5-Nitro-5'-hydroxy-indirubin-3'-oxime (AGM130), an indirubin-3'-oxime derivative, inhibits tumor growth by inducing apoptosis against non-small cell lung cancer in vitro and in vivo.
Identifieur interne : 000F12 ( Main/Exploration ); précédent : 000F11; suivant : 000F135-Nitro-5'-hydroxy-indirubin-3'-oxime (AGM130), an indirubin-3'-oxime derivative, inhibits tumor growth by inducing apoptosis against non-small cell lung cancer in vitro and in vivo.
Auteurs : Mee-Young Ahn [Corée du Sud] ; Tae-Hyung Kim [Corée du Sud] ; Seong-Min Kwon [Corée du Sud] ; Hyo-Eun Yoon [Corée du Sud] ; Hyung-Sik Kim [Corée du Sud] ; Jae-Il Kim [Corée du Sud] ; Yong-Chul Kim [Corée du Sud] ; Keon-Wook Kang [Corée du Sud] ; Sang-Gun Ahn [Corée du Sud] ; Jung-Hoon Yoon [Corée du Sud]Source :
- European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences [ 1879-0720 ] ; 2015.
Descripteurs français
- KwdFr :
- Animaux, Antinéoplasiques (usage thérapeutique), Apoptose, Carcinome pulmonaire non à petites cellules (traitement médicamenteux), Cycle cellulaire (), Humains, Indoles (pharmacologie), Indoles (usage thérapeutique), Lignée cellulaire tumorale, Mâle, Oximes (pharmacologie), Oximes (usage thérapeutique), Protéine oncogène v-akt (antagonistes et inhibiteurs), Récepteurs des somatomédines (antagonistes et inhibiteurs), Souris, Souris nude, Système de signalisation des MAP kinases (), Transplantation tumorale, Tumeurs du poumon (traitement médicamenteux).
- MESH :
- antagonistes et inhibiteurs : Protéine oncogène v-akt, Récepteurs des somatomédines.
- pharmacologie : Indoles, Oximes.
- traitement médicamenteux : Carcinome pulmonaire non à petites cellules, Tumeurs du poumon.
- usage thérapeutique : Antinéoplasiques, Indoles, Oximes.
- Animaux, Apoptose, Cycle cellulaire, Humains, Lignée cellulaire tumorale, Mâle, Souris, Souris nude, Système de signalisation des MAP kinases, Transplantation tumorale.
English descriptors
- KwdEn :
- Animals, Antineoplastic Agents (therapeutic use), Apoptosis, Carcinoma, Non-Small-Cell Lung (drug therapy), Cell Cycle (drug effects), Cell Line, Tumor, Humans, Indoles (pharmacology), Indoles (therapeutic use), Lung Neoplasms (drug therapy), MAP Kinase Signaling System (drug effects), Male, Mice, Mice, Nude, Neoplasm Transplantation, Oncogene Protein v-akt (antagonists & inhibitors), Oximes (pharmacology), Oximes (therapeutic use), Receptors, Somatomedin (antagonists & inhibitors).
- MESH :
- chemical , antagonists & inhibitors : Oncogene Protein v-akt, Receptors, Somatomedin.
- chemical , pharmacology : Indoles, Oximes.
- chemical , therapeutic use : Antineoplastic Agents, Indoles, Oximes.
- drug effects : Cell Cycle, MAP Kinase Signaling System.
- drug therapy : Carcinoma, Non-Small-Cell Lung, Lung Neoplasms.
- Animals, Apoptosis, Cell Line, Tumor, Humans, Male, Mice, Mice, Nude, Neoplasm Transplantation.
