Los ntawm Cocer Peptides 
29 hnub dhau los
Tag nrho cov kab lus thiab cov ntaub ntawv ntawm cov khoom lag luam muab rau ntawm lub vev xaib no tsuas yog rau cov ntaub ntawv tshaj tawm kev tshaj tawm thiab cov hom phiaj kev kawm.
Cov khoom muab rau hauv lub vev xaib no yog npaj tshwj xeeb rau kev tshawb fawb hauv vitro. Kev tshawb fawb hauv vitro (Latin: * hauv iav *, lub ntsiab lus hauv iav) yog ua los ntawm tib neeg lub cev. Cov khoom no tsis yog tshuaj, tsis tau txais kev pom zoo los ntawm US Food and Drug Administration (FDA), thiab yuav tsum tsis txhob siv los tiv thaiv, kho, lossis kho txhua yam mob, kab mob, lossis mob. Nws raug txwv nruj raws li txoj cai los qhia cov khoom no rau hauv tib neeg lossis tsiaj lub cev hauv txhua daim ntawv.
Cov tshuaj Peptide thiab cov tshuaj me me-molecule ob leeg ua lub luag haujlwm tseem ceeb hauv kev txhim kho tshuaj thiab kev siv tshuaj kho mob, tab sis lawv txawv ntawm lawv cov txheej txheem ntawm kev ua thiab kev siv cov yam ntxwv.
Daim duab 1 Kev sib piv ntawm cyclic peptide therapeutics rau classical me me molecules thiab biologics.
1. Mechanism of Action
Mechanism ntawm kev ua ntawm cov tshuaj peptide: cov tshuaj Peptide feem ntau siv lawv cov teebmeem los ntawm kev khi rau cov receptors tshwj xeeb hauv lub cev. Vim lawv cov qauv zoo sib xws rau endogenous bioactive peptides, lawv tuaj yeem lees paub thiab khi rau cov neeg txais kev sib raug zoo, ua kom lossis inhibiting receptor-mediated signaling txoj hauv kev los tswj cov cellular physiological functions. Insulin yog ib yam tshuaj peptide uas khi rau insulin receptors ntawm lub xovtooj ntawm tes, pib ua cov txheej txheem ntawm cov teeb liab hloov mus rau kev txhawb nqa cov piam thaj thiab siv los ntawm cov hlwb, yog li txo cov ntshav qabzib.
Qee cov tshuaj peptide tuaj yeem ua raws li kev ua haujlwm ntawm peptides ntuj. Tom qab khi rau receptors ntawm lub xov tooj ntawm tes, lawv tswj cov txheej txheem ntawm tes xws li kev loj hlob, kev sib txawv, thiab apoptosis, thiab siv los kho ntau yam kab mob xws li mob qog noj ntshav thiab kab mob plawv. Lwm cov tshuaj peptide tuaj yeem ua raws li cov substrates lossis inhibitors ntawm enzymes, cuam tshuam rau kev ua haujlwm enzyme thiab yog li tswj cov txheej txheem metabolic hauv lub cev.
Mechanism ntawm kev txiav txim ntawm cov tshuaj me me-molecule: Cov txheej txheem ntawm kev txiav txim ntawm cov tshuaj me me-molecule yog ntau haiv neeg. Ntau cov tshuaj me me ua rau lawv cov teebmeem los ntawm kev khi rau cov hom phiaj protein, uas tuaj yeem ua enzymes, receptors, ion channels, thiab lwm yam. Nonsteroidal anti-inflammatory tshuaj (NSAIDs) xws li tshuaj aspirin inhibit qhov kev ua ntawm cyclooxygenase (COX), txo cov prostaglandin synthesis, yog li exerting anti-inflammatory, analgesic, thiab antipyretic teebmeem. Kev sib txuas ntawm cov tshuaj me me rau cov hom phiaj yog feem ntau ua raws li cov khoom siv hluav taws xob xws li hydrogen bonds, van der Waals rog, thiab ionic bonds. Qee cov tshuaj me me tuaj yeem nkag mus rau hauv DNA ob chav helix qauv, cuam tshuam nrog DNA replication thiab transcription txheej txheem, thiab siv los kho cov kab mob xws li qog. Lwm cov tshuaj me me tuaj yeem tswj cov ion channel hauv cell membranes, cuam tshuam rau cellular electrophysiological kev ua ub no. Piv txwv li, cov tshuaj antiarrhythmic ua rau cov ion channels hauv cov hlab plawv cov hlab ntsha los tswj cov hlab plawv.
