Carboxyesteres (CES) a cikin metabolism miyagun ƙwayoyi: dauki phenoty da DDI

Keywords: Drug-Drug Interaction(DDI), Carboxylesterase 1, Carboxylesterase 2, CES1, CES2, Liver Carboxylesterase, Intestinal Carboxylesterase, CES Enzyme Inhibition, Drug Metabolic Stability, Reaction Phenotyping.

Samfurin Iphayan

Shigowa da

Carboxyesteres (CES) sune mabuɗin enzymytic enzymes da hannu a cikin metabolism na mahimmin maza da yawa na ESTER - kuma amide - Abubuwan da ke ɗauke da magunguna. Daga cikin waɗannan,Carboxylesting 1 (CES1)daCarboxylesting 2 (CES2)sune manyan shahararrun mutane. Rarraba rarraba nama da kuma substrate da ke Substrate da ke yin CES1 da CES2 na tsakiya zuwa fahimtar metabolism magunguna,Dogarowar magani na miyaguni, daMiyagunciri - Taron miyagun ƙwayoyia cikin ilimin kimiyyar magunguna.

CES1 da CES2: Gwaji da Ayyuka na Aiki

Carboxylestelylesting 1 (CES1) an bayyana sosai a cikin hanta kuma ana kiranta shi azamanKashi Carboxylest. Wannan enzyme an san shi ne da ingantaccen tsarin takamaiman, metaberiving magunguna kamar Oseltamivir, da methylphelrel, da kuma clopidogrel. Sabanin haka, Carboxylestellystreste 2 (CES2) ya fi yawa a cikin hanji, saboda haka ana kiran shi da yawaKayan aikin Carboxylestlestlestlestlestlestleslystall. CES2 tana taka rawar gani a cikin metabolitm na wakilan maganin anticancer kamar Irinotecan da Prodruts kamar Capercitabine.

Adadin bayyanar da CESS1 da CES2 na sa su ci gaba da niyya a Adme (sha, rarraba, sassauƙa, exressism, da exressism m. Duk Carboxylesslylessetilless (CES1) da cawan carboxylestals (CES2) ana tantance kimantawa a lokacin farkon matakan ci gaban kwayoyi.

Matsayi a cikin kwanciyar hankali na miyagun ƙwayoyi

Kwantar da kwayoyi na miyagun ƙwayoyi shine ainihin tushen tushen na Pharmacakingics. CES1 da CES2 suna tasiri sosai da kwanciyar hankali da rabi - Rayuwar Imter - dauke da talakawa talakawa. CES1, kasancewa Carboxylesslylesslylest, yana tasirin tsarin tsarin da plasma bayyanar. CES2, a matsayin akwati na ciki, da farko yana shafar farkon - Pass hydrolysis na kwayoyin halitta na baki. Kimanin yadda waɗannan enzymes ya mamaye kwayoyin 'yan takara ke taimakawa inganta tsarin miyagun ƙwayoyi da isarwa.

Enotying tare da ces enzymes

Enotyingyana da mahimmanci don sanin ainihin enzymes da ke daukar ƙwayoyin cuta. Dukkanin CES1 da CES2 suna da alaƙa da wannan karatun don fahimtar takamaiman gudummawar su. Cikakken Search Search phenoty na iya sanar da ci gaban Prodrugs da aka tsara don kunnawa da CES1 ko CES2, yana ba da izinin isar da miyagun ƙwayoyi da inganta bioavailability.

Masu binciken suna amfani da CESS1 da CES2 enzymes, aikin hanta (don carboomes hanta (don aikin hanji) don yin cikakkiyar haɗuwa. Manufar shine a rage bambance kuma tabbatar da cewa hanyoyin rayuwa suna da kyau - halayyar.

CES ENZYME

CES ENZYMEWannan damuwa ce saboda yuwuwar sa don haifar da mahimmancin miyagun ƙwayoyi. Hana CESS1 na iya lalata metabolism na substrater, yana haifar da yawan matakan magani da guba. Hakazalika, CES2 da ke hana a cikin hanji na iya rage kunnawa Prodrug, runtse ingancin warkewa.

Yawancin miyagun ƙwayoyi masu yawa - Binciken hulɗa na miyagun ƙwayoyi yanzu sun haɗa da allo don abubuwan haɗin enzyme. Wannan yana taimakawa wajen yin hasashen halayen sabbin magunguna na sabbin abubuwa masu guba da kuma tsara dabarun dosing waɗanda ke rage haɗari.

Misali, Co - Mumani na CES1 mai shigowa da methylphene zai iya daukaka plasma plasma na aiki da miyagun ƙwayoyi, yana haifar da haɗarin tasirin miyagun ƙwayoyi. Hakazalika, CES2 da ake bukata a lokacin da chemotherapy na iya tsoma baki tare da kunna Irinotecan, yana rage aikin anticomer.

Aikace-aikace a cikin binciken magunguna

Carboxylesrylest 1 (CES1) da CESBOXYLELYTELY 2 (CES2) sun zama kayan aikin da ba a sani ba a cikin binciken magunguna na zamani. Mahimmancin bincikensu:

• Annabta m magani na rayuwa.
• Gudanar da martani na phenoty don daidaitaccen enzing.
• Kimanta ces enzyme inhibitionbition ga hasashen magani - hulda miyagun ƙwayoyi.
• Tsararren ces - Prodru mai kunna prodrups don isarwa.

Matsayi na CES1 a matsayin Carda Carda Carboxyleslyles da CES2 a matsayin babban CarboxmylestalstalmyLylestalstals - wanda aka kafa cikin saitunan bincike na ilimi da masana'antu. Ta hanyar hada da ketraarin da ketraping CES, ya zama bututun cigurori, masana kimiyya na iya kirkirar magunguna da mafi inganci.

Ƙarshe

A ƙarshe, Carboxylestlylylylylylay 1 da Carboxylylylylylylylyles 2 sun fi enaboles kawai enzymes - suna da mahimmancin tasirin ƙwayoyi da aminci. Dual mai da hankali kan CES1 (Carboxylestellylest na CES1 (CE CARBOBOBOBOXYLALSTELSTER, da magani Enotme) yana da kyau ga 'yan takarar miyagun ƙwayoyi suna da kyau - halaye kafin gwajin asibiti. Fahimtar zurfin fahimtar CES ba kawai sauƙaƙe ƙirar miyagun ƙwayoyi ba amma kuma haɓaka raunin warkewa da ke sa kasuwa.