Publications by authors named "Dan Niculescu-Duvaz"

32Publications

2-Aminomethylene-5-sulfonylthiazole Inhibitors of Lysyl Oxidase (LOX) and LOXL2 Show Significant Efficacy in Delaying Tumor Growth.

Authors:
Deborah A Smithen Leo M H Leung Mairi Challinor Rae Lawrence HaoRan Tang Dan Niculescu-Duvaz Simon P Pearce Robert Mcleary Filipa Lopes Mohammed Aljarah Michael Brown Louise Johnson Graeme Thomson Richard Marais Caroline Springer

J Med Chem 2020 03 4;63(5):2308-2324. Epub 2019 Sep 4.

Drug Discovery Unit, Cancer Research UK Manchester Institute, University of Manchester, Alderley Park, Macclesfield SK10 4TG, United Kingdom.

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March 2020

Author Correction: Lysyl oxidase drives tumour progression by trapping EGF receptors at the cell surface.

Authors:
HaoRan Tang Leo Leung Grazia Saturno Amaya Viros Duncan Smith Gianpiero Di Leva Eamonn Morrison Dan Niculescu-Duvaz Filipa Lopes Louise Johnson Nathalie Dhomen Caroline Springer Richard Marais

Nat Commun 2019 Jul 18;10(1):3151. Epub 2019 Jul 18.

Molecular Oncology Group, Cancer Research UK Manchester Institute, University of Manchester, Manchester, M20 4BX, UK.

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July 2019

Anti-metastatic Inhibitors of Lysyl Oxidase (LOX): Design and Structure-Activity Relationships.

Authors:
Leo Leung Dan Niculescu-Duvaz Deborah Smithen Filipa Lopes Cedric Callens Robert McLeary Grazia Saturno Lawrence Davies Mohammed Aljarah Michael Brown Louise Johnson Alfonso Zambon Tim Chambers Delphine Ménard Natasha Bayliss Ruth Knight Laura Fish Rae Lawrence Mairi Challinor HaoRan Tang Richard Marais Caroline Springer

J Med Chem 2019 06 23;62(12):5863-5884. Epub 2019 May 23.

Cancer Research UK Centre for Cancer Therapeutics , The Institute of Cancer Research , 15 Cotswold Road , London SM2 5NG , United Kingdom.

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June 2019

Lysyl oxidase drives tumour progression by trapping EGF receptors at the cell surface.

Authors:
HaoRan Tang Leo Leung Grazia Saturno Amaya Viros Duncan Smith Gianpiero Di Leva Eamonn Morrison Dan Niculescu-Duvaz Filipa Lopes Louise Johnson Nathalie Dhomen Caroline Springer Richard Marais

Nat Commun 2017 04 18;8:14909. Epub 2017 Apr 18.

Molecular Oncology Group, Cancer Research UK Manchester Institute, University of Manchester, Manchester M20 4BX, UK.

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April 2017

Paradox-Breaking RAF Inhibitors that Also Target SRC Are Effective in Drug-Resistant BRAF Mutant Melanoma.

Authors:
Maria Romina Girotti Filipa Lopes Natasha Preece Dan Niculescu-Duvaz Alfonso Zambon Lawrence Davies Steven Whittaker Grazia Saturno Amaya Viros Malin Pedersen Bart M J M Suijkerbuijk Delphine Menard Robert McLeary Louise Johnson Laura Fish Sarah Ejiama Berta Sanchez-Laorden Juliane Hohloch Neil Carragher Kenneth Macleod Garry Ashton Anna A Marusiak Alberto Fusi John Brognard Margaret Frame Paul Lorigan Richard Marais Caroline Springer

Cancer Cell 2017 03;31(3):466

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March 2017

Paradox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanoma.

Authors:
Maria Romina Girotti Filipa Lopes Natasha Preece Dan Niculescu-Duvaz Alfonso Zambon Lawrence Davies Steven Whittaker Grazia Saturno Amaya Viros Malin Pedersen Bart M J M Suijkerbuijk Delphine Menard Robert McLeary Louise Johnson Laura Fish Sarah Ejiama Berta Sanchez-Laorden Juliane Hohloch Neil Carragher Kenneth Macleod Garry Ashton Anna A Marusiak Alberto Fusi John Brognard Margaret Frame Paul Lorigan Richard Marais Caroline Springer

Cancer Cell 2015 Jan 11;27(1):85-96. Epub 2014 Dec 11.

Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, UK. Electronic address:

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January 2015

BRAF inhibitors induce metastasis in RAS mutant or inhibitor-resistant melanoma cells by reactivating MEK and ERK signaling.

