Millennium Pharmaceuticals, Inc. (MLNM) Message Board

STOCKTALK

We've detected that you're using an ad content blocking browser plug-in or feature. Ads provide a critical source of revenue to the continued operation of Silicon Investor. We ask that you disable ad blocking while on Silicon Investor in the best interests of our community. If you are not using an ad blocker but are still receiving this message, make sure your browser's tracking protection is set to the 'standard' level.

Biotech / Medical : Millennium Pharmaceuticals, Inc. (MLNM)

Public Reply Prvt Reply Mark as Last Read File

Previous 10 Next 10 Previous Next

From: Icebrg	10/25/2007 11:14:49 AM
	of 3044

Antimalarial activity of the anticancer and proteasome inhibitor bortezomib and its analog ZL3B. Reynolds JM, El Bissati K, Brandenburg J, Gunzl A, Ben Mamoun C. BMC Clin Pharmacol. 2007 Oct 23;7(1):13 ABSTRACT: BACKGROUND: The high rate of mortality due to malaria and the worldwide distribution of parasite resistance to the commonly used antimalarial drugs chloroquine and pyrimethamine emphasize the urgent need for the development of new antimalarial drugs. An alternative approach to the long and uncertain process of designing and developing new compounds is to identify among the armamentarium of drugs already approved for clinical treatment of various human diseases those that may have strong antimalarial activity. METHODS: Proteasome inhibitor bortezomib (VelcadeTM: [(1R)-3-methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(pyrazinylcarbonyl) amino]propyl]amino]butyl] boronic acid), which has been approved for treatment of patients with multiple myeloma, and a second boronate analog Z-Leu-Leu-Leu-B(OH)2 (ZL3B), were tested against four different strains of P. falciparum (3D7, HB3, W2 and Dd2) that are either sensitive or have different levels of resistance to the antimalarial drugs pyrimethamine and chloroquine. RESULTS: Bortezomib and ZL3B are equally effective against drug-sensitive and -resistant parasites and block intraerythrocytic development prior to DNA synthesis, but have no effect on parasite egress or invasion. CONCLUSION: The identification of bortezomib and its analog as potent antimalarial drugs will set the stage for the advancement of this class of compounds alone or in combination therapy for treatment of malaria, and emphasize the need for large-scale screens to identify new antimalarials within the library of clinically approved compounds.

Report TOU Violation

Share This Post

Public Reply Prvt Reply Mark as Last Read File

Previous 10 Next 10 Previous Next