Synthesis and bioactivity of a Goralatide analog with antileukemic activity

Zhiliang Li; Iryna Oleksandrivna Lebedyeva; Vita M. Golubovskaya; William G. Cance; Khalid A. Alamry; Hassan M. Faidallah; C. Dennis Hall; Alan R. Katritzky

doi:10.1016/j.bmc.2015.04.061

Synthesis and bioactivity of a Goralatide analog with antileukemic activity

Zhiliang Li, Iryna Oleksandrivna Lebedyeva, Vita M. Golubovskaya, William G. Cance, Khalid A. Alamry, Hassan M. Faidallah, C. Dennis Hall, Alan R. Katritzky

Research output: Contribution to journal › Article › peer-review

1 Scopus citations

Abstract

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.

Original language	English (US)
Pages (from-to)	5056-5060
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry
Volume	23
Issue number	15
DOIs	https://doi.org/10.1016/j.bmc.2015.04.061
State	Published - Jul 23 2015

Keywords

Anticancer
Antileukemic
Goralatide
Peptide
Peptidomimetic

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmc.2015.04.061

Cite this

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abstract = "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.",

keywords = "Anticancer, Antileukemic, Goralatide, Peptide, Peptidomimetic",

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T1 - Synthesis and bioactivity of a Goralatide analog with antileukemic activity

AU - Li, Zhiliang

AU - Lebedyeva, Iryna Oleksandrivna

AU - Golubovskaya, Vita M.

AU - Cance, William G.

AU - Alamry, Khalid A.

AU - Faidallah, Hassan M.

AU - Dennis Hall, C.

AU - Katritzky, Alan R.

PY - 2015/7/23

Y1 - 2015/7/23

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AB - 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.

KW - Anticancer

KW - Antileukemic

KW - Goralatide

KW - Peptide

KW - Peptidomimetic

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Synthesis and bioactivity of a Goralatide analog with antileukemic activity

Abstract

Keywords

ASJC Scopus subject areas

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