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      KCI등재 SCIE SCOPUS

      Transient Receptor Potential Vanilloid 1 Expression and Functionality in MCF-7 Cells: A Preliminary Investigation

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      https://www.riss.kr/link?id=A104425982

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      다국어 초록 (Multilingual Abstract)

      Purpose: Transient receptor potential vanilloid 1 (TRPV1) is a nonselectivecation channel belonging to the transient receptor potentialfamily, and it is expressed in different neoplastic tissues.
      Its activation is associated with regulation of cancer growth andprogression. The aim of this research was to study the expressionand pharmacological characteristics of TRPV1 in cells derivedfrom human breast cancer MCF-7 cells. Methods: TRPV1presence was assessed by binding studies and Western blotting.
      Receptor binding characteristics were evaluated through competitionassays, while 3-(4,5-dimethylthiazol-2-yl)-2,5,-dipheyltetrazoliumbromide reduction assays were performed to confirman early hypothesis regarding the modulation of cancer cell proliferation.
      The functionality of TRPV1 was evaluated by measuringCa2+ uptake in the presence of increasing concentrations ofTRPV1 agonists and antagonists. Results: Binding studies identifieda single class of TRPV1 (Bmax 1,492±192 fmol/mg protein),and Western blot showed a signal at 100 kDa corresponding tothe molecular weight of human TRPV1. Among the different testedagonists and antagonists, anandamide (Ki: 2.8×10-11 M) and5-iodoresiniferatoxin (5-I-RTX) (Ki: 5.6×10-11 M) showed the highestdegrees of affinity for TRPV1, respectively. All tested TRPV1agonists and antagonists caused a significant (p<0.05) decreasein cell growth rate in MCF-7 cells. For agonists and antagonists,the efficacy of tested compounds displayed the following rankorder: resiniferatoxin>anandamide>capsaicin and 5-I-RTX=capsazepine, respectively. Conclusion: These data indicate thatboth TRPV1 agonists and antagonists induce significant inhibitionof MCF-7 cell growth. Even though the mechanisms involvedin the antiproliferative effects of TRPV1 agonists and antagonistsshould be further investigated, it has been suggestedthat agonists cause desensitization of the receptor, leading to alterationin Ca2+-influx regulation. By contrast, antagonists causea functional block of the receptor with consequent fatal dysregulationof cell homeostasis.
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      Purpose: Transient receptor potential vanilloid 1 (TRPV1) is a nonselectivecation channel belonging to the transient receptor potentialfamily, and it is expressed in different neoplastic tissues. Its activation is associated with regulation of cancer ...

      Purpose: Transient receptor potential vanilloid 1 (TRPV1) is a nonselectivecation channel belonging to the transient receptor potentialfamily, and it is expressed in different neoplastic tissues.
      Its activation is associated with regulation of cancer growth andprogression. The aim of this research was to study the expressionand pharmacological characteristics of TRPV1 in cells derivedfrom human breast cancer MCF-7 cells. Methods: TRPV1presence was assessed by binding studies and Western blotting.
      Receptor binding characteristics were evaluated through competitionassays, while 3-(4,5-dimethylthiazol-2-yl)-2,5,-dipheyltetrazoliumbromide reduction assays were performed to confirman early hypothesis regarding the modulation of cancer cell proliferation.
      The functionality of TRPV1 was evaluated by measuringCa2+ uptake in the presence of increasing concentrations ofTRPV1 agonists and antagonists. Results: Binding studies identifieda single class of TRPV1 (Bmax 1,492±192 fmol/mg protein),and Western blot showed a signal at 100 kDa corresponding tothe molecular weight of human TRPV1. Among the different testedagonists and antagonists, anandamide (Ki: 2.8×10-11 M) and5-iodoresiniferatoxin (5-I-RTX) (Ki: 5.6×10-11 M) showed the highestdegrees of affinity for TRPV1, respectively. All tested TRPV1agonists and antagonists caused a significant (p<0.05) decreasein cell growth rate in MCF-7 cells. For agonists and antagonists,the efficacy of tested compounds displayed the following rankorder: resiniferatoxin>anandamide>capsaicin and 5-I-RTX=capsazepine, respectively. Conclusion: These data indicate thatboth TRPV1 agonists and antagonists induce significant inhibitionof MCF-7 cell growth. Even though the mechanisms involvedin the antiproliferative effects of TRPV1 agonists and antagonistsshould be further investigated, it has been suggestedthat agonists cause desensitization of the receptor, leading to alterationin Ca2+-influx regulation. By contrast, antagonists causea functional block of the receptor with consequent fatal dysregulationof cell homeostasis.