Authors:
Berta Sanchez-Laorden Amaya Viros Maria Romina Girotti Malin Pedersen Grazia Saturno Alfonso Zambon Dan Niculescu-Duvaz Samra Turajlic Andrew Hayes Martin Gore James Larkin Paul Lorigan Martin Cook Caroline Springer Richard Marais

Sci Signal 2014 Mar 25;7(318):ra30. Epub 2014 Mar 25.

1Molecular Oncology Group, Cancer Research UK Manchester Institute, The University of Manchester, Manchester M20 4BX, UK.

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March 2014

Potent BRAF kinase inhibitors based on 2,4,5-trisubstituted imidazole with naphthyl and benzothiophene 4-substituents.

Authors:
Dan Niculescu-Duvaz Ion Niculescu-Duvaz Bart M J M Suijkerbuijk Delphine Ménard Alfonso Zambon Lawrence Davies Jean-Francois Pons Steven Whittaker Richard Marais Caroline J Springer

Bioorg Med Chem 2013 Mar 3;21(5):1284-304. Epub 2013 Jan 3.

The Institute of Cancer Research, Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, 15 Cotswold Road, Sutton, Surrey SM2 5NG, United Kingdom.

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March 2013

BRAF as a therapeutic target: a patent review (2006 - 2012).

Authors:
Alfonso Zambon Dan Niculescu-Duvaz Ion Niculescu-Duvaz Richard Marais Caroline J Springer

Expert Opin Ther Pat 2013 Feb 7;23(2):155-64. Epub 2013 Jan 7.

The Institute of Cancer Research, Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, 15 Cotswold Road, Sutton, Surrey, SM2 5NG, UK.

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February 2013

Inhibiting EGF receptor or SRC family kinase signaling overcomes BRAF inhibitor resistance in melanoma.

Authors:
Maria R Girotti Malin Pedersen Berta Sanchez-Laorden Amaya Viros Samra Turajlic Dan Niculescu-Duvaz Alfonso Zambon John Sinclair Andrew Hayes Martin Gore Paul Lorigan Caroline Springer James Larkin Claus Jorgensen Richard Marais

Cancer Discov 2013 Feb 14;3(2):158-67. Epub 2012 Dec 14.

Signal Transduction Team, The Institute of Cancer Research, Royal Marsden Hospital, London, UK.

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February 2013

Topical 5-fluorouracil elicits regressions of BRAF inhibitor-induced cutaneous squamous cell carcinoma.

Authors:
Amaya Viros Robert Hayward Matthew Martin Sharona Yashar Clarissa C Yu Berta Sanchez-Laorden Alfonso Zambon Dan Niculescu-Duvaz Caroline Springer Roger S Lo Richard Marais

J Invest Dermatol 2013 Jan 16;133(1):274-6. Epub 2012 Aug 16.

Seccio Dermatologia, Departament de Medicina, Hospital Universitari Vall d’Hebron, Universitat Autonomade Barcelona, Spain.

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January 2013

RAS mutations in cutaneous squamous-cell carcinomas in patients treated with BRAF inhibitors.

Authors:
Fei Su Amaya Viros Carla Milagre Kerstin Trunzer Gideon Bollag Olivia Spleiss Jorge S Reis-Filho Xiangju Kong Richard C Koya Keith T Flaherty Paul B Chapman Min Jung Kim Robert Hayward Matthew Martin Hong Yang Qiongqing Wang Holly Hilton Julie S Hang Johannes Noe Maryou Lambros Felipe Geyer Nathalie Dhomen Ion Niculescu-Duvaz Alfonso Zambon Dan Niculescu-Duvaz Natasha Preece Lídia Robert Nicholas J Otte Stephen Mok Damien Kee Yan Ma Chao Zhang Gaston Habets Elizabeth A Burton Bernice Wong Hoa Nguyen Mark Kockx Luc Andries Brian Lestini Keith B Nolop Richard J Lee Andrew K Joe James L Troy Rene Gonzalez Thomas E Hutson Igor Puzanov Bartosz Chmielowski Caroline J Springer Grant A McArthur Jeffrey A Sosman Roger S Lo Antoni Ribas Richard Marais

N Engl J Med 2012 Jan;366(3):207-15

Hoffmann-La Roche, Nutley, NJ, USA.

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January 2012

Small molecule inhibitors of BRAF in clinical trials.

Authors:
Alfonso Zambon Ion Niculescu-Duvaz Dan Niculescu-Duvaz Richard Marais Caroline J Springer

Bioorg Med Chem Lett 2012 Jan 3;22(2):789-92. Epub 2011 Dec 3.

