MaghrebDataLibMedV2, Main, Exploration, bibRecord, 000470

Targeting prohibitin with small molecules to promote melanogenesis and apoptosis in melanoma cells.

Identifieur interne : 000470 ( Main/Exploration ); précédent : 000469; suivant : 000471

Targeting prohibitin with small molecules to promote melanogenesis and apoptosis in melanoma cells.

Auteurs : Amel Djehal [Algérie] ; Mohammad Krayem [Belgique] ; Ahmad Najem [Belgique] ; Hassan Hammoud [France] ; Thierry Cresteil [France] ; Canan G. Nebigil [France] ; Dong Wang [République populaire de Chine] ; Peng Yu [République populaire de Chine] ; Embarek Bentouhami [Algérie] ; Ghanem E. Ghanem [Belgique] ; Laurent Désaubry [République populaire de Chine]

Source :

European journal of medicinal chemistry [ 1768-3254 ] ; 2018.

RBID : pubmed:29960207

Descripteurs français

KwdFr :
- Antinéoplasiques (composition chimique), Antinéoplasiques (pharmacologie), Apoptose (effets des médicaments et des substances chimiques), Bibliothèques de petites molécules (composition chimique), Bibliothèques de petites molécules (pharmacologie), Cellules cancéreuses en culture (MeSH), Humains (MeSH), Mélanocytes (effets des médicaments et des substances chimiques), Mélanome (anatomopathologie), Mélanome (traitement médicamenteux), Prolifération cellulaire (effets des médicaments et des substances chimiques), Protéines de répression (composition chimique), Protéines de répression (pharmacologie), Relation dose-effet des médicaments (MeSH), Relation structure-activité (MeSH), Structure moléculaire (MeSH), Tests de criblage d'agents antitumoraux (MeSH).
MESH :
- anatomopathologie : Mélanome.
- composition chimique : Antinéoplasiques, Bibliothèques de petites molécules, Protéines de répression.
- effets des médicaments et des substances chimiques : Apoptose, Mélanocytes, Prolifération cellulaire.
- pharmacologie : Antinéoplasiques, Bibliothèques de petites molécules, Protéines de répression.
- traitement médicamenteux : Mélanome.
- Cellules cancéreuses en culture, Humains, Relation dose-effet des médicaments, Relation structure-activité, Structure moléculaire, Tests de criblage d'agents antitumoraux.

English descriptors

KwdEn :
- Antineoplastic Agents (chemistry), Antineoplastic Agents (pharmacology), Apoptosis (drug effects), Cell Proliferation (drug effects), Dose-Response Relationship, Drug (MeSH), Drug Screening Assays, Antitumor (MeSH), Humans (MeSH), Melanocytes (drug effects), Melanoma (drug therapy), Melanoma (pathology), Molecular Structure (MeSH), Repressor Proteins (chemistry), Repressor Proteins (pharmacology), Small Molecule Libraries (chemistry), Small Molecule Libraries (pharmacology), Structure-Activity Relationship (MeSH), Tumor Cells, Cultured (MeSH).
MESH :
- chemical , chemistry : Antineoplastic Agents, Repressor Proteins, Small Molecule Libraries.
- chemical , pharmacology : Antineoplastic Agents, Repressor Proteins, Small Molecule Libraries.
- drug effects : Apoptosis, Cell Proliferation, Melanocytes.
- drug therapy : Melanoma.
- pathology : Melanoma.
- Dose-Response Relationship, Drug, Drug Screening Assays, Antitumor, Humans, Molecular Structure, Structure-Activity Relationship, Tumor Cells, Cultured.

Abstract

Prohibitins 1 and 2 (PHB1/2) are scaffold proteins that are involved in both melanogenesis and oncogenic pathways. We hypothesized that a PHB1 ligand, melanogenin, may display anti-cancer effects in addition to its known melanogenic activity in melanocytes. Here, we disclose a convenient synthesis of melanogenin, and its analogs. We found that, among 57 new melanogenin analogs, two (Mel9 and Mel41) significantly promoted both melanogenesis in melanocytes by activating one of the PHB2-interacting proteins, microtubule-associated protein light chain 3 (LC3), and upregulating the expression of microphthalmia associated transcription factor (MITF). These analogs also activate ERK. Besides, in addition to their promelanogenic activities, we uncovered that melanogenin and its active analogs induce apoptosis in several cancer cell lines, including melanoma cells, and that this effect is caused by an inhibition of AKT survival pathway. Our findings present a new putative function for PHBs as regulators of LC3/ERK/MITF melanogenic signaling, and suggest that Mel9 and Mel41 may provide the basis for the development of new drugs candidates to treat melanoma and other types of cancers.