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      참고문헌 (Reference)

      1 Everaerts W, "Where is TRPV1 expressed in the bladder, do we see the real channel?" 379 : 421-425, 2009

      2 Bodó E, "Vanilloid receptor-1 (VR1) is widely expressed on various epithelial and mesenchymal cell types of human skin" 123 : 410-413, 2004

      3 Caterina MJ, "Transient receptor potential ion channels as participants in thermosensation and thermoregulation" 292 : R64-R76, 2007

      4 Youlden DR, "The descriptive epidemiology of female breast cancer: an international comparison of screening, incidence, survival and mortality" 36 : 237-248, 2012

      5 Scatchard G, "The attractions of proteins for small molecules and ions" 51 : 660-672, 1949

      6 Veronesi B, "The TRPV1 receptor: target of toxicants and therapeutics" 89 : 1-3, 2006

      7 Zhang L, "TRPM8 in prostate cancer cells: a potential diagnostic and prognostic marker with a secretory function?" 13 : 27-38, 2006

      8 Nilius B, "TRP channels in disease" 1772 : 805-812, 2007

      9 Santoni G, "TRP channels and cancer: new targets for diagnosis and chemotherapy" 11 : 54-67, 2011

      10 Salazar H, "Structural determinants of gating in the TRPV1 channel" 16 : 704-710, 2009

      1 Everaerts W, "Where is TRPV1 expressed in the bladder, do we see the real channel?" 379 : 421-425, 2009

      2 Bodó E, "Vanilloid receptor-1 (VR1) is widely expressed on various epithelial and mesenchymal cell types of human skin" 123 : 410-413, 2004

      3 Caterina MJ, "Transient receptor potential ion channels as participants in thermosensation and thermoregulation" 292 : R64-R76, 2007

      4 Youlden DR, "The descriptive epidemiology of female breast cancer: an international comparison of screening, incidence, survival and mortality" 36 : 237-248, 2012

      5 Scatchard G, "The attractions of proteins for small molecules and ions" 51 : 660-672, 1949

      6 Veronesi B, "The TRPV1 receptor: target of toxicants and therapeutics" 89 : 1-3, 2006

      7 Zhang L, "TRPM8 in prostate cancer cells: a potential diagnostic and prognostic marker with a secretory function?" 13 : 27-38, 2006

      8 Nilius B, "TRP channels in disease" 1772 : 805-812, 2007

      9 Santoni G, "TRP channels and cancer: new targets for diagnosis and chemotherapy" 11 : 54-67, 2011

      10 Salazar H, "Structural determinants of gating in the TRPV1 channel" 16 : 704-710, 2009

      11 Lin YS, "Sensitization of capsaicinsensitive lung vagal afferents by anandamide in rats: role of transient receptor potential vanilloid 1 receptors" 106 : 1142-1152, 2009

      12 Rossi T, "Selectivity of action of glycyrrhizin derivatives on the growth of MCF-7 and HEP-2 cells" 23 (23): 3813-3818, 2003

      13 Chou MZ, "Resiniferatoxin binds to the capsaicin receptor (TRPV1) near the extracellular side of the S4 transmembrane domain" 43 : 2501-2511, 2004

      14 Cheng Y, "Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction" 22 : 3099-3108, 1973

      15 Rigoni M, "Neurogenic responses mediated by vanilloid receptor-1(TRPV1) are blocked by the high affinity antagonist, iodo-resiniferatoxin" 138 : 977-985, 2003

