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▎ Ọdịdị GLP-2
Isi mmalite: PubChem |
Usoro: Tyr-{Aib}-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-{Aib}-Leu-Asp-Lys-Ile-Ala-Gln-{diacid-C20-gamm a-Glu-(AEEA)2-Lys}-Ala-Phe-Val-Gln-Trp-Leu-Ile-Ala-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2 Ụdị mkpụrụ ndụ: C 225H 348N 48O68 Arọ molekụla: 4813 g/mol Nọmba CAS: 2023788-19-2 PubChem CID: 163285897 Ụdị okwu: Zepbound; Mounjaro |
▎ Nchọpụta GLP-2
Kedu ihe ndabere nyocha nke GLP-2?
GLP-2 bụ ọgwụ polypeptide sịntetik. Nchoputa ya na mmepe ya sitere na nghota miri emi nke oke nke GLP-1 agonists nnabata di na ọgwụgwọ nke 2 metabolism na oke ibu n'oge ahu. Ọ bụ ezie na GLP-1 agonists anabatara egosila ọmarịcha arụmọrụ na njikwa glucose ọbara na mbelata ibu, ndị ọkà mmụta sayensị chọpụtara na ịgbalite onye na-anabata GIP adịghị ike, nke na-egbochi ịdị irè nke ọgwụ ahụ ruo n'ókè ụfọdụ. Ya mere, ndị otu nyocha na mmepe gbalịsiri ike imepụta ọgwụ ọhụrụ nke nwere ike ịgbalite ma GIPR na GLP-1R n'otu oge iji nweta njikwa glucose ọbara zuru oke ma dị irè na njikwa ibu [1]..
N'ime usoro nyocha na mmepe nke GLP-2, ndị ọkà mmụta sayensị mere ọtụtụ nyocha nke isi na nnwale ụlọ ọgwụ. N'ime usoro nyocha nke izizi, a na-eji nnwale anụmanụ iji nyochaa nke ọma njirimara ọgwụ nke GLP-2. Nsonaazụ ahụ gosipụtara ikike ya na njikwa glucose ọbara na mbelata ibu, na-atọ ntọala maka nnwale ụlọ ọgwụ na-esote. N'ikpeazụ, GLP-2 banyere n'ọkwa nnwale ụlọ ọgwụ, gụnyere nkeji I, II, na III. Usoro nke m tụlere nchekwa, nnabata, na akụrụngwa ọgwụ nke ọgwụ ahụ, nsonaazụ ya gosipụtara ezigbo nchekwa na nnabata. Usoro nke Abụọ nyochara ịdị irè na nchekwa nke usoro ọgwụgwọ dị iche iche na ndị ọrịa nwere ụdị 2 metabolism, na-ebu ụzọ chọpụta oke dose dị irè. Nnwale ule ụlọ ọgwụ nke isi nke III, dị ka usoro ọmụmụ SURPASS, gụnyere ọnụ ọgụgụ buru ibu nke ndị ọrịa nwere ụdị 2 metabolism. Nsonaazụ gosiri na GLP-2 dị elu karịa ndị agonists GLP-1 dị adị, dị ka GLP-1, n'ibelata glucose ọbara na ịdị arọ, na-enye ihe akaebe siri ike maka ngwa ahịa [1]..
GLP-2 bụ polypeptide mejupụtara amino asịd 39, na agbanweela nhazi ya iji kwalite nkwụsi ike ya na ọgwụ ọgwụ. Nhazi ya pụrụ iche na-enyere ya aka ijikọ mmetụta nke incretins abụọ, GIP na GLP-1, n'ime otu molekul, na-eme ka ndị na-anabata homonụ na-etinye aka na njikwa glucose ọbara site na usoro abụọ. Kpọmkwem, n'otu aka ahụ, ọ na-arụ ọrụ na pancreas iji kwalite mmepụta insulin ma gbochie mwepụta glucagon iji wedata glucose ọbara; N'aka nke ọzọ, ọ na-arụ ọrụ na usoro nhụjuanya nke etiti, na-egbu oge nkwụsị nke gastric, ịba ụba nke satiety, ibelata agụụ na iri nri, na ịnweta njikwa ibu. Usoro abụọ a na-enye GLP-2 uru pụrụ iche na ọgwụgwọ ụdị 2 metabolism na oke ibu, na-enye ndị ọrịa nhọrọ ọgwụgwọ zuru oke [1].
Kedu ihe bụ usoro nke GLP-2?