Abstract
This study examined the anti-tumor effects of AGM130, a novel indirubin-3'-oxime derivative in A549 human non-small cell lung cancer cells. AGM130 significantly inhibited the proliferation and arrested the cell cycle of G2/M phase. Induction of apoptosis was detected in AGM130-treated A549 cells. The protein levels of Cytochrome c release, Bax, cleaved caspases and PARP were increased in AGM130 treated cells, whereas Bcl-2 levels were decreased. AGM130 inhibited Insulin-like growth factor 1 receptor (IGF1R), AKT/mTOR signaling and inactivated mitogen-activated protein kinases (MAPK). AGM130 also induced slight autophagy as pro-survival function and autophagy inhibition by chloroquine (CQ) induced necrosis. In vivo tumor xenograft model, AGM130 dose-dependently suppressed transplanted A549 cell tumor growth and induced the expression of proliferative cell nuclear antigen (PCNA). AGM130 also increased TUNEL positive apoptotic cell populations and the induction of glandular differentiation with mucin pool compared with vehicle-treated control in tumor tissue. These results suggest that AGM130 is an effective novel indirubin-3'-oxime derivative of anti-cancer drug and may be an attractive candidate for non-small cell lung cancer therapy.
DOI: 10.1016/j.ejps.2015.08.015
PubMed: 26342773
Affiliations:
Links toward previous steps (curation, corpus...)
- to stream PubMed, to step Corpus: 000234
- to stream PubMed, to step Curation: 000234
- to stream PubMed, to step Checkpoint: 000267
- to stream Ncbi, to step Merge: 000311
- to stream Ncbi, to step Curation: 000311
- to stream Ncbi, to step Checkpoint: 000311
- to stream Main, to step Merge: 000F13
- to stream Main, to step Curation: 000F12
Le document en format XML
<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">5-Nitro-5'-hydroxy-indirubin-3'-oxime (AGM130), an indirubin-3'-oxime derivative, inhibits tumor growth by inducing apoptosis against non-small cell lung cancer in vitro and in vivo.</title><author><name sortKey="Ahn, Mee Young" sort="Ahn, Mee Young" uniqKey="Ahn M" first="Mee-Young" last="Ahn">Mee-Young Ahn</name><affiliation wicri:level="1"><nlm:affiliation>Department of Oral & Maxillofacial Pathology, College of Dentistry, Wonkwang Bone Regeneration Research Institute, Daejeon Dental Hospital, Wonkwang University, Daejeon 302-120, Republic of Korea.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Department of Oral & Maxillofacial Pathology, College of Dentistry, Wonkwang Bone Regeneration Research Institute, Daejeon Dental Hospital, Wonkwang University, Daejeon 302-120</wicri:regionArea><wicri:noRegion>Daejeon 302-120</wicri:noRegion></affiliation></author><author><name sortKey="Kim, Tae Hyung" sort="Kim, Tae Hyung" uniqKey="Kim T" first="Tae-Hyung" last="Kim">Tae-Hyung Kim</name><affiliation wicri:level="1"><nlm:affiliation>Division of Toxicology, School of Pharmacy, Sungkyunkwan University, Suwon 440-746, Republic of Korea.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Division of Toxicology, School of Pharmacy, Sungkyunkwan University, Suwon 440-746</wicri:regionArea><wicri:noRegion>Suwon 440-746</wicri:noRegion></affiliation></author><author><name sortKey="Kwon, Seong Min" sort="Kwon, Seong Min" uniqKey="Kwon S" first="Seong-Min" last="Kwon">Seong-Min Kwon</name><affiliation wicri:level="1"><nlm:affiliation>Department of Oral & Maxillofacial Pathology, College of Dentistry, Wonkwang Bone Regeneration Research Institute, Daejeon Dental Hospital, Wonkwang University, Daejeon 302-120, Republic of Korea.