Re: [藥理] 抗癌藥 bortezomib

看板Pharmacy作者pharmawind (Pharma Wind)時間14年前 (2010/05/01 22:32)推噓17(17推 0噓 6→)

留言23則, 17人參與討論串2/3 (看更多)

※ 引述《gogoflower (萬花筒)》之銘言： : 想請問這藥物的機制 : 書上說是抑制proteasome 但是這和cancer有什麼關係呢 : 我在網路上都找不到耶 : 有沒有高手能解答 : 感謝 !!!!! The proteasome is an enzyme complex that is responsible for degrading proteins that control the cell cycle. Some of the proteins degraded by proteosomes regulate critical functions for cancer growth, such as regulation of the cell cycle, transcription factors, apoptosis, angiogenesis, and cell adhesion. One proteosome inhibitor, bortezomib, is commercially available. Bortezomib has very specific affinity for the catalytic portion of the proteosome.It can induce apoptosis in cancer cells indirectly. Bortezomib is a specific inhibitor of the 26S proteasome; one consequence of 26S proteasome inhibition is the accumulation of IκB, an inhibitor of the major transcription factor NF-κB. NF-κB induces transcription of genes that block cell death pathways and promote cell proliferation. Its activity depends on its release from its inhibitory partner protein, IκB, in the cytoplasm and move to the nucleus. When IκB fails to degrade, through the actions of bortezomib, NF-κB remains in the cytoplasm, preventing it from transcribing the genes that promote cancer growth. 簡單來說~ 就是這樣~ ╔════════Ｙ═════Ｙ═════Ｙ═════Ｙ════════╗ ║　　　　　　　　　　　　　　　　　　　　　　　　　　　　　　　　　　　║ ║ 　　　　　 Bortezomib ║ ║ IκB (緊抓不放) 　 IκB ╮ 　 ╱ ║ ║ \ NF-κB 　 │ ↙ Inhibit║ ║ 　 NF-κB ∣ ╭┬┬ ┬┬╮ ║ ║ ╲ ∣ NF-κB ╞ Proteosome ╡ ║ ║ ╲↗ ↓ ＼ ╞ 26S ╡ ║ ║ ╭──────────╮ IκB(緊抓不放) ╰┴┴ ┴┴╯ ║ ║ ∣　∪∪∪∪　細胞核　│　　　　　　　　　｜ ║ ║ ︱ ∩∩∩∩　 │　 ↓ ║ ║ 　 │　 NF-κB │ ● o .0. ║ ║ ╰─────↘────╯ ○‧○. ║ ║ release Anti-apoptosis factors O。Ｏ. ║ ║ ↘ ║ ║　　　　　　　　　　　Tumor survival ║ ╚═══════════════════════════════════╝ 1. NF-κB在細胞質中會被IκB抓住而無法進入細胞核中，也就無法發號細胞生長　　與抑制細胞凋亡的指令。 2. 而Proteosome 26S是負責降解IκB的Enzyme（牽涉到Ubiquitin, 略）。 3. Bortezomib可抑制Proteosome 26S，使得IκB的量變多，進而使NF-κB無法進入細胞膜促進轉錄、發揮作用，便無法抵抗apoptosis signal。 Bortezomib is approved for the treatment of patients with multiple myeloma and mantle cell lymphoma. Ref: Pharmacotherapy- A Pathophysiologic Approach, 7th ed, 2008;17:2107 如有錯誤　敬請各位前輩不吝指正 -- █◣ ◢█ Los Angeles φlin798183 Ｍ ◢ ★ ◣ Lakers █ ＃２４ ██ ██ █◤◢█ ◢█ ｒ █ █ █ ◤◥ ◤◥ ◢◢◣ █ █ ◤ ﹒ █◥█◤ ██◤ ◤ ★ ◢█◣ ◢ █ ◣ █◤◤ █◤◢█ ◢ ８ █◢█◣ █ ◢ ◢█◣ █ ◤ █ █ █ ◢◣ █ █ █ １ █ █ ◤ █ █ █ █◤◢ █ ★ █ ◤ ◥◤ █◤◢█ ◢█◣ ◥ ◤ ◢██ ██◤ ◥█◤ -- ※ 發信站: 批踢踢實業坊(ptt.cc) ◆ From: 118.170.206.15

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ayoun22

05/01 23:41, , 1^F

05/01 23:41, 1^F

※ 編輯: pharmawind 來自: 118.170.206.15 (05/01 23:50)

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IAMTHELAW

05/01 23:50, , 2^F

05/01 23:50, 2^F

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danielh2o2

05/01 23:50, , 3^F