The Institute of Cancer Research, Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, 15 Cotswold Road, Sutton, Surrey SM2 5NG, United Kingdom.

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January 2012

Novel tricyclic pyrazole BRAF inhibitors with imidazole or furan central scaffolds.

Authors:
Dan Niculescu-Duvaz Ion Niculescu-Duvaz Bart M J M Suijkerbuijk Delphine Ménard Alfonso Zambon Arnaud Nourry Lawrence Davies Helen A Manne Frank Friedlos Lesley Ogilvie Douglas Hedley Andrew K Takle David M Wilson Jean-Francois Pons Tom Coulter Ruth Kirk Neus Cantarino Steven Whittaker Richard Marais Caroline J Springer

Bioorg Med Chem 2010 Sep 15;18(18):6934-52. Epub 2010 Jun 15.

Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, 15 Cotswold Road, Sutton, Surrey SM2 5NG, United Kingdom.

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September 2010

Novel hinge binder improves activity and pharmacokinetic properties of BRAF inhibitors.

Authors:
Alfonso Zambon Delphine Ménard Bart M J M Suijkerbuijk Ion Niculescu-Duvaz Steven Whittaker Dan Niculescu-Duvaz Arnaud Nourry Lawrence Davies Helen A Manne Filipa Lopes Natasha Preece Douglas Hedley Lesley M Ogilvie Ruth Kirk Richard Marais Caroline J Springer

J Med Chem 2010 Aug;53(15):5639-55

The Institute of Cancer Research, Cancer Research UK Centre for Cancer Therapeutics, Sutton, Surrey, UK.

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August 2010

Gatekeeper mutations mediate resistance to BRAF-targeted therapies.

Authors:
Steven Whittaker Ruth Kirk Robert Hayward Alfonso Zambon Amaya Viros Neus Cantarino Annette Affolter Arnaud Nourry Dan Niculescu-Duvaz Caroline Springer Richard Marais

Sci Transl Med 2010 Jun;2(35):35ra41

Institute of Cancer Research, London, UK.

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June 2010

Development of novel, highly potent inhibitors of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF): increasing cellular potency through optimization of a distal heteroaromatic group.

Authors:
Bart M J M Suijkerbuijk Ion Niculescu-Duvaz Catherine Gaulon Harmen P Dijkstra Dan Niculescu-Duvaz Delphine Ménard Alfonso Zambon Arnaud Nourry Lawrence Davies Helen A Manne Frank Friedlos Lesley M Ogilvie Douglas Hedley Filipa Lopes Natasha P U Preece Javier Moreno-Farre Florence I Raynaud Ruth Kirk Steven Whittaker Richard Marais Caroline J Springer

J Med Chem 2010 Apr;53(7):2741-56

The Institute of Cancer Research, Cancer Research UK Centre for Cancer Therapeutics, 15 Cotswold Road, Sutton, Surrey SM2 5NG, United Kingdom.

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April 2010

BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.

Authors:
Arnaud Nourry Alfonso Zambon Lawrence Davies Ion Niculescu-Duvaz Harmen P Dijkstra Delphine Ménard Catherine Gaulon Dan Niculescu-Duvaz Bart M J M Suijkerbuijk Frank Friedlos Helen A Manne Ruth Kirk Steven Whittaker Richard Marais Caroline J Springer

J Med Chem 2010 Mar;53(5):1964-78

Cancer Research UK Centre of Cancer Therapeutics, The Institute of Cancer Research, 15 Cotswold Road, Sutton, Surrey SM2 5NG, United Kingdom.

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March 2010

C-end your drugs using peptide tags.

Authors:
Dan Niculescu-Duvaz Caroline Springer Richard Marais

Pigment Cell Melanoma Res 2010 Apr 20;23(2):157-9. Epub 2010 Jan 20.

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April 2010

Novel potent BRAF inhibitors: toward 1 nM compounds through optimization of the central phenyl ring.

Authors:
Delphine Ménard Ion Niculescu-Duvaz Harmen P Dijkstra Dan Niculescu-Duvaz Bart M J M Suijkerbuijk Alfonso Zambon Arnaud Nourry Esteban Roman Lawrence Davies Helen A Manne Frank Friedlos Ruth Kirk Steven Whittaker Adrian Gill Richard D Taylor Richard Marais Caroline J Springer

J Med Chem 2009 Jul;52(13):3881-91

The Institute of Cancer Research, UK Centre for Cancer Therapeutics, Sutton, Surrey SM2 5NG, United Kingdom.

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July 2009