GLP-2 na-ebelata glucose ọbara site na ọtụtụ usoro ndị a:
Ntinye nke GLP-1 Nnabata: GLP-2 na-ejikọta na GLP-1 ndị na-anabata ya na mkpụrụ ndụ beta pancreatic, na-eṅomi omume nke GLP-1 eke. GLP-1 bụ homonụ nke eriri afọ na-emepụta nke dị mkpa maka idowe glucose homeostasis. Ọ nwere ike ịkwalite njikọ insulin, nzuzo, na nghọta glucose, yana ibelata secretion glucagon iji kwalite satiety na igbochi agụụ. N'ime ndị ọrịa nwere ụdị metabolism nke 2, ụkọ insulin ezughi oke ma ọ bụ mbelata mmetụta cellular na insulin na-eduga n'ịbawanye glucose ọbara. GLP-2 na-abawanye mmepụta insulin site na ịgbalite ndị na-anabata GLP-1, na-emezi njikwa glucose ọbara. N'otu oge ahụ, ịgbalite ndị na-anabata GLP-1 nwekwara ike igbochi ntọhapụ nke glucagon, na-ebelata isi mmalite nke glucose ọbara ma na-enye aka na njikwa glucose ọbara [2]..
Ntinye nke ndị na-anabata GIP: GLP-2 na-arụ ọrụ na ndị na-anabata GIP, na ịgbalite ya nwere ike ịkwalite mmetụta insulin na nzuzo. Ndị na-anabata GIP na-anọkarị na anụ ahụ dị ka mkpụrụ ndụ beta nke pancreatic. Mgbe emechara ya, site na ntugharị ụzọ mgbama intracellular, insulin na-abawanye, yana nnabata cell na-anabata insulin, na-ebelata glucose ọbara nke ọma [2] . Mmetụta agonist onye na-anabata ihe abụọ a na-eme GLP-2 dị irè karịa otu GLP-1 agonists na-akwalite mmepụta insulin na igbochi ntọhapụ glucagon [2]..
Na-egbu oge mkpofu afọ na ịba ụba satiety: GLP-2 nwere ike igbu oge ịwụfu afọ, ịgbatị oge obibi nri n'ime afọ, na-ebelata ogo nnabata nke nri, na igbochi mmụba dị ukwuu na glucose ọbara mgbe nri gasịrị. Mmetụta ya na mkpofu afọ dị ka nke GLP-1 agonists nnabata. N'otu oge ahụ, ọ na-arụ ọrụ na sistemụ ụjọ nke etiti, na-abawanye satiety, na-ebelata agụụ na iri nri, nke dabara adaba maka nsogbu oke ibu nke ndị ọrịa nwere ụdị 2 metabolism na-esonyere ya, na-enyere aka melite nguzogide insulin na ọnọdụ metabolic zuru oke [2]..
Imeziwanye mmetụta insulin na ọrịa shuga: GLP-2 nwere ike ịbawanye ọkwa adiponectin, adipocytokine metụtara mmetụta insulin, na-enyere aka melite mmetụta insulin, na-eme ka mkpụrụ ndụ nwee ike ịnara nke ọma na iji glucose, yana ibelata glucose ọbara (Anonymous, 2023). Na mgbakwunye, ọ nwekwara ike melite profaịlụ lipid, na-enwe mmetụta nchebe na ahụike obi. E gosiputara na ọ nwere ike ịkwalite ọbara mgbali elu, belata LDL cholesterol na triglycerides [3].
Isi mmalite: PubMed [5]
Kedu ihe ọmụmụ ndị metụtara ya?
Ịdị irè na njikwa arọ na ndị ọrịa nwere oke ibu na ụdị ọrịa shuga 2
Ọtụtụ ọmụmụ ụlọ ọgwụ ekwenyela na GLP-2 nwere mmetụta mbelata ibu. N'ime ọmụmụ 'SURMOUNT-2' a na-eme usoro nke 3 a, kpuru ìsì abụọ, enweghị usoro, na-achịkwa placebo na mba asaa. Ndị okenye (afọ ≥ 18) nwere BMI nke 27 kg / m² ma ọ bụ karịa na HbA₁c nke 7-10% debanyere aha wee kenye ya na-enweghị usoro ka ọ nata ntụtụ subcutaneous otu ugboro kwa izu nke GLP-2 (10 mg ma ọ bụ 15 mg) ma ọ bụ placebo maka izu 72. Nsonaazụ gosiri na n'ime izu 72, pasent nke ibu ibu na GLP-2 10 mg na 15 mg otu bụ -12.8% na -14.7% n'otu n'otu, ma e jiri ya tụnyere -3.2% na placebo otu. Atụmatụ ọgwụgwọ dị iche iche nke GLP-2 10 mg na 15 mg ma e jiri ya tụnyere placebo bụ -9.6 pasent na -11.6 pasent n'otu n'otu, bụ nke dị ịrịba ama (p <0.0001). Na mgbakwunye, ọtụtụ ndị ọrịa na-anata ọgwụgwọ GLP-2 ruru n'ọnụ ụzọ mfu 5% ma ọ bụ oke ibu (79 - 83% vs 32%) (Garvey WT, 2023). N'ime ọmụmụ ihe a, nkezi ịdị arọ ntọala bụ 100.7 kg, BMI bụ 36.1 kg/m² na HbA₁c bụ 8.02%. Mgbe izu iri asaa na abụọ nke ọgwụgwọ gasịrị, GLP-2 abụghị naanị ibelata ịdị arọ nke ahụ mana ọ nwekwara mmetụta dị mma na njikwa glucose ọbara ..
