Zobrazeno 1 - 10 of 10 pro vyhledávání: '"Ben Acton"'
1
Fluoromethylcyclopropylamine derivatives as potential in vivo toxicophores - A cautionary disclosure
Autor: Ben, Acton, Helen F, Small, Kate M, Smith, Alison, McGonagle, Alexandra I J, Stowell, Dominic I, James, Niall M, Hamilton, Nicola, Hamilton, James R, Hitchin, Colin P, Hutton, Ian D, Waddell, Donald J, Ogilvie, Allan M, Jordan
Publikováno v: Bioorganic & Medicinal Chemistry Letters
Graphical abstract
Fluorination of metabolic hotspots in a molecule is a common medicinal chemistry strategy to improve in vivo half-life and exposure and, generally, this strategy offers significant benefits. Here, we report the application of
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::7b50f36beef114bfc9c4974d31ff98d0
https://pubmed.ncbi.nlm.nih.gov/30616904
Zobrazit plný text záznamu
2
Cell-active Small Molecule Inhibitors of the DNA-damage Repair Enzyme Poly(ADP-ribose) Glycohydrolase (PARG): Discovery and Optimization of Orally Bioavailable Quinazolinedione Sulfonamides
Autor: Julie A. Tucker, Ben Acton, Ian D. Waddell, Alexandra Stowell, Nicola Hamilton, Niall M. Hamilton, Kate M. Smith, Stuart Donald Jones, James R. Hitchin, Bohdan Waszkowycz, Alison E. McGonagle, Dominic I. James, Allan M. Jordan, Daniel P. Mould, Clifford David Jones, Colin Hutton, Helen F. Small, Emma E. Fairweather, Donald J. Ogilvie, Louise A. Griffiths
Publikováno v: Waszkowycz, B, Smith, K, Mcgonagle, A, Jordan, A, Acton, B, Fairweather, E, Griffiths, L, Hamilton, N M, Hamilton, N, Hitchin, J R, Hutton, C, James, D I, Jones, C D, Jones, S, Mould, D, Small, H F, Stowell, A, Tucker, J, Waddell, I & Ogilvie, D J 2018, ' Cell-active Small Molecule Inhibitors of the DNA-damage Repair Enzyme Poly(ADP-ribose) Glycohydrolase (PARG): Discovery and Optimization of Orally Bioavailable Quinazolinedione Sulfonamides ', Journal of Medicinal Chemistry, vol. 61, no. 23, pp. 10767–10792 . https://doi.org/10.1021/acs.jmedchem.8b01407
DNA damage repair enzymes are promising targets in the development of new therapeutic agents for a wide range of cancers and potentially other diseases. The enzyme poly(ADP-ribose) glycohydrolase (PARG) plays a pivotal role in the regulation of DNA r
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1e713bd6a754c7026f2f63ab3b3df4e2
https://doi.org/10.1021/acs.jmedchem.8b01407
Zobrazit plný text záznamu
3
Abstract A123: Delivery of a potent, selective, and efficacious RET inhibitor for the treatment of RET-driven lung adenocarcinoma
Autor: Ian D. Waddell, Helen F. Small, Samantha Hitchin, Allan M. Jordan, Mandy Watson, Habiba Begum, Rebecca Newton, Ben Acton, Donald J. Ogilvie, Paul A.T. Kelly
Publikováno v: Molecular Cancer Therapeutics. 17:A123-A123
Background: Constitutive activation of RET kinase activity following mutation or rearrangement can lead to the development of cancers such as medullary thyroid carcinoma and lung adenocarcinoma. The currently approved therapeutics for these diseases
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ed7e31fb4d1262c1e87e15138d2bb330
https://doi.org/10.1158/1535-7163.targ-17-a123
Zobrazit plný text záznamu
4
Abstract 2092: A potent and selective RET inhibitor with efficacy in RET-driven mouse models of medullary thyroid carcinoma and lung adenocarcinoma
Autor: Samantha Hitchin, Mandy Watson, Ian D. Waddell, Helen F. Small, Allan M. Jordan, Donald J. Ogilvie, Habiba Begum, Gina Paris, Rebecca Newton, Ben Acton, Paul A.T. Kelly
Publikováno v: Cancer Research. 77:2092-2092
Background: The aim of this CRUK-MI Drug Discovery project is to deliver a RET-selective inhibitor for the treatment of cancers with RET activating mutations, which include 1-2% of lung adenocarcinomas and medullary thyroid cancers (MTC). Recent data
