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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
*Corresponding author for this work
  • University of Florida
    ,
  • Roswell Park Cancer Institute
    ,
  • King Abdulaziz University
Scholary 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.

Publication Information

Output type

Scholary Output:
Contribution to journal
Article
 Peer-review

Original language

English (US)

Pages from-to (Number of pages)

Pages 5056-5060 (5 pages)

Journal (Volume, Issue Number)

Bioorganic and Medicinal Chemistry (Volume 23, Issue 15)

Publication milestones

  • Published - 07/23/2015

Publication status

Published - 07/23/2015

ISSN

0968-0896

Publication IDs

  • Scopus: 84937519253
  • PubMed: 26048023

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Author count
8
SciVal
Paper percentile
23
Scopus
citations
2, opens in new tab
Fractional count
1
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0.13
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7
Fractional count
0.88
Fractional count
1
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1

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Citation count
2
Captures
10

Funding Details

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.
FundersFunding numbers
NSTIP Strategic Technologies Program
-
UF
-