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

Chemistry and Physics

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

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

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title = "Synthesis and bioactivity of a Goralatide analog with antileukemic activity",

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",

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

note = "Funding Information: We thank the University of Florida for the support of this project. This project was also supported by the NSTIP Strategic Technologies Program in the Kingdom of Saudi Arabia-Project N o . 12-ADV2732-03. The authors also, acknowledge with thanks Science and Technology Unit, King Abdulaziz University for technical support. The authors are grateful to Dr. Rachel A. Jones, Mr. Z. Wang for helpful discussions and Dr. M.C.A. Dancel for HRMS analyses. Publisher Copyright: {\textcopyright} 2015 Elsevier Ltd. All rights reserved.",

year = "2015",

month = jul,

day = "23",

doi = "10.1016/j.bmc.2015.04.061",

language = "English (US)",

volume = "23",

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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.

N1 - Funding Information: We thank the University of Florida for the support of this project. This project was also supported by the NSTIP Strategic Technologies Program in the Kingdom of Saudi Arabia-Project N o . 12-ADV2732-03. The authors also, acknowledge with thanks Science and Technology Unit, King Abdulaziz University for technical support. The authors are grateful to Dr. Rachel A. Jones, Mr. Z. Wang for helpful discussions and Dr. M.C.A. Dancel for HRMS analyses. Publisher Copyright: © 2015 Elsevier Ltd. All rights reserved.

PY - 2015/7/23

Y1 - 2015/7/23

N2 - 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.

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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ER -

Synthesis and bioactivity of a Goralatide analog with antileukemic activity

Abstract

Keywords

ASJC Scopus subject areas

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