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Department of Oral & Maxillofacial Pathology, College of Dentistry, Wonkwang Bone Regeneration Research Institute, Daejeon Dental Hospital, Wonkwang University, Daejeon 302-120</wicri:regionArea><wicri:noRegion>Daejeon 302-120</wicri:noRegion></affiliation></author><author><name sortKey="Yoon, Hyo Eun" sort="Yoon, Hyo Eun" uniqKey="Yoon H" first="Hyo-Eun" last="Yoon">Hyo-Eun Yoon</name><affiliation wicri:level="1"><nlm:affiliation>Department of Oral & Maxillofacial Pathology, College of Dentistry, Wonkwang Bone Regeneration Research Institute, Daejeon Dental Hospital, Wonkwang University, Daejeon 302-120, Republic of Korea.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Department of Oral & Maxillofacial Pathology, College of Dentistry, Wonkwang Bone Regeneration Research Institute, Daejeon Dental Hospital, Wonkwang University, Daejeon 302-120</wicri:regionArea><wicri:noRegion>Daejeon 302-120</wicri:noRegion></affiliation></author><author><name sortKey="Kim, Hyung Sik" sort="Kim, Hyung Sik" uniqKey="Kim H" first="Hyung-Sik" last="Kim">Hyung-Sik Kim</name><affiliation wicri:level="1"><nlm:affiliation>Division of Toxicology, School of Pharmacy, Sungkyunkwan University, Suwon 440-746, Republic of Korea.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Division of Toxicology, School of Pharmacy, Sungkyunkwan University, Suwon 440-746</wicri:regionArea><wicri:noRegion>Suwon 440-746</wicri:noRegion></affiliation></author><author><name sortKey="Kim, Jae Il" sort="Kim, Jae Il" uniqKey="Kim J" first="Jae-Il" last="Kim">Jae-Il Kim</name><affiliation wicri:level="1"><nlm:affiliation>School of Life Sciences, Gwangju Institute of Science and Technology (GIST), Gwangju 500-712, Republic of Korea; Division of Drug Discovery, Anygen Co., Ltd., Gwangju 500-712, Republic of Korea.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>School of Life Sciences, Gwangju Institute of Science and Technology (GIST), Gwangju 500-712, Republic of Korea; Division of Drug Discovery, Anygen Co., Ltd., Gwangju 500-712</wicri:regionArea><wicri:noRegion>Gwangju 500-712</wicri:noRegion></affiliation></author><author><name sortKey="Kim, Yong Chul" sort="Kim, Yong Chul" uniqKey="Kim Y" first="Yong-Chul" last="Kim">Yong-Chul Kim</name><affiliation wicri:level="1"><nlm:affiliation>School of Life Sciences, Gwangju Institute of Science and Technology (GIST), Gwangju 500-712, Republic of Korea; Division of Drug Discovery, Anygen Co., Ltd., Gwangju 500-712, Republic of Korea.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>School of Life Sciences, Gwangju Institute of Science and Technology (GIST), Gwangju 500-712, Republic of Korea; Division of Drug Discovery, Anygen Co., Ltd., Gwangju 500-712</wicri:regionArea><wicri:noRegion>Gwangju 500-712</wicri:noRegion></affiliation></author><author><name sortKey="Kang, Keon Wook" sort="Kang, Keon Wook" uniqKey="Kang K" first="Keon-Wook" last="Kang">Keon-Wook Kang</name><affiliation wicri:level="4"><nlm:affiliation>College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul 151-742, Republic of Korea.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul 151-742</wicri:regionArea><placeName><settlement type="city">Séoul</settlement><region type="capital">Région capitale de Séoul</region></placeName><orgName type="university">Université nationale de Séoul</orgName><placeName><settlement type="city">Séoul</settlement></placeName></affiliation></author><author><name sortKey="Ahn, Sang Gun" sort="Ahn, Sang Gun" uniqKey="Ahn S" first="Sang-Gun" last="Ahn">Sang-Gun Ahn</name><affiliation wicri:level="1"><nlm:affiliation>Department of Pathology, College of Dentistry, Chosun University, Gwangju 501-759, Republic of Korea.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Department of Pathology, College of Dentistry, Chosun University, Gwangju 501-759</wicri:regionArea><wicri:noRegion>Gwangju 501-759</wicri:noRegion></affiliation></author><author><name sortKey="Yoon, Jung Hoon" sort="Yoon, Jung Hoon" uniqKey="Yoon J" first="Jung-Hoon" last="Yoon">Jung-Hoon Yoon</name><affiliation wicri:level="1"><nlm:affiliation>Department of Oral & Maxillofacial Pathology, College of Dentistry, Wonkwang Bone Regeneration Research Institute, Daejeon Dental Hospital, Wonkwang University, Daejeon 302-120, Republic of Korea. Electronic address: opathyoon@wku.ac.kr.