Octa-O-bis-(R,R)-Tartarate Ditellurane (SAS) is a new Te(IV) compound, comprised of two tellurium atoms, each liganded by four oxygen atoms from two carboxylates and two alkoxides of two tartaric acids. Unlike many other Te(IV) compounds, SAS was highly stable in aqueous solution. It interacted with thiols to form an unstable Te(SR)(4) product. The product of the interaction of SAS with cysteine was isolated and characterized by mass spectroscopy and elemental analysis. SAS selectively inactivated cysteine proteases, but it did not inactivate other families of proteolytic enzymes. It displayed selectivity towards the cysteine protease cathepsin B, a human enzyme of pharmaceutical interest, with a second order rate constant k(i)/K(i)=5900 M(-1) s(-1).

Download full-text PDF

Source
http://dx.doi.org/10.1002/cmdc.200700155DOI Listing

Publication Analysis

Top Keywords

octa-o-bis-rr-tartarate ditellurane
8
ditellurane sas
8
sas
5
sas novel
4
novel bioactive
4
bioactive organotelluriumiv
4
organotelluriumiv compound
4
compound synthesis
4
synthesis characterization
4
characterization protease
4

Similar Publications

Inhibition of α4β1 Integrin Activity by Small Tellurium Compounds Regulates PD-L1 Expression and Enhances Antitumor Effects.

Int J Biol Sci

September 2024

C.A.I.R. Institute, The Safdiè AIDS and Immunology Research Center, The Mina & Everard Goodman Faculty of Life Sciences, Bar-Ilan University, Ramat-Gan, Israel.

Various cancer treatment approaches that inhibit the activity of the programmed death-1/programmed death-ligand 1 (PD-1/PD-L1) axis, a key player in tumor immune evasion, have been developed. We show that the immunomodulatory small tellurium complexes AS101 (ammonium trichloro(dioxoethylene-o,o')tellurate) and SAS (octa-O-bis(R,R)-tartarate ditellurane) suppress PD-L1 expression in a variety of human and mouse malignant cells via the modulation of α4β1 very late antigen- (VLA-4) integrin activity. Consequently, the expression of pAkt and its downstream effector pNFκB are inhibited.

View Article and Find Full Text PDF

Multiple Myeloma, effectively treated by chemotherapeutic drugs, relapses due to drug resistance. We tested here the capacity of mesenchymal stromal cells, from the bone marrow of patients or from adipose tissue of healthy individuals, to induce drug resistance in Myeloma cell lines. We show that drug resistance can be achieved by factors secreted by the various MSC's.

View Article and Find Full Text PDF

The study shows that treatment of NOD mice with either of two tellurium-based small molecules, AS101 [ammonium trichloro(dioxoethylene-o,o')tellurate] or SAS [octa-O-bis-(R,R)-tartarate ditellurane] could preserve β cells function and mass. These beneficial effects were reflected in decreased incidence of diabetes, improved glucose clearance, preservation of body weight, and increased survival. The normal glucose levels were associated with increased insulin levels, preservation of β cell mass and increased islet size.

View Article and Find Full Text PDF

The small tellurium-based compound SAS suppresses inflammation in human retinal pigment epithelium.

Mol Vis

November 2016

C.A.I.R. Institute, The Safdié AIDS and Immunology Research Center, The Mina & Everard Goodman Faculty of Life Sciences, Bar-Ilan University, Ramat-Gan 52900, Israel.

Article Synopsis
  • Pathological angiogenesis and chronic inflammation are key factors in the development of choroidal neovascularization (CNV) in eye diseases, prompting a study on the effects of a compound called SAS on retinal pigment epithelial (RPE) cells.
  • SAS was demonstrated to inhibit specific integrins on RPE cells, enhance the expression of protective factors such as PEDF, and significantly reduce inflammatory gene expression linked to angiogenesis when RPE cells were co-cultured with endothelial cells.
  • The findings indicate that SAS could serve as an effective anti-inflammatory treatment for chorioretinal conditions, potentially improving therapeutic strategies in managing these diseases.
View Article and Find Full Text PDF

Antibacterial effects of the tellurium compound OTD on E. coli isolates.

Arch Microbiol

January 2014

The Mina and Everard Goodman Faculty of Life Sciences, Bar-Ilan University, 5290002, Ramat Gan, Israel.

The antibacterial effects of a new organo-tellurium compound [Octa-O-bis-(R,R)-tartarate ditellurane (OTD)] on Escherichia coli isolates as a model are shown. OTD was found to be a bactericidal drug. It exhibits inhibition zones on a protein-rich agar medium but not in a protein-poor medium unless a thiol is added.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!