Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Ainslie Whiting"'
Autor:
Luke R Odell, Nigel C. Jones, Ngoc Chau, Mark J. Robertson, Joseph I Ambrus, Fiona M Deane, Kelly A. Young, Ainslie Whiting, Jing Xue, Kate Prichard, James A. Daniel, Nick N. Gorgani, Terence J O'brien, Phillip J Robinson, Adam McCluskey
Publikováno v:
RSC Medicinal Chemistry.
We show that dansylcadaverine (1) a known in-cell inhibitor of clathrin mediated endocytosis (CME), moderately inhibits dynamin I (dynI) GTPase activity (IC50 45 μM) and transferrin (Tfn) endocytosis in U2OS...
Autor:
Ngoc Chau, Phillip J. Robinson, Wiebke Stahlschmidt, Jennifer R. Baker, Adam McCluskey, Ainslie Whiting, Volker Haucke, Mark J. Robertson, Lisa von Kleist, Marc Nazaré, André Horatscheck, Samantha Sauer
Publikováno v:
Organic & Biomolecular Chemistry. 14:11266-11278
The development of a (Z)-5-((6,8-dichloro-4-oxo-4H-chromen-3-yl)methylene)-2-thioxothiazolidin-4-one (2), rhodanine-based lead that led to the Pitstop® 2 family of clathrin inhibitors is described herein. Head group substitution and bioisosteric rep
Autor:
Shannon R. Joseph, James A. Daniel, Phillip J. Robinson, Peter Maamary, Adam McCluskey, Sai Krishnan, Lingbo Hu, Lisa von Kleist, Ainslie Whiting, Volker Haucke, Ngoc Chau, Fiona Simpson, Mohammed K. Abdel-Hamid
Publikováno v:
Traffic. 16:635-654
Chlorpromazine is a phenothiazine-derived antipsychotic drug (APD) that inhibits clathrin-mediated endocytosis (CME) in cells by an unknown mechanism. We examined whether its action and that of other APDs might be mediated by the GTPase activity of d
Autor:
Anna Mariana, Ngoc Chau, Ainslie Whiting, Kylie A. MacGregor, Phillip J. Robinson, Luke R. Odell, Adam McCluskey, Mohammed K. Abdel-Hamid
Publikováno v:
Organic & Biomolecular Chemistry. 13:8016-8028
Fragment-based in silico screening against dynamin I (dynI) GTPase activity identified the 1,8-naphthalimide framework as a potential scaffold for the design of new inhibitors targeting the GTP binding pocket of dynI. Structure-based design, synthesi
Autor:
Mark J. Robertson, Wiebke Stahlschmidt, Kylie A. MacGregor, Phillip J. Robinson, Lisa von Kleist, Adam McCluskey, Ngoc Chau, Kelly A. Young, Ainslie Whiting, Volker Haucke
Publikováno v:
Journal of Medicinal Chemistry. 57:131-143
We reported the first small molecule inhibitors of the interaction between the clathrin N-terminal domain (TD) and endocyctic accessory proteins (i.e., clathrin inhibition1). Initial screening of a ∼17 000 small molecule ChemBioNet library identifi
Autor:
Anna Mariana, Jennette A. Sakoff, Kelly A. Young, Luke R. Odell, Jayne Gilbert, Timothy A. Hill, Damien J. Keating, Aimee E. Novelle, Nick N. Gorgani, Phillip J. Robinson, Ngoc Chau, Megan Chircop, Ellen M. van Dam, James A. Daniel, Fiona M. Deane, Michael A. Cousin, Ainslie Whiting, Adam McCluskey, Annie Quan, Swetha Perera, Andrew B. McGeachie
Publikováno v:
ACS Chemical Biology. 8:1507-1518
Dynamin is required for clathrin-mediated endocytosis (CME). Its GTPase activity is stimulated by phospholipid binding to its PH domain, which induces helical oligomerization. We have designed a series of novel pyrimidine-based "Pyrimidyn" compounds
Autor:
Joseph I. Ambrus, Ngoc Chau, Ainslie Whiting, Anna Mariana, Gordana Hadzic, Volker Haucke, Adam McCluskey, D. Yuri Pomè, Phillip J. Robinson, Emily D.E.R. Hyde, Lisa von Kleist, Mark J. Robertson
Publikováno v:
ACS medicinal chemistry letters, 3(5): 352–356
Six focused rhodanine-based libraries, 60 compounds in total, were synthesized and evaluated as potential dynamin I GTPase inhibitors. Twenty-six were more potent than the lead compound with 13 returning IC50 values ≤10 μM, making the Rhodadyn ser
The Pthaladyns: GTP Competitive Inhibitors of Dynamin I and II GTPase Derived from Virtual Screening
Autor:
Mark J. Robertson, Ainslie Whiting, Anna Mariana, Adam McCluskey, Nick N. Gorgani, Ruben Abagyan, Christopher P. Gordon, Dian Herlinda Octorina Howan, Luke R. Odell, Ngoc Chau, Phillip J. Robinson, James A. Daniel
Publikováno v:
Journal of Medicinal Chemistry. 53:5267-5280
We report the development of a homology model for the GTP binding domain of human dynamin I based on the corresponding crystal structure of Dictyostelium discoidum dynamin A. Virtual screening identified 2-[(2-biphenyl-2-yl-1,3-dioxo-2,3-dihydro-1H-i
Autor:
James A, Daniel, Ngoc, Chau, Mohammed K, Abdel-Hamid, Lingbo, Hu, Lisa, von Kleist, Ainslie, Whiting, Sai, Krishnan, Peter, Maamary, Shannon R, Joseph, Fiona, Simpson, Volker, Haucke, Adam, McCluskey, Phillip J, Robinson
Publikováno v:
Traffic (Copenhagen, Denmark). 16(6)
Chlorpromazine is a phenothiazine-derived antipsychotic drug (APD) that inhibits clathrin-mediated endocytosis (CME) in cells by an unknown mechanism. We examined whether its action and that of other APDs might be mediated by the GTPase activity of d
Autor:
Mohammed K. Abdel-Hamid, Adam McCluskey, Ainslie Whiting, Kylie A. MacGregor, Ngoc Chau, Phillip J. Robinson, Luke R. Odell
Publikováno v:
European journal of medicinal chemistry. 85
Virtual screening of the ChemDiversity and ChemBridge compound databases against dynamin I (dynI) GTPase activity identified 2,5-bis-(benzylamino)-1,4-benzoquinone 1 as a 273 ± 106 μM inhibitor. In silico lead optimization and focused library-led s