68280-76-2Relevant academic research and scientific papers
Synthesis and bioactivity of a Goralatide analog with antileukemic activity
Li, Zhiliang,Lebedyeva, Iryna O.,Golubovskaya, Vita M.,Cance, William G.,Alamry, Khalid A.,Faidallah, Hassan M.,Dennis Hall,Katritzky, Alan R.
, p. 5056 - 5060 (2015/08/03)
Natural tetrapeptide Goralatide (AcSDKP) is a selective inhibitor of primitive haematopoietic cell proliferation. It is not stable in vivo and decomposes within 4.5 min when applied to live cells. In this work we developed an analog of Goralatide that exhibits cytotoxicity towards human myeloid HL-60, HEL, Nalm-6 leukemia cells, endothelial HUVEC, glioblastoma U251 and transformed kidney 293T cells. The Goralatide analog showed significant stability in organic solution with no tendency to degrade oxidatively.
NAcSDKP analogues resistant to angiotensin-converting enzyme
Gaudron,Adeline,Potier,Thierry
, p. 3963 - 3968 (2007/10/03)
Two series of analogues of the tetrapeptide NAcSDKP, an inhibitor of hematopoietic stem cell proliferation, were prepared, and their enzymatic stability toward rabbit lung angiotensin-converting enzyme (ACE) was evaluated as well as their capacity to inhibit NAcSDKP hydrolysis by this enzyme. In the first series, each of the peptide bonds has been successively replaced by an aminomethylene bond. In the second one, the C-terminus of the peptide has been modified by decarboxylation or amidation. The results reported here indicate that all of these molecules but one have good stability toward the enzyme but none of the compounds is able to inhibit NAcSDKP hydrolysis by ACE.
Synthesis and activity of NAcSerAspLysPro analogues on cellular interactions between T-cell and erythrocytes in rosette formation
Thierry,Papet,Saez-Servent,Plissonneau-Haumont,Potier,Lenfant
, p. 2122 - 2127 (2007/10/02)
Analogues of NAcSerAspLysPro (AcSDKP), a natural regulator of hematopoiesis isolated from fetal calf bone marrow, were synthesized. The biological activity of these molecules were evaluated in vitro in the rosette assay, which measures the interaction bet