DOI: 10.1016/j.ejmech.2018.06.052
PubMed: 29960207

Affiliations:

Links toward previous steps (curation, corpus...)

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Le document en format XML

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<author><name sortKey="Bentouhami, Embarek" sort="Bentouhami, Embarek" uniqKey="Bentouhami E" first="Embarek" last="Bentouhami">Embarek Bentouhami</name>
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<country xml:lang="fr">Algérie</country>
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<author><name sortKey="Ghanem, Ghanem E" sort="Ghanem, Ghanem E" uniqKey="Ghanem G" first="Ghanem E" last="Ghanem">Ghanem E. Ghanem</name>
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<author><name sortKey="Desaubry, Laurent" sort="Desaubry, Laurent" uniqKey="Desaubry L" first="Laurent" last="Désaubry">Laurent Désaubry</name>
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<profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Antineoplastic Agents (chemistry)</term>
<term>Antineoplastic Agents (pharmacology)</term>
<term>Apoptosis (drug effects)</term>
<term>Cell Proliferation (drug effects)</term>
<term>Dose-Response Relationship, Drug (MeSH)</term>
<term>Drug Screening Assays, Antitumor (MeSH)</term>
<term>Humans (MeSH)</term>
<term>Melanocytes (drug effects)</term>
<term>Melanoma (drug therapy)</term>
<term>Melanoma (pathology)</term>
<term>Molecular Structure (MeSH)</term>
<term>Repressor Proteins (chemistry)</term>
<term>Repressor Proteins (pharmacology)</term>
<term>Small Molecule Libraries (chemistry)</term>
<term>Small Molecule Libraries (pharmacology)</term>
<term>Structure-Activity Relationship (MeSH)</term>
<term>Tumor Cells, Cultured (MeSH)</term>
</keywords>
<keywords scheme="KwdFr" xml:lang="fr"><term>Antinéoplasiques (composition chimique)</term>
<term>Antinéoplasiques (pharmacologie)</term>
<term>Apoptose (effets des médicaments et des substances chimiques)</term>
<term>Bibliothèques de petites molécules (composition chimique)</term>
<term>Bibliothèques de petites molécules (pharmacologie)</term>
<term>Cellules cancéreuses en culture (MeSH)</term>
<term>Humains (MeSH)</term>
<term>Mélanocytes (effets des médicaments et des substances chimiques)</term>
<term>Mélanome (anatomopathologie)</term>
<term>Mélanome (traitement médicamenteux)</term>
<term>Prolifération cellulaire (effets des médicaments et des substances chimiques)</term>
<term>Protéines de répression (composition chimique)</term>
<term>Protéines de répression (pharmacologie)</term>
<term>Relation dose-effet des médicaments (MeSH)</term>
<term>Relation structure-activité (MeSH)</term>
<term>Structure moléculaire (MeSH)</term>
<term>Tests de criblage d'agents antitumoraux (MeSH)</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Antineoplastic Agents</term>
<term>Repressor Proteins</term>
<term>Small Molecule Libraries</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Antineoplastic Agents</term>
<term>Repressor Proteins</term>
<term>Small Molecule Libraries</term>
</keywords>
<keywords scheme="MESH" qualifier="anatomopathologie" xml:lang="fr"><term>Mélanome</term>
</keywords>
<keywords scheme="MESH" qualifier="composition chimique" xml:lang="fr"><term>Antinéoplasiques</term>
<term>Bibliothèques de petites molécules</term>
<term>Protéines de répression</term>
</keywords>
<keywords scheme="MESH" qualifier="drug effects" xml:lang="en"><term>Apoptosis</term>
<term>Cell Proliferation</term>
<term>Melanocytes</term>
</keywords>
<keywords scheme="MESH" qualifier="drug therapy" xml:lang="en"><term>Melanoma</term>
</keywords>
<keywords scheme="MESH" qualifier="effets des médicaments et des substances chimiques" xml:lang="fr"><term>Apoptose</term>
<term>Mélanocytes</term>
<term>Prolifération cellulaire</term>
</keywords>
<keywords scheme="MESH" qualifier="pathology" xml:lang="en"><term>Melanoma</term>
</keywords>
<keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Antinéoplasiques</term>
<term>Bibliothèques de petites molécules</term>
<term>Protéines de répression</term>
</keywords>
<keywords scheme="MESH" qualifier="traitement médicamenteux" xml:lang="fr"><term>Mélanome</term>
</keywords>
