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Items: 36

1.

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

Smithen DA, Leung LMH, Challinor M, Lawrence R, Tang H, Niculescu-Duvaz D, Pearce SP, Mcleary R, Lopes F, Aljarah M, Brown M, Johnson L, Thomson G, Marais R, Springer C.

J Med Chem. 2019 Sep 4. doi: 10.1021/acs.jmedchem.9b01112. [Epub ahead of print]

PMID:
31430136
2.

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

Tang H, Leung L, Saturno G, Viros A, Smith D, Leva GD, Morrison E, Niculescu-Duvaz D, Lopes F, Johnson L, Dhomen N, Springer C, Marais R.

Nat Commun. 2019 Jul 18;10(1):3151. doi: 10.1038/s41467-019-11220-x.

3.

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

Leung L, Niculescu-Duvaz D, Smithen D, Lopes F, Callens C, McLeary R, Saturno G, Davies L, Aljarah M, Brown M, Johnson L, Zambon A, Chambers T, Ménard D, Bayliss N, Knight R, Fish L, Lawrence R, Challinor M, Tang H, Marais R, Springer C.

J Med Chem. 2019 Jun 27;62(12):5863-5884. doi: 10.1021/acs.jmedchem.9b00335. Epub 2019 May 23.

PMID:
31070916
4.

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

Tang H, Leung L, Saturno G, Viros A, Smith D, Di Leva G, Morrison E, Niculescu-Duvaz D, Lopes F, Johnson L, Dhomen N, Springer C, Marais R.

Nat Commun. 2017 Apr 18;8:14909. doi: 10.1038/ncomms14909. Erratum in: Nat Commun. 2019 Jul 18;10(1):3151.

5.

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

Girotti MR, Lopes F, Preece N, Niculescu-Duvaz D, Zambon A, Davies L, Whittaker S, Saturno G, Viros A, Pedersen M, Suijkerbuijk BMJM, Menard D, McLeary R, Johnson L, Fish L, Ejiama S, Sanchez-Laorden B, Hohloch J, Carragher N, Macleod K, Ashton G, Marusiak AA, Fusi A, Brognard J, Frame M, Lorigan P, Marais R, Springer C.

Cancer Cell. 2017 Mar 13;31(3):466. doi: 10.1016/j.ccell.2017.02.007. No abstract available.

6.

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

Girotti MR, Lopes F, Preece N, Niculescu-Duvaz D, Zambon A, Davies L, Whittaker S, Saturno G, Viros A, Pedersen M, Suijkerbuijk BM, Menard D, McLeary R, Johnson L, Fish L, Ejiama S, Sanchez-Laorden B, Hohloch J, Carragher N, Macleod K, Ashton G, Marusiak AA, Fusi A, Brognard J, Frame M, Lorigan P, Marais R, Springer C.

Cancer Cell. 2015 Jan 12;27(1):85-96. doi: 10.1016/j.ccell.2014.11.006. Epub 2014 Dec 11. Erratum in: Cancer Cell. 2017 Mar 13;31(3):466.

7.

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

Sanchez-Laorden B, Viros A, Girotti MR, Pedersen M, Saturno G, Zambon A, Niculescu-Duvaz D, Turajlic S, Hayes A, Gore M, Larkin J, Lorigan P, Cook M, Springer C, Marais R.

Sci Signal. 2014 Mar 25;7(318):ra30. doi: 10.1126/scisignal.2004815.

PMID:
24667377
8.

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

Niculescu-Duvaz D, Niculescu-Duvaz I, Suijkerbuijk BM, Ménard D, Zambon A, Davies L, Pons JF, Whittaker S, Marais R, Springer CJ.

Bioorg Med Chem. 2013 Mar 1;21(5):1284-304. doi: 10.1016/j.bmc.2012.12.035. Epub 2013 Jan 3.

PMID:
23376011
9.

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

Zambon A, Niculescu-Duvaz D, Niculescu-Duvaz I, Marais R, Springer CJ.

Expert Opin Ther Pat. 2013 Feb;23(2):155-64. doi: 10.1517/13543776.2013.741593. Epub 2013 Jan 7. Review.

PMID:
23294221
10.

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

Girotti MR, Pedersen M, Sanchez-Laorden B, Viros A, Turajlic S, Niculescu-Duvaz D, Zambon A, Sinclair J, Hayes A, Gore M, Lorigan P, Springer C, Larkin J, Jorgensen C, Marais R.

Cancer Discov. 2013 Feb;3(2):158-67. doi: 10.1158/2159-8290.CD-12-0386. Epub 2012 Dec 14.

11.

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

Viros A, Hayward R, Martin M, Yashar S, Yu CC, Sanchez-Laorden B, Zambon A, Niculescu-Duvaz D, Springer C, Lo RS, Marais R.

J Invest Dermatol. 2013 Jan;133(1):274-6. doi: 10.1038/jid.2012.268. Epub 2012 Aug 16. No abstract available. Erratum in: J Invest Dermatol. 2013 Jun;133(6):1691.

