Výsledky vyhledávání - "David W. Foley"

Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity

Autor: Ross Collins, Hyunah Lee, D. Heulyn Jones, Jonathan M. Elkins, Jason A. Gillespie, Carys Thomas, Alex G. Baldwin, Kimberley Jones, Loren Waters, Marie Paine, John R. Atack, Simon E. Ward, Olivera Grubisha, David W. Foley

Publikováno v: Journal of Medicinal Chemistry. 65:13705-13713

LIM domain kinases 1 and 2 (LIMK1 and LIMK2) regulate actin dynamics and subsequently key cellular functions such as proliferation and migration. LIMK1 and LIMK2 phosphorylate and inactivate cofilin leading to increased actin polymerization. As a res

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ec61e46daab0767af551fe05809ccb38
https://doi.org/10.1021/acs.jmedchem.2c00751

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Administration in fed state but not controlled release in the colon increases oral bioavailability of DF030263, a promising drug candidate for chronic lymphocytic leukemia

Autor: Atheer Zgair, Leonid Kagan, Jong Bong Lee, Hwi-yeol Yun, Peter Fischer, Min Gi Kim, Tae Hwan Kim, Pavel Gershkovich, Xiaowei Zang, Rui Gao, Ting Qian Ooi, David W. Foley, Hao Shao, Wan Tying Soh, Anthony J. Wilson, Gregory Voronin, Fadi Soukarieh

Publikováno v: European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V. 165

For treatment of chronic cancers, the oral administration route is preferred as it provides numerous advantages over other delivery routes. However, these benefits of oral chemotherapy can be limited due to unfavorable pharmacokinetics. Accordingly,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3d06c6df5d069734a67bb06f9f93664c
https://pubmed.ncbi.nlm.nih.gov/33991611

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Structure-based design of highly selective 2,4,5-trisubstituted pyrimidine CDK9 inhibitors as anti-cancer agents

Autor: Chris Pepper, Frankie Lam, Hao Shao, David W. Foley, Peter Fischer, Tracey D. Bradshaw, Abdullahi Y. Abbas, Shiliang Huang, Shudong Wang, Pavel Gershkovich

Cyclin-dependent kinases (CDKs) are a family of Ser/Thr kinases involved in cell cycle and transcriptional regulation. CDK9 regulates transcriptional elongation and this unique property has made it a potential target for several diseases. Due to the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3fa0033351dd727bdb5075ba87dd64aa

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True or false? challenges and recent highlights in the development of aspirin prodrugs

Autor: David W. Foley, Steffan Willetts

Aspirin is a widely used medicine for a variety of indications. It is unique amongst non-steroidal anti-inflammatory drugs (NSAIDs) in that it causes irreversible acetylation of COX enzymes. Like all NSAIDs however, aspirin causes severe gastrointest

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9fc1a7a489762bda8c74e87afb518b45

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A cyclosporine derivative is a substrate of the oligopeptide transporter PepT1

Autor: David Meredith, Isabel Bermudez, David W. Foley, Patrick D. Bailey

Publikováno v: MedChemComm. 7:999-1002

The mammalian proton-coupled oligopeptide transporter PepT1 is recognised as an important route of oral drug delivery. Peptide-based compounds offer great potential as drugs but their application is limited by poor membrane permeability, amongst othe

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5d68a392ce4caa577bf33bebc1c37f76
https://doi.org/10.1039/c5md00575b

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Communicating Our Science to Our Customers: Drug Discovery in Five Simple Experiments

Autor: Lesley-Anne Pearson, David W. Foley

Publikováno v: ACS Medicinal Chemistry Letters. 8:143-144

The complexities of modern drug discovery-an interdisciplinary process that often takes years and costs billions-can be extremely challenging to explain to a public audience. We present details of a 30 minute demonstrative lecture that uses well-know

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::87b996a9d6e97af6aba2afab7b7d8a16
https://doi.org/10.1021/acsmedchemlett.7b00015

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Bioavailability Through PepT1: The Role of Computer Modelling in Intelligent Drug Design

Autor: David Meredith, Patrick D. Bailey, Jeyaganesh Rajamanickam, David W. Foley

Publikováno v: Current Computer Aided-Drug Design. 6:68-78

In addition to being responsible for the majority of absorption of dietary nitrogen, the mammalian proton-coupled di- and tri-peptide transporter PepT1 is also recognised as a major route of drug delivery for several important classes of compound, in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7a4ae639145729b5924bf4a07e306bd6
https://doi.org/10.2174/157340910790980133

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An energy supply network of nutrient absorption coordinated by calcium and T1R taste receptors in rat small intestine

Autor: Rachel Pettcrew, Myrtani Pieri, David W. Foley, E. J. Shepherd, David Meredith, Pat D. Bailey, Norma Lister, Philip A. Helliwell, George L. Kellett, Richard Boyd, Julie Affleck, Oliver J. Mace, John R. Bronk, Emma L. Morgan

Publikováno v: The Journal of Physiology. 587:195-210

T1R taste receptors are present throughout the gastrointestinal tract. Glucose absorption comprises active absorption via SGLT1 and facilitated absorption via GLUT2 in the apical membrane. Trafficking of apical GLUT2 is rapidly up-regulated by glucos

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5eadd0302f7a981d2afdd5bad46d9c75
https://doi.org/10.1113/jphysiol.2008.159616

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Synthesis, structure-activity relationship and biological evaluation of 2,4,5-trisubstituted pyrimidine CDK inhibitors as potential anti-tumour agents

Autor: Xiangrui Jiang, Peter Fischer, Shiliang Huang, Shenhua Shi, Hao Shao, Frankie Lam, Shudong Wang, Xiangrui Liu, Nadiah Baharin, David W. Foley, Abdullah Y. Abbas

Publikováno v: European journal of medicinal chemistry. 70

A series of 2,4,5-trisubstituted pyrimidines have been synthesised and characterised, which exhibited potent CDK inhibition and anti-proliferative activities. The structure–activity relationship is analysed and a rational for CDK9 selectivity is di

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fdfef124e2e13161fb49c3ba523ec15a
https://pubmed.ncbi.nlm.nih.gov/24185375

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Substituted 4-(thiazol-5-yl)-2-(phenylamino)pyrimidines are highly active CDK9 inhibitors: synthesis, X-ray crystal structures, structure-activity relationship, and anticancer activities

Autor: Jane A. Endicott, Chris Pepper, Alison J. Hole, Abdullahi Y. Abbas, Shenhua Shi, Frankie Lam, Shudong Wang, Martin E.M. Noble, Sonja Baumli, Hao Shao, Xiangrui Liu, David W. Foley, Shiliang Huang, Peter Fischer

Publikováno v: Journal of Medicinal Chemistry

Cancer cells often have a high demand for antiapoptotic proteins in order to resist programmed cell death. CDK9 inhibition selectively targets survival proteins and reinstates apoptosis in cancer cells. We designed a series of 4-thiazol-2- anilinopyr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::10ca38616b46173ee2f7407ba2de20a5
https://pubmed.ncbi.nlm.nih.gov/23301767

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