2. Cov ntawv thov
Daim ntawv thov hauv kev kho kab mob - tshuaj Peptide: Cov tshuaj Peptide qhia tau hais tias muaj txiaj ntsig zoo hauv kev kho mob ntawm ntau yam kab mob. Hauv kev kho mob ntshav qab zib, ntxiv rau insulin, glucagon-zoo li peptide-1 (GLP-1) analogues yog lwm chav kawm tseem ceeb ntawm cov tshuaj peptide. Lawv txhawb kev tsim cov tshuaj insulin, inhibit glucagon tso tawm, thiab ncua lub plab zom mov, yog li txo qis cov piam thaj hauv cov ntshav, nrog rau qhov zoo xws li kev pheej hmoo ntawm hypoglycemia thiab tswj qhov hnyav. Hauv kev kho mob qog noj ntshav, qee yam tshuaj tiv thaiv kab mob peptides tuaj yeem khi rau cov receptors tshwj xeeb ntawm cov qog hlwb, ua rau cov qog cell apoptosis lossis inhibiting qog angiogenesis, yog li ua tiav lub hom phiaj ntawm kev txo cov qog loj hlob thiab metastasis. Hauv kev kho kab mob plawv, qee yam tshuaj peptide tuaj yeem tswj hwm vascular tone thiab inhibit platelet aggregation, ua lub luag haujlwm tseem ceeb hauv kev tiv thaiv thiab kho cov kab mob plawv. Cov tshuaj Peptide kuj muaj qee qhov kev txwv, xws li qhov ncauj qhov ncauj tsawg, feem ntau xav tau kev tswj hwm ntawm cov kev tsis yog qhov ncauj xws li txhaj tshuaj, uas qee qhov txwv cov neeg mob yooj yim siv tshuaj.
Kev siv hauv kev kho kab mob - Cov tshuaj me me-molecule: Cov tshuaj me me-molecule yog siv dav hauv cov chaw kho mob, npog ntau yam kab mob. Hauv kev tswj hwm tus kab mob, tshuaj tua kab mob thiab lwm yam tshuaj me me tuaj yeem tiv thaiv lossis tua cov kab mob, kab mob, thiab lwm yam kab mob, cawm tau ntau tus neeg txoj sia. Hauv kev kho kab mob plawv, statins inhibit HMG-CoA reductase kom txo qis cov roj cholesterol, yog li tiv thaiv thiab kho cov kab mob plawv. Hauv kev kho mob hlwb thiab paj hlwb, cov tshuaj me me xws li tshuaj tiv thaiv kev ntxhov siab thiab cov tshuaj tiv thaiv kab mob tuaj yeem tswj cov qib neurotransmitter lossis kev ua haujlwm, yog li txhim kho cov neeg mob cov tsos mob. Qhov zoo ntawm cov tshuaj me me muaj xws li qhov ncauj bioavailability siab, nrog rau feem ntau yog siv los ntawm qhov ncauj, ua rau cov neeg mob ua raws li qhov zoo.
Qhov chaw
[1] Ji X, Nielsen AL, Heinis C. Cyclic Peptides for Drug Development[J]. Angewandte Chemie International Edition, 2023,63:e202308251.DOI:10.1002/anie.202308251.
[2] Rahman MA, Akter S, Dorotea D, et al. Renoprotective peev xwm ntawm me me molecule tej yam ntuj tso khoom tsom mitochondrial dysfunction [J]. Frontiers in Pharmacology, 2022,13:925993.DOI:10.3389/fphar.2022.925993.