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Department of Oral & Maxillofacial Pathology, College of Dentistry, Wonkwang Bone Regeneration Research Institute, Daejeon Dental Hospital, Wonkwang University, Daejeon 302-120</wicri:regionArea><wicri:noRegion>Daejeon 302-120</wicri:noRegion></affiliation></author></titleStmt><publicationStmt><idno type="wicri:source">PubMed</idno><date when="2015">2015</date><idno type="RBID">pubmed:26342773</idno><idno type="pmid">26342773</idno><idno type="doi">10.1016/j.ejps.2015.08.015</idno><idno type="wicri:Area/PubMed/Corpus">000234</idno><idno type="wicri:explorRef" wicri:stream="PubMed" wicri:step="Corpus" wicri:corpus="PubMed">000234</idno><idno type="wicri:Area/PubMed/Curation">000234</idno><idno type="wicri:explorRef" wicri:stream="PubMed" wicri:step="Curation">000234</idno><idno type="wicri:Area/PubMed/Checkpoint">000267</idno><idno type="wicri:explorRef" wicri:stream="Checkpoint" wicri:step="PubMed">000267</idno><idno type="wicri:Area/Ncbi/Merge">000311</idno><idno type="wicri:Area/Ncbi/Curation">000311</idno><idno type="wicri:Area/Ncbi/Checkpoint">000311</idno><idno type="wicri:Area/Main/Merge">000F13</idno><idno type="wicri:Area/Main/Curation">000F12</idno><idno type="wicri:Area/Main/Exploration">000F12</idno></publicationStmt><sourceDesc><biblStruct><analytic><title xml:lang="en">5-Nitro-5'-hydroxy-indirubin-3'-oxime (AGM130), an indirubin-3'-oxime derivative, inhibits tumor growth by inducing apoptosis against non-small cell lung cancer in vitro and in vivo.</title><author><name sortKey="Ahn, Mee Young" sort="Ahn, Mee Young" uniqKey="Ahn M" first="Mee-Young" last="Ahn">Mee-Young Ahn</name><affiliation wicri:level="1"><nlm:affiliation>Department of Oral & Maxillofacial Pathology, College of Dentistry, Wonkwang Bone Regeneration Research Institute, Daejeon Dental Hospital, Wonkwang University, Daejeon 302-120, Republic of Korea.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Department of Oral & Maxillofacial Pathology, College of Dentistry, Wonkwang Bone Regeneration Research Institute, Daejeon Dental Hospital, Wonkwang University, Daejeon 302-120</wicri:regionArea><wicri:noRegion>Daejeon 302-120</wicri:noRegion></affiliation></author><author><name sortKey="Kim, Tae Hyung" sort="Kim, Tae Hyung" uniqKey="Kim T" first="Tae-Hyung" last="Kim">Tae-Hyung Kim</name><affiliation wicri:level="1"><nlm:affiliation>Division of Toxicology, School of Pharmacy, Sungkyunkwan University, Suwon 440-746, Republic of Korea.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Division of Toxicology, School of Pharmacy, Sungkyunkwan University, Suwon 440-746</wicri:regionArea><wicri:noRegion>Suwon 440-746</wicri:noRegion></affiliation></author><author><name sortKey="Kwon, Seong Min" sort="Kwon, Seong Min" uniqKey="Kwon S" first="Seong-Min" last="Kwon">Seong-Min Kwon</name><affiliation wicri:level="1"><nlm:affiliation>Department of Oral & Maxillofacial Pathology, College of Dentistry, Wonkwang Bone Regeneration Research Institute, Daejeon Dental Hospital, Wonkwang University, Daejeon 302-120, Republic of Korea.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Department of Oral & Maxillofacial Pathology, College of Dentistry, Wonkwang Bone Regeneration Research Institute, Daejeon Dental Hospital, Wonkwang University, Daejeon 302-120</wicri:regionArea><wicri:noRegion>Daejeon 302-120</wicri:noRegion></affiliation></author><author><name sortKey="Yoon, Hyo Eun" sort="Yoon, Hyo Eun" uniqKey="Yoon H" first="Hyo-Eun" last="Yoon">Hyo-Eun Yoon</name><affiliation wicri:level="1"><nlm:affiliation>Department of Oral & Maxillofacial Pathology, College of Dentistry, Wonkwang Bone Regeneration Research Institute, Daejeon Dental Hospital, Wonkwang University, Daejeon 302-120, Republic of Korea.