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::af4d41d88f48a88a7d1eec6bfa94c2e7
https://doi.org/10.1158/1538-7445.am2017-2092
Zobrazit plný text záznamu
5
Abstract 3715: Benzimidazolone sulphonamides - potent, selective and drug-like inhibitors of poly(ADP Ribose) Glycohydrolase (PARG)
Autor: Stuart Donald Jones, James R. Hitchin, Julie A. Tucker, Donald J. Ogilvie, Alison E. McGonagle, Helen F. Small, Cliff Jones, Katherine Clegg Smith, Ben Acton, Bohdan Waszkowycz, Colin Hutton, Allan M. Jordan, Ian D. Waddell, Alex Stowell, Dominic I. James, Nicola Hamilton
Publikováno v: Cancer Research. 76:3715-3715
In recent years, many proteins involved in DNA repair, such as ATR, ATM and PARP, have received considerable attention as potential points of therapeutic intervention in cancer. Indeed, these efforts have recently delivered several agents into clinic
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a369d40a7b7c358c70282e25c732f04e
https://doi.org/10.1158/1538-7445.am2016-3715
Zobrazit plný text záznamu
6
Abstract 3714: Optimisation of quinazolinedione sulphonamides as novel inhibitors of poly(ADP Ribose) glycohydrolase (PARG)
Autor: Nicola Hamilton, Stuart Donald Jones, Ben Acton, Bohdan Waszkowycz, Helen F. Small, Katherine Clegg Smith, Allan M. Jordan, Daniel P. Mould, Julie A. Tucker, Donald J. Ogilvie, Ian D. Waddell, Dominic I. James, Alex Stowell, Alison E. McGonagle, Cliff Jones
Publikováno v: Cancer Research. 76:3714-3714
The macrodomain protein poly(ADP ribose) glycohydrolase (PARG) has been shown to be a critical component in the repair of single stand DNA breaks and counteracts the function of the ARTD family of poly(ADP ribose) polymerases, commonly known as the P
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::189433740f0d1df0d075fea4683860ac
https://doi.org/10.1158/1538-7445.am2016-3714
Zobrazit plný text záznamu
7
Abstract C39: First-in-class inhibitors of the putatively undruggable DNA repair target Poly(ADP-ribose) glycohydrolase (PARG)
Autor: Stuart Donald Jones, Bohdan Waszkowycz, Daniel P. Mould, Nicola Hamilton, Helen F. Small, Sam Fritzl, Alison E. McGonagle, Emma E. Fairweather, Dominic I. James, Alexandra Stowell, Ben Acton, Allan M. Jordan, Niall M. Hamilton, Donald J. Ogilvie, Ian D. Waddell, Kate M. Smith, Sarah Holt, James Hitchen, Colin Hutton
Publikováno v: Molecular Cancer Therapeutics. 14:C39-C39
Poly(ADP-ribose) glycohydrolase (PARG) is the only enzyme known to catalyse hydrolysis of the O-glycosidic linkages of ADP-ribose polymers, thereby reversing the effects of poly(ADP-ribose) polymerases (PARPs). PARG depletion, using RNAi, results in
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b9816dbf4f7964a45b732efd4e40b9a1
https://doi.org/10.1158/1535-7163.targ-15-c39
Zobrazit plný text záznamu
8
Abstract 3656: PARG inhibition: development of novel compounds and a biomarker strategy to determine cell line sensitivity in breast cancer
Autor: Sarah Holt, Ben Acton, Katherine Clegg Smith, Alison E. McGonagle, Bohdan Waszkowycz, Dominic I. James, Ian D. Waddell, James Hitchen, Niall M. Hamilton, Helen F. Small, Donald J. Ogilvie, Allan M. Jordan, Colin Huttom, Emma E. Fairweather, Alex Stowell, Nicola Hamilton
Publikováno v: Cancer Research. 75:3656-3656
Background: DNA single strand breaks (SSBs) are the most common type of damage occurring in cells. Poly (ADP ribose) polymerase (PARP) binds to SSBs and auto-ribosylates itself using NAD+ as a substrate. PARG is the only enzyme known to efficiently c
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::052a37cd6af34cffec8364d9f5556f70
https://doi.org/10.1158/1538-7445.am2015-3656
Zobrazit plný text záznamu

Vyhledávací nástroje:

Upřesnit hledání

Omezení vyhledávání
Plný text Recenzováno Digitální knihovna AV ČR
Zdroje