Novel Blocker of Onco SK3 Channels Derived from Scorpion Toxin Tamapin and Active against Migration of Cancer Cells

Marlen Mayorga-Flores; Aurélie Chantôme; Carolina Monserrath Melchor-Meneses; Isabelle Domingo; Gustavo Alfredo Titaux-Delgado; Rodrigo Galindo-Murillo; Christophe Vandier; Federico Del Río-Portilla

doi:10.1021/acsmedchemlett.0c00300

Novel Blocker of Onco SK3 Channels Derived from Scorpion Toxin Tamapin and Active against Migration of Cancer Cells

Marlen Mayorga-Flores, Aurélie Chantôme, Carolina Monserrath Melchor-Meneses, Isabelle Domingo, Gustavo Alfredo Titaux-Delgado, Rodrigo Galindo-Murillo, Christophe Vandier, Federico Del Río-Portilla

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

10 Scopus citations

Abstract

Peptide-based therapy against cancer is a field of great interest for biomedical developments. Since it was shown that SK3 channels promote cancer cell migration and metastatic development, we started using these channels as targets for the development of antimetastatic drugs. Particularly, tamapin (a peptide found in the venom of the scorpion Mesobuthus tamulus) is the most specific toxin against the SK2 channel currently known. Considering this fact, we designed diverse tamapin mutants based on three different hypotheses to discover a new potent molecule to block SK3 channels. We performed in vitro studies to evaluate this new toxin derivative inhibitor of cancer cell migration. Our results can be used to generate a new tamapin-based therapy against cancer cells that express SK3 channels.

Original language	English (US)
Pages (from-to)	1627-1633
Number of pages	7
Journal	ACS Medicinal Chemistry Letters
Volume	11
Issue number	8
DOIs	https://doi.org/10.1021/acsmedchemlett.0c00300
State	Published - Aug 13 2020
Externally published	Yes

Keywords

MDA-MB-435s
SK2 channels
SK3 channels
migration cells
scorpion toxins
tamapin

ASJC Scopus subject areas

Biochemistry
Drug Discovery
Organic Chemistry

Access to Document

10.1021/acsmedchemlett.0c00300

Cite this

Mayorga-Flores, M., Chantôme, A., Melchor-Meneses, C. M., Domingo, I., Titaux-Delgado, G. A., Galindo-Murillo, R., Vandier, C., & Del Río-Portilla, F. (2020). Novel Blocker of Onco SK3 Channels Derived from Scorpion Toxin Tamapin and Active against Migration of Cancer Cells. ACS Medicinal Chemistry Letters, 11(8), 1627-1633. https://doi.org/10.1021/acsmedchemlett.0c00300

Mayorga-Flores, M, Chantôme, A, Melchor-Meneses, CM, Domingo, I, Titaux-Delgado, GA, Galindo-Murillo, R, Vandier, C & Del Río-Portilla, F 2020, 'Novel Blocker of Onco SK3 Channels Derived from Scorpion Toxin Tamapin and Active against Migration of Cancer Cells', ACS Medicinal Chemistry Letters, vol. 11, no. 8, pp. 1627-1633. https://doi.org/10.1021/acsmedchemlett.0c00300

@article{336765ee0b8943c3b901a9037b4e7281,

title = "Novel Blocker of Onco SK3 Channels Derived from Scorpion Toxin Tamapin and Active against Migration of Cancer Cells",

abstract = "Peptide-based therapy against cancer is a field of great interest for biomedical developments. Since it was shown that SK3 channels promote cancer cell migration and metastatic development, we started using these channels as targets for the development of antimetastatic drugs. Particularly, tamapin (a peptide found in the venom of the scorpion Mesobuthus tamulus) is the most specific toxin against the SK2 channel currently known. Considering this fact, we designed diverse tamapin mutants based on three different hypotheses to discover a new potent molecule to block SK3 channels. We performed in vitro studies to evaluate this new toxin derivative inhibitor of cancer cell migration. Our results can be used to generate a new tamapin-based therapy against cancer cells that express SK3 channels.",

keywords = "MDA-MB-435s, SK2 channels, SK3 channels, migration cells, scorpion toxins, tamapin",

author = "Marlen Mayorga-Flores and Aur{\'e}lie Chant{\^o}me and Melchor-Meneses, {Carolina Monserrath} and Isabelle Domingo and Titaux-Delgado, {Gustavo Alfredo} and Rodrigo Galindo-Murillo and Christophe Vandier and {Del R{\'i}o-Portilla}, Federico",

note = "Publisher Copyright: Copyright {\textcopyright} 2020 American Chemical Society.",

year = "2020",

month = aug,

day = "13",

doi = "10.1021/acsmedchemlett.0c00300",

language = "English (US)",

volume = "11",

pages = "1627--1633",

journal = "ACS Medicinal Chemistry Letters",

issn = "1948-5875",

publisher = "American Chemical Society",

number = "8",

}

TY - JOUR

T1 - Novel Blocker of Onco SK3 Channels Derived from Scorpion Toxin Tamapin and Active against Migration of Cancer Cells

AU - Mayorga-Flores, Marlen

AU - Chantôme, Aurélie

AU - Melchor-Meneses, Carolina Monserrath

AU - Domingo, Isabelle

AU - Titaux-Delgado, Gustavo Alfredo

AU - Galindo-Murillo, Rodrigo

AU - Vandier, Christophe

AU - Del Río-Portilla, Federico

PY - 2020/8/13

Y1 - 2020/8/13

N2 - Peptide-based therapy against cancer is a field of great interest for biomedical developments. Since it was shown that SK3 channels promote cancer cell migration and metastatic development, we started using these channels as targets for the development of antimetastatic drugs. Particularly, tamapin (a peptide found in the venom of the scorpion Mesobuthus tamulus) is the most specific toxin against the SK2 channel currently known. Considering this fact, we designed diverse tamapin mutants based on three different hypotheses to discover a new potent molecule to block SK3 channels. We performed in vitro studies to evaluate this new toxin derivative inhibitor of cancer cell migration. Our results can be used to generate a new tamapin-based therapy against cancer cells that express SK3 channels.

AB - Peptide-based therapy against cancer is a field of great interest for biomedical developments. Since it was shown that SK3 channels promote cancer cell migration and metastatic development, we started using these channels as targets for the development of antimetastatic drugs. Particularly, tamapin (a peptide found in the venom of the scorpion Mesobuthus tamulus) is the most specific toxin against the SK2 channel currently known. Considering this fact, we designed diverse tamapin mutants based on three different hypotheses to discover a new potent molecule to block SK3 channels. We performed in vitro studies to evaluate this new toxin derivative inhibitor of cancer cell migration. Our results can be used to generate a new tamapin-based therapy against cancer cells that express SK3 channels.

KW - MDA-MB-435s

KW - SK2 channels

KW - SK3 channels

KW - migration cells

KW - scorpion toxins

KW - tamapin

UR - http://www.scopus.com/inward/record.url?scp=85092273359&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=85092273359&partnerID=8YFLogxK

U2 - 10.1021/acsmedchemlett.0c00300

DO - 10.1021/acsmedchemlett.0c00300

M3 - Article

C2 - 32832033

AN - SCOPUS:85092273359

SN - 1948-5875

VL - 11

SP - 1627

EP - 1633

JO - ACS Medicinal Chemistry Letters

JF - ACS Medicinal Chemistry Letters

IS - 8

ER -

Novel Blocker of Onco SK3 Channels Derived from Scorpion Toxin Tamapin and Active against Migration of Cancer Cells

Abstract

Keywords

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this