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Department of Oral & Maxillofacial Pathology, College of Dentistry, Wonkwang Bone Regeneration Research Institute, Daejeon Dental Hospital, Wonkwang University, Daejeon 302-120</wicri:regionArea><wicri:noRegion>Daejeon 302-120</wicri:noRegion></affiliation></author><author><name sortKey="Kim, Hyung Sik" sort="Kim, Hyung Sik" uniqKey="Kim H" first="Hyung-Sik" last="Kim">Hyung-Sik Kim</name><affiliation wicri:level="1"><nlm:affiliation>Division of Toxicology, School of Pharmacy, Sungkyunkwan University, Suwon 440-746, Republic of Korea.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Division of Toxicology, School of Pharmacy, Sungkyunkwan University, Suwon 440-746</wicri:regionArea><wicri:noRegion>Suwon 440-746</wicri:noRegion></affiliation></author><author><name sortKey="Kim, Jae Il" sort="Kim, Jae Il" uniqKey="Kim J" first="Jae-Il" last="Kim">Jae-Il Kim</name><affiliation wicri:level="1"><nlm:affiliation>School of Life Sciences, Gwangju Institute of Science and Technology (GIST), Gwangju 500-712, Republic of Korea; Division of Drug Discovery, Anygen Co., Ltd., Gwangju 500-712, Republic of Korea.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>School of Life Sciences, Gwangju Institute of Science and Technology (GIST), Gwangju 500-712, Republic of Korea; Division of Drug Discovery, Anygen Co., Ltd., Gwangju 500-712</wicri:regionArea><wicri:noRegion>Gwangju 500-712</wicri:noRegion></affiliation></author><author><name sortKey="Kim, Yong Chul" sort="Kim, Yong Chul" uniqKey="Kim Y" first="Yong-Chul" last="Kim">Yong-Chul Kim</name><affiliation wicri:level="1"><nlm:affiliation>School of Life Sciences, Gwangju Institute of Science and Technology (GIST), Gwangju 500-712, Republic of Korea; Division of Drug Discovery, Anygen Co., Ltd., Gwangju 500-712, Republic of Korea.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>School of Life Sciences, Gwangju Institute of Science and Technology (GIST), Gwangju 500-712, Republic of Korea; Division of Drug Discovery, Anygen Co., Ltd., Gwangju 500-712</wicri:regionArea><wicri:noRegion>Gwangju 500-712</wicri:noRegion></affiliation></author><author><name sortKey="Kang, Keon Wook" sort="Kang, Keon Wook" uniqKey="Kang K" first="Keon-Wook" last="Kang">Keon-Wook Kang</name><affiliation wicri:level="4"><nlm:affiliation>College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul 151-742, Republic of Korea.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul 151-742</wicri:regionArea><placeName><settlement type="city">Séoul</settlement><region type="capital">Région capitale de Séoul</region></placeName><orgName type="university">Université nationale de Séoul</orgName><placeName><settlement type="city">Séoul</settlement></placeName></affiliation></author><author><name sortKey="Ahn, Sang Gun" sort="Ahn, Sang Gun" uniqKey="Ahn S" first="Sang-Gun" last="Ahn">Sang-Gun Ahn</name><affiliation wicri:level="1"><nlm:affiliation>Department of Pathology, College of Dentistry, Chosun University, Gwangju 501-759, Republic of Korea.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Department of Pathology, College of Dentistry, Chosun University, Gwangju 501-759</wicri:regionArea><wicri:noRegion>Gwangju 501-759</wicri:noRegion></affiliation></author><author><name sortKey="Yoon, Jung Hoon" sort="Yoon, Jung Hoon" uniqKey="Yoon J" first="Jung-Hoon" last="Yoon">Jung-Hoon Yoon</name><affiliation wicri:level="1"><nlm:affiliation>Department of Oral & Maxillofacial Pathology, College of Dentistry, Wonkwang Bone Regeneration Research Institute, Daejeon Dental Hospital, Wonkwang University, Daejeon 302-120, Republic of Korea. Electronic address: opathyoon@wku.ac.kr.