      16 Czifra G, "Increased expressions of cannabinoid receptor-1 and transient receptor potential vanilloid-1 in human prostate carcinoma" 135 : 507-514, 2009

      17 Marincsák R, "Increased expression of TRPV1 in squamous cell carcinoma of the human tongue" 15 : 328-335, 2009

      18 Li J, "Increased GFR and renal excretory function by activation of TRPV1 in the isolated perfused kidney" 57 : 239-246, 2008

      19 Kauer JA, "Hot flash: TRPV channels in the brain" 32 : 215-224, 2009

      20 Dhennin-Duthille I, "High expression of transient receptor potential channels in human breast cancer epithelial cells and tissues: correlation with pathological parameters" 28 : 813-822, 2011

      21 Kalogris C, "Expression of transient receptor potential vanilloid-1(TRPV1) in urothelial cancers of human bladder: relation to clinicopathological and molecular parameters" 57 : 744-752, 2010

      22 Sanchez MG, "Expression of the transient receptor potential vanilloid 1 (TRPV1) in LNCaP and PC-3 prostate cancer cells and in human prostate tissue" 515 : 20-27, 2005

      23 Ho WY, "Development of multicellular tumor spheroid (MCTS) culture from breast cancer cell and a high throughput screening method using the MTT assay" 7 : e44640-, 2012

      24 Tóth A, "Design of a high-affinity competitive antagonist of the vanilloid receptor selective for the calcium entry-linked receptor population" 65 : 282-291, 2004

      25 Sung B, "Capsazepine, a TRPV1 antagonist, sensitizes colorectal cancer cells to apoptosis by TRAIL through ROS-JNK-CHOP-mediated upregulation of death receptors" 53 : 1977-1987, 2012

      26 Contassot E, "Arachidonyl ethanolamide induces apoptosis of uterine cervix cancer cells via aberrantly expressed vanilloid receptor-1" 93 : 182-188, 2004

      27 Ligresti A, "Antitumor activity of plant cannabinoids with emphasis on the effect of cannabidiol on human breast carcinoma" 318 : 1375-1387, 2006

      28 Santoni G, "Antioncogenic effects of transient receptor potential vanilloid 1 in the progression of transitional urothelial cancer of human bladder" 2012 : 458238-, 2012

      29 Menéndez L, "Analgesic effects of capsazepine and resiniferatoxin on bone cancer pain in mice" 393 : 70-73, 2006

      30 Sanz-Salvador L, "Agonist- and Ca2+-dependent desensitization of TRPV1 channel targets the receptor to lysosomes for degradation" 287 : 19462-19471, 2012

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      학술지 이력

      학술지 이력
      연월일 이력구분 이력상세 등재구분
      2023 평가예정 해외DB학술지평가 신청대상 (해외등재 학술지 평가)
      2020-01-01 평가 등재학술지 유지 (해외등재 학술지 평가) KCI등재
      2011-04-06 학술지명변경 외국어명 : Journal of Korean Breast Cancer -> Journal of Breast Cancer KCI등재
      2011-03-23 학술지명변경 외국어명 : Journal of Korean Breast Cancer -> 미등록 KCI등재
      2011-03-04 학술지명변경 한글명 : 한국유방암학회지 -> Journal of Breast Cancer KCI등재
      2011-01-01 평가 등재학술지 선정 (등재후보2차) KCI등재
      2010-01-01 평가 등재후보 1차 PASS (등재후보1차) KCI등재후보
      2008-01-01 평가 SCIE 등재 (신규평가) KCI등재후보
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      학술지 인용정보

      학술지 인용정보
      기준연도 WOS-KCI 통합IF(2년) KCIF(2년) KCIF(3년)
      2016 1.99 0.19 1.31
      KCIF(4년) KCIF(5년) 중심성지수(3년) 즉시성지수
      0.96 0.77 0.448 0.06
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