H., et al.
Published: (2017)
by: Chen, H., et al.
Published: (2017)
Fabrication of β-cyclodextrin modified mesostructured silica coated multi-walled carbon nanotubes composites and application for paraben removal
by: Ding, Chuyuan, et al.
Published: (2018)
by: Ding, Chuyuan, et al.
Published: (2018)
Characterisation of the native β-alanine pathway in Cupriavidus necator H16: an attractive route towards 3-hydroxypropionic acid production.
by: Orol Gómez, Diego
Published: (2020)
by: Orol Gómez, Diego
Published: (2020)
Suppression of PKC-α attenuates TNF-α-evoked cerebral barrier breakdown via regulations of MMP-2 and plasminogen–plasmin system
by: Abdullah, Zuraidah, et al.
Published: (2016)
by: Abdullah, Zuraidah, et al.
Published: (2016)
A study of α-Adrenoceptor agonists on porcine nasal and extra-nasal vasculature: insight into decongestant activity
by: Abdulrahman, Aseel
Published: (2019)
by: Abdulrahman, Aseel
Published: (2019)
Advances in the application of N-sulfinyl auxiliaries to the synthesis of pyrrolidines and α-amino acid derivatives
by: O'Connor, Daniel
Published: (2020)
by: O'Connor, Daniel
Published: (2020)
Preparation of potent and selective αvβ6 integrin inhibitors for the treatment of idiopathic pulmonary fibrosis and synthetic approaches towards the total synthesis of mescengricin
by: Robinson, Henry Duncan
Published: (2021)
by: Robinson, Henry Duncan
Published: (2021)
Thecal cell sensitivity to luteinizing hormone and insulin in polycystic ovarian syndrome
by: Cadagan, David, et al.
Published: (2016)
by: Cadagan, David, et al.
Published: (2016)
Similar Items
-
Impact of the calcium form of β-hydroxy-β-methylbutyrate upon human skeletal muscle protein metabolism
by: Wilkinson, Daniel J., et al.
Published: (2017) -
The molecular basis of Gs protein efficacy at the b2- adrenoceptor
by: Harwood, Clare
Published: (2022) -
Defining the mechanism of galectin-3-mediated TGF-β1 activation and its role in lung fibrosis
by: Calver, J.F.
Published: (2023) -
Effect of encapsulation of D-limonene on the moisture adsorption property of ß-cyclodextrin
by: Fang, Zhongxiang, et al.
Published: (2013) -
Investigations into β2-adrenoceptor pharmacology: kinetic analysis, mechanotransduction and allosteric modulation
by: Cullum, Sean A.
Published: (2024)