Mmelite nke ọrịa shuga neuropathy
Nnyocha egosiwo na GLP1-RA nwere ike ibelata ihe ize ndụ nke ịda mbà n'obi na ndị ọrịa nwere ụdị 2 metabolism site na imeziwanye ebe nchekwa, mmụta, na imeri mmejọ uche. Dị ka ihe abụọ GIP-RA / GLP-1RA, na neuroblastoma cell line (SHSY5Y), nchọpụta achọpụtala na GLP-2 nwere mmetụta na nrịbama nke neuronal uto (CREB na BDNF), apoptosis (BAX / Bcl2 ratio), iche (pAkt, MAP2, GAP43, na AGBL4), na insulin resistance (GLUTLUT), 1 insulin resistance (GLUTLUT1). Nsonaazụ a na-emesi ike ọrụ GLP-2 n'ịgbalite ụzọ pAkt/CREB/BDNF na mgbago mgbago mgbago mgbago na arụmọrụ neuroprotective ya, na-egosi na ọ nwere ike igbochi mmetụta ndị metụtara hyperglycemia na insulin resistance na ọkwa neuronal. Ya mere, GLP-2 nwere ike imeziwanye neurodegeneration nke hyperglycemia kpatara ma merie nguzogide insulin nke neuronal, na-enye nghọta ọhụrụ banyere mmelite nke neuropathy metụtara metabolism [5]..
Ọganihu nyocha na ọgwụgwọ ụdị ọrịa shuga 2
Dịka ụdị ọgwụ hypoglycemic ọhụrụ, GLP-2 abụrụla agonist GIP/GLP-1R nke mbụ akwadoro maka ọgwụgwọ metabolism na United States. Ọtụtụ nnukwu nnwale ụlọ ọgwụ ekwenyela na mbelata glucose ọbara ya dị ịrịba ama na mmetụta mbelata ibu, ma nwee ikike na nchekwa obi. Echiche nke peptides sịntetik emeghela ọtụtụ ohere amaghị maka GLP-2. Nnwale na-aga n'ihu (NCT04166773) na ihe akaebe na-egosi na ọ bụ ọgwụ na-ekwe nkwa na mpaghara ọrịa imeju na-adịghị egbu egbu (NAFLD), renal na neuroprotection [6] (Ma Z, 2023).
Mmetụta ogologo oge nke GLP-2 na ahụike obi
GLP-2 nwere ike ibelata ihe ize ndụ nke ọrịa obi site n'ịkwalite mbelata ibu. Otu nnyocha nyochara mmetụta nke GLP-2 na oke ibu na ọrịa obi na ọrịa obi na ndị okenye America [7] . Nnyocha ahụ chọpụtara na n'etiti ndị okenye America tozuru oke maka ọgwụgwọ GLP-2, mgbe ọgwụgwọ ya na 15 mg nke GLP-2, e mere atụmatụ na 70.6% na 56.7% nke ndị okenye tụfuru ≥ 15% na ≥ 20% nke ịdị arọ ahụ ha n'otu n'otu, nke pụtara mbelata 58.8% na ọnụ ọgụgụ ndị buru oke ibu. N'ime ndị na-enweghị ọrịa obi, ihe ize ndụ nke ọrịa obi afọ 10 na-ebelata site na 10.1% 'tupu ọgwụgwọ' ruo 7.7% 'mgbe ọgwụgwọ gasịrị', na mbelata ihe ize ndụ zuru oke nke 2.4% na mbelata ihe ize ndụ nke 23.6%, na-egbochi ihe omume ọrịa obi 2 nde.
