Protein Information

Name ubiquitin
Synonyms HMG20; RPS27A; UBA80; UBCEP 1; UBCEP1; UBA52; UBCEP 2; UBCEP2…

Compound Information

Name piperazine
CAS piperazine

Reference List

PubMed Abstract RScore(About this table)
15708793 Nguewa PA, Fuertes MA, Iborra S, Najajreh Y, Gibson D, Martinez E, Alonso C, Perez JM: Water soluble cationic trans-platinum complexes which induce programmed cell death in the protozoan parasite Leishmania infantum. J Inorg Biochem. 2005 Mar;99(3):727-36. Epub 2005 Jan 1.

We have evaluated the cytotoxic properties against the protozoan Leishmania infantum of four water soluble cationic trans-Pt (II) Cl (2) compounds containing as inert groups NH3 and piperazine (1), 4-picoline and piperazine (2), n-butylamine and piperazine (3), and NH3 and 4-piperidino-piperidine (4).
Similarly to cis-diamminedichloroplatinum (II) and trans-diamminedichloroplatinum (II), the interaction of compounds 3 and 4 with ubiquitin results in an increase of the alpha-helix content of the protein as observed by circular dichroism spectroscopy.
2(0,0,0,2) Details
12459912 Najajreh Y, Peleg-Shulman T, Moshel O, Farrell N, Gibson D: Ligand effects on the binding of cis- and trans-[PtCl (2) Am (1) Am (2)] to proteins. J Biol Inorg Chem. 2003 Jan;8(1-2):167-75. Epub 2002 Sep 25.

As part of a systematic study of the basic principles that govern the formation and reactivity of Pt-protein adducts, we report the effect of substituting the amine ligand of cis- and trans-[PtCl (2)(NH (3))(2)] complexes with bulkier planar aromatic or nonplanar cyclic amine ligands on the binding properties of the complexes to ubiquitin and to horse heart myoglobin.
The introduction of a charged piperazine ligand significantly decreased the rate of binding to the protein, possibly owing to electrostatic interactions or hydrogen-bond formations with the surface of the protein.
1(0,0,0,1) Details
12431046 Najajreh Y, Perez JM, Navarro-Ranninger C, Gibson D: Novel soluble cationic trans-diaminedichloroplatinum (II) complexes that are active against cisplatin resistant ovarian cancer cell lines. J Med Chem. 2002 Nov 21;45(24):5189-95.

The platinum-piperazine complexes bind proteins (ubiquitin and myoglobin) very slowly as compared to cisplatin and to their neutral piperidine analogues.
81(1,1,1,1) Details
17982703 Yu Z, Wang F, Milacic V, Li X, Cui QC, Zhang B, Yan B, Dou QP: Evaluation of copper-dependent proteasome-inhibitory and apoptosis-inducing activities of novel pyrrolidine dithiocarbamate analogues. Int J Mol Med. 2007 Dec;20(6):919-25.

One of the most important strategies to regulate apoptosis is via the ubiquitin-proteasome pathway.
However, after the pyrrolidine ring was substituted with morpholine, the activity of the mixtures slightly decreased but was completely lost when piperazine with the attached ethyl group was used for the substitution.
1(0,0,0,1) Details