</nlm:affiliation><country xml:lang="fr">Corée du Sud</country><wicri:regionArea>Department of Oral & Maxillofacial Pathology, College of Dentistry, Wonkwang Bone Regeneration Research Institute, Daejeon Dental Hospital, Wonkwang University, Daejeon 302-120</wicri:regionArea><wicri:noRegion>Daejeon 302-120</wicri:noRegion></affiliation></author></analytic><series><title level="j">European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences</title><idno type="eISSN">1879-0720</idno><imprint><date when="2015" type="published">2015</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals</term><term>Antineoplastic Agents (therapeutic use)</term><term>Apoptosis</term><term>Carcinoma, Non-Small-Cell Lung (drug therapy)</term><term>Cell Cycle (drug effects)</term><term>Cell Line, Tumor</term><term>Humans</term><term>Indoles (pharmacology)</term><term>Indoles (therapeutic use)</term><term>Lung Neoplasms (drug therapy)</term><term>MAP Kinase Signaling System (drug effects)</term><term>Male</term><term>Mice</term><term>Mice, Nude</term><term>Neoplasm Transplantation</term><term>Oncogene Protein v-akt (antagonists & inhibitors)</term><term>Oximes (pharmacology)</term><term>Oximes (therapeutic use)</term><term>Receptors, Somatomedin (antagonists & inhibitors)</term></keywords><keywords scheme="KwdFr" xml:lang="fr"><term>Animaux</term><term>Antinéoplasiques (usage thérapeutique)</term><term>Apoptose</term><term>Carcinome pulmonaire non à petites cellules (traitement médicamenteux)</term><term>Cycle cellulaire ()</term><term>Humains</term><term>Indoles (pharmacologie)</term><term>Indoles (usage thérapeutique)</term><term>Lignée cellulaire tumorale</term><term>Mâle</term><term>Oximes (pharmacologie)</term><term>Oximes (usage thérapeutique)</term><term>Protéine oncogène v-akt (antagonistes et inhibiteurs)</term><term>Récepteurs des somatomédines (antagonistes et inhibiteurs)</term><term>Souris</term><term>Souris nude</term><term>Système de signalisation des MAP kinases ()</term><term>Transplantation tumorale</term><term>Tumeurs du poumon (traitement médicamenteux)</term></keywords><keywords scheme="MESH" type="chemical" qualifier="antagonists & inhibitors" xml:lang="en"><term>Oncogene Protein v-akt</term><term>Receptors, Somatomedin</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Indoles</term><term>Oximes</term></keywords><keywords scheme="MESH" type="chemical" qualifier="therapeutic use" xml:lang="en"><term>Antineoplastic Agents</term><term>Indoles</term><term>Oximes</term></keywords><keywords scheme="MESH" qualifier="antagonistes et inhibiteurs" xml:lang="fr"><term>Protéine oncogène v-akt</term><term>Récepteurs des somatomédines</term></keywords><keywords scheme="MESH" qualifier="drug effects" xml:lang="en"><term>Cell Cycle</term><term>MAP Kinase Signaling System</term></keywords><keywords scheme="MESH" qualifier="drug therapy" xml:lang="en"><term>Carcinoma, Non-Small-Cell Lung</term><term>Lung Neoplasms</term></keywords><keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Indoles</term><term>Oximes</term></keywords><keywords scheme="MESH" qualifier="traitement médicamenteux" xml:lang="fr"><term>Carcinome pulmonaire non à petites cellules</term><term>Tumeurs du poumon</term></keywords><keywords scheme="MESH" qualifier="usage thérapeutique" xml:lang="fr"><term>Antinéoplasiques</term><term>Indoles</term><term>Oximes</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Apoptosis</term><term>Cell Line, Tumor</term><term>Humans</term><term>Male</term><term>Mice</term><term>Mice, Nude</term><term>Neoplasm Transplantation</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Animaux</term><term>Apoptose</term><term>Cycle cellulaire</term><term>Humains</term><term>Lignée cellulaire