Aminopeptidase

A randomised evaluation of low-dose cytosine arabinoside (ara-C) plus tosedostat versus low-dose ara-C in older patients with acute myeloid leukaemia: results of the LI-1 trial

55 views | Feb 24 2023

The "Pick-a-Winner" LI-1 trial of 243 older acute myeloid leukemia (AML) patients who were not suitable for intensive treatment showed no statistically significant improvement in complete remission, overall response, or overall survival with the addition of tosedostat, a selective oral aminopeptidase inhibitor, to low-dose cytosine arabinoside. [Read the Full Post]

Aminopeptidases in Cancer, Biology and Prospects for Pharmacological Intervention

50 views | Feb 24 2023

Aminopeptidases play a crucial role in cellular processes and functions, including metabolism, signaling, angiogenesis, and immunology, and their overexpression in tumor cells can facilitate rapid proliferation, leading to potential use as a targeted approach for new oncological treatments. [Read the Full Post]

Learn about the prescription medication Methazolamide

2938 views | May 26 2013

Methazolamide is a carbonic anhydrase inhibitor with Ki of 50 nM, 14 nM and 36 nM for hCA I, hCA II and bCA IV isoforms, respectively. [Read the Full Post]

Effects of oral administration of methazolamide on intraocular pressure

2889 views | May 22 2013

In vitro characterization of the erythrocyte distribution of methazolamide: a model of erythrocyte transport and binding kinetics [Read the Full Post]

TOSEDOSTAT: INHIBITING AMINOPEPTIDASES IN CANCERS

3455 views | Mar 18 2012

AMINOPEPTIDASES AND THEIR INHIBITION: Aminopeptidases catalyze the cleavage of amino acids of proteins or peptide substrates. Such enzymes are zinc dependant and located throughout most mammalian tissue and in certain plant extracts. They are essential for many cellular maintenance functions and are release systemically from the small intestine. Since these enzymes act by hydrolysis amino acids located at the amino groups of terminal proteins inhibition of their processes would affect cell proliferation, secretion, invasion and angiogenesis. Small molecule inhibitors for the inhibition of aminopeptidases have been developed for oncological use. CHR-2797 is a pro-drug for an aminopeptidase inhibitor that is marketed by Chroma Therapeutics under the trade name of Tosedostat. Tosedostat aminopeptidase inhibitor under goes cellular modulation to the active metabolite (CHR79888) via hydrolysis of a methoxy group. This metabolite is poorly membrane permeable, resulting in cellular accumulation. In animal models Toseostad has proved to be a significant inhibitor of proliferation and has demonstrated anti-angiogenic activity. [Read the Full Post]