12.

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

Su F, Viros A, Milagre C, Trunzer K, Bollag G, Spleiss O, Reis-Filho JS, Kong X, Koya RC, Flaherty KT, Chapman PB, Kim MJ, Hayward R, Martin M, Yang H, Wang Q, Hilton H, Hang JS, Noe J, Lambros M, Geyer F, Dhomen N, Niculescu-Duvaz I, Zambon A, Niculescu-Duvaz D, Preece N, Robert L, Otte NJ, Mok S, Kee D, Ma Y, Zhang C, Habets G, Burton EA, Wong B, Nguyen H, Kockx M, Andries L, Lestini B, Nolop KB, Lee RJ, Joe AK, Troy JL, Gonzalez R, Hutson TE, Puzanov I, Chmielowski B, Springer CJ, McArthur GA, Sosman JA, Lo RS, Ribas A, Marais R.

N Engl J Med. 2012 Jan 19;366(3):207-15. doi: 10.1056/NEJMoa1105358.

13.

Small molecule inhibitors of BRAF in clinical trials.

Zambon A, Niculescu-Duvaz I, Niculescu-Duvaz D, Marais R, Springer CJ.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):789-92. doi: 10.1016/j.bmcl.2011.11.060. Epub 2011 Dec 3. Review.

PMID:
22222036
14.

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

Niculescu-Duvaz D, Niculescu-Duvaz I, Suijkerbuijk BM, Ménard D, Zambon A, Nourry A, Davies L, Manne HA, Friedlos F, Ogilvie L, Hedley D, Takle AK, Wilson DM, Pons JF, Coulter T, Kirk R, Cantarino N, Whittaker S, Marais R, Springer CJ.

Bioorg Med Chem. 2010 Sep 15;18(18):6934-52. doi: 10.1016/j.bmc.2010.06.031. Epub 2010 Jun 15.

15.

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

Zambon A, Ménard D, Suijkerbuijk BM, Niculescu-Duvaz I, Whittaker S, Niculescu-Duvaz D, Nourry A, Davies L, Manne HA, Lopes F, Preece N, Hedley D, Ogilvie LM, Kirk R, Marais R, Springer CJ.

J Med Chem. 2010 Aug 12;53(15):5639-55. doi: 10.1021/jm100383b.

PMID:
20597484
16.

Gatekeeper mutations mediate resistance to BRAF-targeted therapies.

Whittaker S, Kirk R, Hayward R, Zambon A, Viros A, Cantarino N, Affolter A, Nourry A, Niculescu-Duvaz D, Springer C, Marais R.

Sci Transl Med. 2010 Jun 9;2(35):35ra41. doi: 10.1126/scitranslmed.3000758.

17.

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.

Suijkerbuijk BM, Niculescu-Duvaz I, Gaulon C, Dijkstra HP, Niculescu-Duvaz D, Ménard D, Zambon A, Nourry A, Davies L, Manne HA, Friedlos F, Ogilvie LM, Hedley D, Lopes F, Preece NP, Moreno-Farre J, Raynaud FI, Kirk R, Whittaker S, Marais R, Springer CJ.

J Med Chem. 2010 Apr 8;53(7):2741-56. doi: 10.1021/jm900607f.

PMID:
20199087
18.

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

Nourry A, Zambon A, Davies L, Niculescu-Duvaz I, Dijkstra HP, Ménard D, Gaulon C, Niculescu-Duvaz D, Suijkerbuijk BM, Friedlos F, Manne HA, Kirk R, Whittaker S, Marais R, Springer CJ.

J Med Chem. 2010 Mar 11;53(5):1964-78. doi: 10.1021/jm901509a.

PMID:
20148563
19.

C-end your drugs using peptide tags.

Niculescu-Duvaz D, Springer C, Marais R.

Pigment Cell Melanoma Res. 2010 Apr;23(2):157-9. doi: 10.1111/j.1755-148X.2010.00675.x. Epub 2010 Jan 20. No abstract available.

PMID:
20088872
20.

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

Ménard D, Niculescu-Duvaz I, Dijkstra HP, Niculescu-Duvaz D, Suijkerbuijk BM, Zambon A, Nourry A, Roman E, Davies L, Manne HA, Friedlos F, Kirk R, Whittaker S, Gill A, Taylor RD, Marais R, Springer CJ.

J Med Chem. 2009 Jul 9;52(13):3881-91. doi: 10.1021/jm900242c.

PMID:
19473026
21.

Pyridoimidazolones as novel potent inhibitors of v-Raf murine sarcoma viral oncogene homologue B1 (BRAF).

Niculescu-Duvaz D, Gaulon C, Dijkstra HP, Niculescu-Duvaz I, Zambon A, Ménard D, Suijkerbuijk BM, Nourry A, Davies L, Manne H, Friedlos F, Ogilvie L, Hedley D, Whittaker S, Kirk R, Gill A, Taylor RD, Raynaud FI, Moreno-Farre J, Marais R, Springer CJ.

