資源 » 參考數(shù)據(jù)庫 » 客戶發(fā)表文獻(xiàn)

至今，GenScript的服務(wù)及產(chǎn)品已被Cell, Nature, Science, PNAS等1300多家生物醫(yī)藥類雜志引用近萬次，處于行業(yè)領(lǐng)先水平。NIH、哈佛、耶魯、斯坦福、普林斯頓、杜克大學(xué)等約400家全球著名機(jī)構(gòu)使用GenScript的基因合成、多肽服務(wù)、抗體服務(wù)和蛋白服務(wù)等成功地發(fā)表科研成果，再次證明GenScript 有能力幫助業(yè)內(nèi)科學(xué)家Make research easy.

A potentiator of orthosteric ligand activity at GLP-1R acts via covalent modification.

Nat Chem Biol.. 2014-08; 10(8):629-31

Nolte WM, Fortin JP, Stevens BD, Aspnes GE, Griffith DA, Hoth LR, Ruggeri RB, Mathiowetz AM, Limberakis C, Hepworth D, Carpino PA. Worldwide Medicinal Chemistry, Pfizer PharmaTherapeutics Research and Development, Cambridge, Massachusetts, USA USA.

Products/Services Used	Details	Operation

摘要

We report that 4-(3-(benzyloxy)phenyl)-2-ethylsulfinyl-6-(trifluoromethyl)pyrimidine (BETP), which behaves as a positive allosteric modulator at the glucagon-like peptide-1 receptor (GLP-1R), covalently modifies cysteines 347 and 438 in GLP-1R. C347, located in intracellular loop 3 of GLP-1R, is critical to the activity of BETP and a structurally distinct GLP-1R ago-allosteric modulator, N-(tert-butyl)-6,7-dichloro-3-(methylsulfonyl)quinoxalin-2-amine. We further show that substitution of cysteine for phenylalanine 345 in the glucagon receptor is sufficient to confer sensitivity to BETP.