<keywords scheme="MESH" xml:lang="en"><term>Dose-Response Relationship, Drug</term>
<term>Drug Screening Assays, Antitumor</term>
<term>Humans</term>
<term>Molecular Structure</term>
<term>Structure-Activity Relationship</term>
<term>Tumor Cells, Cultured</term>
</keywords>
<keywords scheme="MESH" xml:lang="fr"><term>Cellules cancéreuses en culture</term>
<term>Humains</term>
<term>Relation dose-effet des médicaments</term>
<term>Relation structure-activité</term>
<term>Structure moléculaire</term>
<term>Tests de criblage d'agents antitumoraux</term>
</keywords>
</textClass>
</profileDesc>
</teiHeader>
<front><div type="abstract" xml:lang="en">Prohibitins 1 and 2 (PHB1/2) are scaffold proteins that are involved in both melanogenesis and oncogenic pathways. We hypothesized that a PHB1 ligand, melanogenin, may display anti-cancer effects in addition to its known melanogenic activity in melanocytes. Here, we disclose a convenient synthesis of melanogenin, and its analogs. We found that, among 57 new melanogenin analogs, two (Mel9 and Mel41) significantly promoted both melanogenesis in melanocytes by activating one of the PHB2-interacting proteins, microtubule-associated protein light chain 3 (LC3), and upregulating the expression of microphthalmia associated transcription factor (MITF). These analogs also activate ERK. Besides, in addition to their promelanogenic activities, we uncovered that melanogenin and its active analogs induce apoptosis in several cancer cell lines, including melanoma cells, and that this effect is caused by an inhibition of AKT survival pathway. Our findings present a new putative function for PHBs as regulators of LC3/ERK/MITF melanogenic signaling, and suggest that Mel9 and Mel41 may provide the basis for the development of new drugs candidates to treat melanoma and other types of cancers.</div>
</front>
</TEI>
<affiliations><list><country><li>Algérie</li>
<li>Belgique</li>
<li>France</li>
<li>République populaire de Chine</li>
</country>
<region><li>Région de Bruxelles-Capitale</li>
<li>Île-de-France</li>
</region>
<settlement><li>Bruxelles</li>
<li>Chatenay-Malabry</li>
<li>Paris</li>
<li>Tianjin</li>
</settlement>
<orgName><li>Université Paris-Sud</li>
<li>Université libre de Bruxelles</li>
</orgName>
</list>
<tree><country name="Algérie"><noRegion><name sortKey="Djehal, Amel" sort="Djehal, Amel" uniqKey="Djehal A" first="Amel" last="Djehal">Amel Djehal</name>
</noRegion>
<name sortKey="Bentouhami, Embarek" sort="Bentouhami, Embarek" uniqKey="Bentouhami E" first="Embarek" last="Bentouhami">Embarek Bentouhami</name>
</country>
<country name="Belgique"><region name="Région de Bruxelles-Capitale"><name sortKey="Krayem, Mohammad" sort="Krayem, Mohammad" uniqKey="Krayem M" first="Mohammad" last="Krayem">Mohammad Krayem</name>
</region>
<name sortKey="Ghanem, Ghanem E" sort="Ghanem, Ghanem E" uniqKey="Ghanem G" first="Ghanem E" last="Ghanem">Ghanem E. Ghanem</name>
<name sortKey="Najem, Ahmad" sort="Najem, Ahmad" uniqKey="Najem A" first="Ahmad" last="Najem">Ahmad Najem</name>
</country>
<country name="France"><noRegion><name sortKey="Hammoud, Hassan" sort="Hammoud, Hassan" uniqKey="Hammoud H" first="Hassan" last="Hammoud">Hassan Hammoud</name>
</noRegion>
<name sortKey="Cresteil, Thierry" sort="Cresteil, Thierry" uniqKey="Cresteil T" first="Thierry" last="Cresteil">Thierry Cresteil</name>
<name sortKey="Nebigil, Canan G" sort="Nebigil, Canan G" uniqKey="Nebigil C" first="Canan G" last="Nebigil">Canan G. Nebigil</name>
</country>
<country name="République populaire de Chine"><noRegion><name sortKey="Wang, Dong" sort="Wang, Dong" uniqKey="Wang D" first="Dong" last="Wang">Dong Wang</name>
</noRegion>
<name sortKey="Desaubry, Laurent" sort="Desaubry, Laurent" uniqKey="Desaubry L" first="Laurent" last="Désaubry">Laurent Désaubry</name>
<name sortKey="Yu, Peng" sort="Yu, Peng" uniqKey="Yu P" first="Peng" last="Yu">Peng Yu</name>
</country>
</tree>
</affiliations>
</record>

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Targeting prohibitin with small molecules to promote melanogenesis and apoptosis in melanoma cells.

Targeting prohibitin with small molecules to promote melanogenesis and apoptosis in melanoma cells.

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