tumorale</term><term>Mâle</term><term>Souris</term><term>Souris nude</term><term>Système de signalisation des MAP kinases</term><term>Transplantation tumorale</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">This study examined the anti-tumor effects of AGM130, a novel indirubin-3'-oxime derivative in A549 human non-small cell lung cancer cells. AGM130 significantly inhibited the proliferation and arrested the cell cycle of G2/M phase. Induction of apoptosis was detected in AGM130-treated A549 cells. The protein levels of Cytochrome c release, Bax, cleaved caspases and PARP were increased in AGM130 treated cells, whereas Bcl-2 levels were decreased. AGM130 inhibited Insulin-like growth factor 1 receptor (IGF1R), AKT/mTOR signaling and inactivated mitogen-activated protein kinases (MAPK). AGM130 also induced slight autophagy as pro-survival function and autophagy inhibition by chloroquine (CQ) induced necrosis. In vivo tumor xenograft model, AGM130 dose-dependently suppressed transplanted A549 cell tumor growth and induced the expression of proliferative cell nuclear antigen (PCNA). AGM130 also increased TUNEL positive apoptotic cell populations and the induction of glandular differentiation with mucin pool compared with vehicle-treated control in tumor tissue. These results suggest that AGM130 is an effective novel indirubin-3'-oxime derivative of anti-cancer drug and may be an attractive candidate for non-small cell lung cancer therapy. </div></front></TEI><affiliations><list><country><li>Corée du Sud</li></country><region><li>Région capitale de Séoul</li></region><settlement><li>Séoul</li></settlement><orgName><li>Université nationale de Séoul</li></orgName></list><tree><country name="Corée du Sud"><noRegion><name sortKey="Ahn, Mee Young" sort="Ahn, Mee Young" uniqKey="Ahn M" first="Mee-Young" last="Ahn">Mee-Young Ahn</name></noRegion><name sortKey="Ahn, Sang Gun" sort="Ahn, Sang Gun" uniqKey="Ahn S" first="Sang-Gun" last="Ahn">Sang-Gun Ahn</name><name sortKey="Kang, Keon Wook" sort="Kang, Keon Wook" uniqKey="Kang K" first="Keon-Wook" last="Kang">Keon-Wook Kang</name><name sortKey="Kim, Hyung Sik" sort="Kim, Hyung Sik" uniqKey="Kim H" first="Hyung-Sik" last="Kim">Hyung-Sik Kim</name><name sortKey="Kim, Jae Il" sort="Kim, Jae Il" uniqKey="Kim J" first="Jae-Il" last="Kim">Jae-Il Kim</name><name sortKey="Kim, Tae Hyung" sort="Kim, Tae Hyung" uniqKey="Kim T" first="Tae-Hyung" last="Kim">Tae-Hyung Kim</name><name sortKey="Kim, Yong Chul" sort="Kim, Yong Chul" uniqKey="Kim Y" first="Yong-Chul" last="Kim">Yong-Chul Kim</name><name sortKey="Kwon, Seong Min" sort="Kwon, Seong Min" uniqKey="Kwon S" first="Seong-Min" last="Kwon">Seong-Min Kwon</name><name sortKey="Yoon, Hyo Eun" sort="Yoon, Hyo Eun" uniqKey="Yoon H" first="Hyo-Eun" last="Yoon">Hyo-Eun Yoon</name><name sortKey="Yoon, Jung Hoon" sort="Yoon, Jung Hoon" uniqKey="Yoon J" first="Jung-Hoon" last="Yoon">Jung-Hoon Yoon</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
EXPLOR_STEP=$WICRI_ROOT/Sante/explor/ChloroquineV1/Data/Main/Exploration
HfdSelect -h $EXPLOR_STEP/biblio.hfd -nk 000F12 | SxmlIndent | more
Ou
HfdSelect -h $EXPLOR_AREA/Data/Main/Exploration/biblio.hfd -nk 000F12 | SxmlIndent | more
Pour mettre un lien sur cette page dans le réseau Wicri
{{Explor lien
|wiki= Sante
|area= ChloroquineV1
|flux= Main
|étape= Exploration
|type= RBID
|clé= pubmed:26342773
|texte= 5-Nitro-5'-hydroxy-indirubin-3'-oxime (AGM130), an indirubin-3'-oxime derivative, inhibits tumor growth by inducing apoptosis against non-small cell lung cancer in vitro and in vivo.
}}
Pour générer des pages wiki
HfdIndexSelect -h $EXPLOR_AREA/Data/Main/Exploration/RBID.i -Sk "pubmed:26342773" \
| HfdSelect -Kh $EXPLOR_AREA/Data/Main/Exploration/biblio.hfd \
| NlmPubMed2Wicri -a ChloroquineV1
| This area was generated with Dilib version V0.6.33. |  |