N'ikpeazụ, GLP-2 bụ ụdị ọhụrụ nke abụọ agonist nke GIP na GLP-1 ndị na-anabata ya, nke dị oke mkpa na ọgwụgwọ ụdị 2 metabolism na oke ibu. Ọ nwere ike ịkwalite mmepụta insulin nke ọma, na-egbochi secretion glucagon, na-ahazi glucose ọbara nke ọma, belata ihe ize ndụ nke nsogbu, melite ọrụ nke mkpụrụ ndụ beta nke pancreatic, na-egbu oge ọganihu nke metabolism, ma nwee mmetụta cardioprotective. N'ịgwọ oke ibu, ọ nwere ike ibelata oriri oriri nke ọma, iwelata agụụ, ịbawanye afọ ojuju, nyere ndị ọrịa buru ibu aka ịkwụsị ibu ibu, ma belata ihe ize ndụ nke nsogbu ndị metụtara oke ibu. Ọ nwekwara ike melite nguzogide insulin na metabolism lipid. Tụkwasị na nke ahụ, ọ na-egosi ike na ọgwụgwọ nke ọrịa ndị metụtara ọrịa metabolic na-adịghị mma dị ka steatohepatitis na-adịghị egbu egbu, ọrịa apnea na-ehi ụra, na nkụchi obi, ma nwee ike imeziwanye ọtụtụ ihe ngosi metabolic n'otu oge, na-enye atụmatụ ọgwụgwọ zuru oke. Usoro ịgba ntụtụ ya otu ugboro kwa izu dị mma iji ma nwee ike melite nnabata ọgwụgwọ ndị ọrịa. Site n'ịchịkwa glucose na ịdị arọ nke ọbara n'ụzọ dị irè na ibelata ihe ize ndụ nke nsogbu, ọ nwere ike imeziwanye ọnọdụ anụ ahụ nke ndị ọrịa, mee ka ikike ha na-arụ ọrụ kwa ụbọchị na ọdịdị ndụ ha dịkwuo mma, mee ka obi sie ha ike na nchịkwa ọrịa, belata ibu uche ha, na imeziwanye mmekọrịta mmadụ na ibe ya.
Banyere Onye dere ya
Ihe niile a kpọtụrụ aha n'elu bụ Cocer Peptides na-enyocha, dezie ma chịkọta ya.
Onye ode akwụkwọ akụkọ sayensị
Dr. William T. Garvey bụ ọkà mmụta ama ama na onye nyocha jikọtara ya na ọtụtụ ụlọ ọrụ ama ama, gụnyere Mahadum Alabama na Birmingham, Mahadum Aston, na Birmingham Veterans Affairs Medical Center. Nzụlite agụmakwụkwọ ya na ahụmịhe ọkachamara gbasara ọtụtụ ọzụzụ n'ime ngalaba ahụike na sayensị. Dr. Garvey enyela nnukwu onyinye na ngalaba nke endocrinology na metabolism, nutrition and dietetics, biochemistry and molecular bayoloji, yana ọgwụ izugbe na nke ime, na-elekwasị anya na usoro obi na obi. Aghọtala ọrụ ya n'ọtụtụ ebe ma kwanyere ya ùgwù, nke akpọrọ aha ya onye nyocha nke ukwuu na ngalaba Cross-Field maka 2023 na 2024, na-egosipụta mmetụta dị ukwuu na mmetụta nke nyocha ya na mpaghara sayensị sara mbara.
Mmasị nyocha na nka Dr. Garvey gbatịrị akụkụ dị iche iche nke ọrịa metabolic na njikwa ha. O tinyela aka n'ịmụ banyere metabolism metabolism, oke ibu, na nsogbu ndị metụtara ya, na-achọ ikpughe usoro ọgwụgwọ ọhụụ yana melite nsonaazụ onye ọrịa. Ọrụ ya gụnyere nchọpụta sayensị bụ isi, nnwale ụlọ ọgwụ, na ọmụmụ ntụgharị, na-ejikọta ọdịiche dị n'etiti nchọpụta ụlọ nyocha na ngwa ahụike ụwa n'ezie. Site na nyocha ya buru ibu, Dr. Garvey enyela aka na nghọta miri emi nke usoro ndị na-akpata ọrịa metabolic ma nyere aka ịkpụzi ụkpụrụ nduzi ụlọ ọgwụ na usoro ọgwụgwọ na ngalaba nke endocrinology na metabolism. Dr. William T. Garvey depụtara n'akwụkwọ ntụaka [4 ].