J Med Chem. 2009 Apr 23;52(8):2255-64. doi: 10.1021/jm801509w. Erratum in: J Med Chem. 2009 Sep 24;52(18):5770.

PMID:
19323560
22.

Novel inhibitors of the v-raf murine sarcoma viral oncogene homologue B1 (BRAF) based on a 2,6-disubstituted pyrazine scaffold.

Niculescu-Duvaz I, Roman E, Whittaker SR, Friedlos F, Kirk R, Scanlon IJ, Davies LC, Niculescu-Duvaz D, Marais R, Springer CJ.

J Med Chem. 2008 Jun 12;51(11):3261-74. doi: 10.1021/jm070776b. Epub 2008 May 13.

PMID:
18473434
23.

Long functionalized poly(ethylene glycol)s of defined molecular weight: synthesis and application in solid-phase synthesis of conjugates.

Niculescu-Duvaz D, Getaz J, Springer CJ.

Bioconjug Chem. 2008 Apr;19(4):973-81. doi: 10.1021/bc060242+. Epub 2008 Apr 2.

PMID:
18380471
24.

The EGF receptor Hokey-Cokey.

Niculescu-Duvaz D, Whittaker S, Springer C, Marais R.

Cancer Cell. 2007 Mar;11(3):209-11.

25.

Novel inhibitors of B-RAF based on a disubstituted pyrazine scaffold. Generation of a nanomolar lead.

Niculescu-Duvaz I, Roman E, Whittaker SR, Friedlos F, Kirk R, Scanlon IJ, Davies LC, Niculescu-Duvaz D, Marais R, Springer CJ.

J Med Chem. 2006 Jan 12;49(1):407-16.

PMID:
16392826
26.

B-RAF is a therapeutic target in melanoma.

Karasarides M, Chiloeches A, Hayward R, Niculescu-Duvaz D, Scanlon I, Friedlos F, Ogilvie L, Hedley D, Martin J, Marshall CJ, Springer CJ, Marais R.

Oncogene. 2004 Aug 19;23(37):6292-8.

PMID:
15208680
27.
28.

V599EB-RAF is an oncogene in melanocytes.

Wellbrock C, Ogilvie L, Hedley D, Karasarides M, Martin J, Niculescu-Duvaz D, Springer CJ, Marais R.

Cancer Res. 2004 Apr 1;64(7):2338-42.

29.

Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF.

Wan PT, Garnett MJ, Roe SM, Lee S, Niculescu-Duvaz D, Good VM, Jones CM, Marshall CJ, Springer CJ, Barford D, Marais R; Cancer Genome Project.

Cell. 2004 Mar 19;116(6):855-67.

30.

Design of prodrugs for suicide gene therapy.

Niculescu-Duvaz D, Niculescu-Duvaz I, Springer CJ.

Methods Mol Med. 2004;90:161-202. Review. No abstract available.

PMID:
14657564
31.

Self-immolative nitrogen mustards prodrugs cleavable by carboxypeptidase G2 (CPG2) showing large cytotoxicity differentials in GDEPT.

Niculescu-Duvaz D, Niculescu-Duvaz I, Friedlos F, Martin J, Lehouritis P, Marais R, Springer CJ.

J Med Chem. 2003 Apr 24;46(9):1690-705.

PMID:
12699387
32.

Structure-activity relationship in cationic lipid mediated gene transfection.

Niculescu-Duvaz D, Heyes J, Springer CJ.

Curr Med Chem. 2003 Jul;10(14):1233-61. Review.

PMID:
12678797
33.

Synthesis of novel cationic lipids: effect of structural modification on the efficiency of gene transfer.

Heyes JA, Niculescu-Duvaz D, Cooper RG, Springer CJ.

J Med Chem. 2002 Jan 3;45(1):99-114.

PMID:
11754582
34.

Prodrugs for antibody- and gene-directed enzyme prodrug therapies (ADEPT and GDEPT).

Niculescu-Duvaz I, Friedlos F, Niculescu-Duvaz D, Davies L, Springer CJ.

Anticancer Drug Des. 1999 Dec;14(6):517-38. Review.

PMID:
10834273
35.

Self-immolative anthracycline prodrugs for suicide gene therapy.

Niculescu-Duvaz I, Niculescu-Duvaz D, Friedlos F, Spooner R, Martin J, Marais R, Springer CJ.

J Med Chem. 1999 Jul 1;42(13):2485-9.

PMID:
10395490
36.

Self-immolative nitrogen mustard prodrugs for suicide gene therapy.

Niculescu-Duvaz D, Niculescu-Duvaz I, Friedlos F, Martin J, Spooner R, Davies L, Marais R, Springer CJ.

J Med Chem. 1998 Dec 17;41(26):5297-309.

PMID:
9857097

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