Selected bibliography
Activity of hydrolytic enzymes in tumour cells is a determinant for anti-tumour efficacy of the melphalan containing prodrug J1.
Gullbo J, Wickström M, Tullberg M, Ehrsson H, Lewensohn R, Nygren P, Luthman K, Larsson R. J Drug Target. 2003 Jul;11(6):355-63. PMID: 14668056
https://www.ncbi.nlm.nih.gov/pubmed/14668056
Antitumor activity of the alkylating oligopeptides J1 (L-melphalanyl-p-L-fluorophenylalanine ethyl ester) and P2 (L-prolyl-m-L-sarcolysyl-p-L-fluorophenylalanine ethyl ester): comparison with melphalan.
Gullbo J, Dhar S, Luthman K, Ehrsson H, Lewensohn R, Nygren P, Larsson R. Anticancer Drugs. 2003 Sep;14(8):617-24. PMID: 14501383
https://www.ncbi.nlm.nih.gov/pubmed/14501383
Antitumor efficacy and acute toxicity of the novel dipeptide melphalanyl-p-L-fluorophenylalanine ethyl ester (J1) in vivo.
Gullbo J, Lindhagen E, Bashir-Hassan S, Tullberg M, Ehrsson H, Lewensohn R, Nygren P, De La Torre M, Luthman K, Larsson R. Invest New Drugs. 2004 Nov;22(4):411-20.
https://www.ncbi.nlm.nih.gov/pubmed/15292711
The novel melphalan prodrug J1 inhibits neuroblastoma growth in vitro and in vivo.
Wickström M, Johnsen JI, Ponthan F, Segerström L, Sveinbjörnsson B, Lindskog M, Lövborg H, Viktorsson K, Lewensohn R, Kogner P, Larsson R, Gullbo J. Mol Cancer Ther. 2007 Sep;6(9):2409-17. PMID: 17876040
https://www.ncbi.nlm.nih.gov/pubmed/17876040
The novel alkylating prodrug J1: diagnosis directed activity profile ex vivo and combination analyses in vitro.
Wickström M, Haglund C, Lindman H, Nygren P, Larsson R, Gullbo J. Invest New Drugs. 2008 Jun;26(3):195-204. Epub 2007 Oct 6.
https://www.ncbi.nlm.nih.gov/pubmed/17922077
The alkylating prodrug J1 can be activated by aminopeptidase N, leading to a possible target directed release of melphalan.
Wickström M, Viktorsson K, Lundholm L, Aesoy R, Nygren H, Sooman L, Fryknäs M, Vogel LK, Lewensohn R, Larsson R, Gullbo J. Biochem Pharmacol. 2010 May 1;79(9):1281-90. doi: 10.1016/j.bcp.2009.12.022. Epub 2010 Jan 11. PMID: 20067771
https://www.ncbi.nlm.nih.gov/pubmed/20067771
Aminopeptidase N (CD13) as a target for cancer chemotherapy.
Wickström M, Larsson R, Nygren P, Gullbo J. Cancer Sci. 2011 Mar;102(3):501-8. doi: 10.1111/j.1349-7006.2010.01826.x. Epub 2011 Jan 30. Review. PMID: 21205077
https://www.ncbi.nlm.nih.gov/pubmed/21205077
Drug response in a genetically engineered mouse model of multiple myeloma is predictive of clinical efficacy.
Chesi M, Matthews GM, Garbitt VM, Palmer SE, Shortt J, Lefebure M, Stewart AK, Johnstone RW, Bergsagel PL. Blood. 2012 Jul 12;120(2):376-85. doi: 10.1182/blood-2012-02-412783. Epub 2012 Mar 26. PMID: 22451422
https://www.ncbi.nlm.nih.gov/pubmed/22451422
In vitro and in vivo antitumor activity of a novel alkylating agent, melphalan-flufenamide, against multiple myeloma cells.
Chauhan D, Ray A, Viktorsson K, Spira J, Paba-Prada C, Munshi N, Richardson P, Lewensohn R, Anderson KC. Clin Cancer Res. 2013 Jun 1;19(11):3019-31. doi: 10.1158/1078-0432.CCR-12-3752. Epub 2013 Apr 12. PMID: 23584492
https://www.ncbi.nlm.nih.gov/pubmed/23584492
The novel alkylating prodrug melflufen (J1) inhibits angiogenesis in vitro and in vivo.
Strese S, Wickström M, Fuchs PF, Fryknäs M, Gerwins P, Dale T, Larsson R, Gullbo J. Biochem Pharmacol. 2013 Oct 1;86(7):888-95. doi: 10.1016/j.bcp.2013.07.026. Epub 2013 Aug 8. PMID: 23933387
https://www.ncbi.nlm.nih.gov/pubmed/23933387
First-in-human, phase I/IIa clinical study of the peptidase potentiated alkylator melflufen administered every three weeks to patients with advanced solid tumor malignancies.
Berglund Å, Ullén A, Lisyanskaya A, Orlov S, Hagberg H, Tholander B, Lewensohn R, Nygren P, Spira J, Harmenberg J, Jerling M, Alvfors C, Ringbom M, Nordström E, Söderlind K, Gullbo J. Invest New Drugs. 2015 Dec;33(6):1232-41. doi: 10.1007/s10637-015-0299-2. Epub 2015 Nov 10. PMID: 26553306
https://www.ncbi.nlm.nih.gov/pubmed/26553306
Melphalan-flufenamide is cytotoxic and potentiates treatment with chemotherapy and the Src inhibitor dasatinib in urothelial carcinoma.
Viktorsson K, Shah CH, Juntti T, Hååg P, Zielinska-Chomej K, Sierakowiak A, Holmsten K, Tu J, Spira J, Kanter L, Lewensohn R, Ullén A.
Mol Oncol. 2016 Jan 2. pii: S1574-7891(15)00249-5. PMID: 26827254
https://www.ncbi.nlm.nih.gov/pubmed/26827254