Genomes and Genes
Doron C Greenbaum
Affiliation: University of California
- A role for the protease falcipain 1 in host cell invasion by the human malaria parasiteDoron C Greenbaum
Department of Pharmaceutical Chemistry, Veterans Affairs Medical Center, University of California, San Francisco, CA 94143, USA
Science 298:2002-6. 2002..These results demonstrate a specific role for falcipain 1 in host cell invasion and establish a potential new target for antimalarial therapeutics...
- A cathepsin B-like protease is required for host protein degradation in Trypanosoma bruceiZachary B Mackey
Department of Pathology Tropical Disease Research Unit, University of California, San Francisco, California 94143, USA
J Biol Chem 279:48426-33. 2004..Therefore, tbcatB, but not rhodesain, is essential for T. brucei survival in culture and is the most likely target of the diazomethane protease inhibitor Z-Phe-Ala-CHN(2) in T. brucei...
- Substrate profiling of cysteine proteases using a combinatorial peptide library identifies functionally unique specificitiesYoungchool Choe
Department of Pharmaceutical Chemistry, University of California at San Francisco, California 94143, USA
J Biol Chem 281:12824-32. 2006..This approach provides useful information for developing selective chemical probes to study protease-related pathologies and physiologies...
- The Trypanosoma cruzi protease cruzain mediates immune evasionPatricia S Doyle
Tropical Disease Research Unit and Sandler Center for Drug Discovery, Department of Pathology, University of California, San Francisco, California, United States of America
PLoS Pathog 7:e1002139. 2011..These early events allow T. cruzi survival and replication, and may lead to the spread of infection in acute Chagas' disease...
- Synthesis and structure-activity relationships of parasiticidal thiosemicarbazone cysteine protease inhibitors against Plasmodium falciparum, Trypanosoma brucei, and Trypanosoma cruziDoron C Greenbaum
Sandler Center for Basic Research in Parasitic Diseases, Department of Pathology, University of California San Francisco, San Francisco, CA 94143, USA
J Med Chem 47:3212-9. 2004..Our results suggest that thiosemicarbazones represent validated drug leads that kill several species of protozoan parasites through the inhibition of cysteine proteases as well as other novel targets...
- Small molecule affinity fingerprinting. A tool for enzyme family subclassification, target identification, and inhibitor designDoron C Greenbaum
Department of Pharmaceutical Chemistry, San Francisco, CA 94143, USA
Chem Biol 9:1085-94. 2002..This method could ultimately be used with large enzyme families to aid in the design of selective inhibitors of targets based on limited structural/function information...
- Targeted disruption of Plasmodium falciparum cysteine protease, falcipain 1, reduces oocyst production, not erythrocytic stage growthSaliha Eksi
Department of Biology, Loyola University Chicago, 6525 North Sheridan Rd, Chicago, IL 60626, USA
Mol Microbiol 53:243-50. 2004..However, when falcipain 1 minus parasites were fed to a mosquito, oocyst production was reduced by 70-90%, suggesting an important role for falcipain 1 during parasite development in the mosquito midgut...
- Distinct protein classes including novel merozoite surface antigens in Raft-like membranes of Plasmodium falciparumPaul R Sanders
The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3050 Australia
J Biol Chem 280:40169-76. 2005..This insight into merozoite surfaces provides new opportunities for understanding both erythrocyte invasion and anti-parasite immunity...
- Cathepsin cysteine proteases are effectors of invasive growth and angiogenesis during multistage tumorigenesisJohanna A Joyce
Department of Biochemistry and Biophysics, Diabetes and Comprehensive Cancer Centers, University of California at San Francisco, 94143, USA
Cancer Cell 5:443-53. 2004..Cysteine cathepsins are also upregulated during HPV16-induced cervical carcinogenesis, further encouraging consideration of this protease family as a therapeutic target in human cancers...
- Identification of protein complexes in detergent-resistant membranes of Plasmodium falciparum schizontsPaul R Sanders
The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Melbourne, VIC 3050, Australia
Mol Biochem Parasitol 154:148-57. 2007..Confirmation of MSP-1 oligomerization, together with the isolation of a number of known complexes by BN-PAGE, makes it highly likely that novel interactions occur amongst members of this proteome...
- Is chemical genetics the new frontier for malaria biology?Doron C Greenbaum
Department of Pharmacology, School of Medicine, University of Pennsylvania, PA 19104, USA
Trends Pharmacol Sci 29:51-6. 2008..Unfortunately, standard genetics techniques are limited in scope because of low transfection efficiency and a lack of knockdown techniques, thereby rendering the analysis of essential genes difficult...