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10.1016/j.steroids.2014.07.009

http://scihub22266oqcxt.onion/10.1016/j.steroids.2014.07.009
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C4696022!4696022 !25065587
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suck abstract from ncbi


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pmid25065587
      Steroids 2015 ; 97 (ä): 2-7
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  • Targeting thapsigargin towards tumors #MMPMID25065587
  • Doan NT ; Paulsen ES ; Sehgal P ; Møller JV ; Nissen P ; Denmeade SR ; Isaacs JT ; Dionne CA ; Christensen SB
  • Steroids 2015[May]; 97 (ä): 2-7 PMID25065587 show ga
  • The skin irritating principle from Thapsia garganica was isolated, named thapsigargin and the structure elucidated. By inhibiting the sarco/endoplasmic reticulum Ca(2+) ATPase (SERCA) thapsigargin provokes apoptosis in almost all cells. By conjugating thapsigargin to peptides, which are only substrates for either prostate specific antigen (PSA) or prostate specific membrane antigen (PSMA) prodrugs were created, which selectively affect prostate cancer cells or neovascular tissue in tumors. One of the prodrug is currently tested in clinical phase II. The prodrug under clinical trial has been named mipsagargin.
  • |Animals [MESH]
  • |Antineoplastic Agents, Phytogenic/chemistry/isolation & purification/*pharmacology [MESH]
  • |Apiaceae/*chemistry [MESH]
  • |Apoptosis/drug effects [MESH]
  • |Cell Proliferation/drug effects [MESH]
  • |Enzyme Inhibitors/chemistry/isolation & purification/*pharmacology [MESH]
  • |Humans [MESH]
  • |Male [MESH]
  • |Mice [MESH]
  • |Molecular Structure [MESH]
  • |Neovascularization, Pathologic/drug therapy/pathology [MESH]
  • |Prodrugs/chemistry/isolation & purification/*pharmacology [MESH]
  • |Prostatic Neoplasms/*drug therapy/pathology [MESH]
  • |Sarcoplasmic Reticulum Calcium-Transporting ATPases/antagonists & inhibitors/metabolism [MESH]
  • |Soft Tissue Neoplasms/*drug therapy/pathology [MESH]


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