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논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 발행연도
- 2015.12
- 수록면
- 168 - 174 (7page)
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초록· 키워드
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The importance of conformational change has recently become a focus for considering the mechanisms by whichinsulin and its receptor combine to achieve an effective ligand-receptor complex. Although the insulin structure boundto its receptor (active structure) is still unknown, there are evidences that conformational change takes place in thecarboxy terminal region of the insulin B-chain on receptor binding. In the present study, we have produced varioussingle-chain insulin analogs where C-terminus of B-chain and N-terminus of A-chain are connected by various shortpeptides. Significant increase of bioactivity was noticed when two pairs of dibasic residues were included as part of theconnecting peptide, indicating that the distance between C-terminus of B-chain and N-terminus of A-chain changes dueto the repulsive force between RR and KR residues, probably further apart than without the RR and KR residues. Proteinmodeling suggests that insulin and single-chain insulin analogs need to open up their receptor-binding pockets for theiractivities. The development of highly active single-chain insulin analog may facilitate the design of novel insulin analogs ornon-peptide alternatives.
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참고문헌 (22)
참고문헌 신청
Blundell, T. L. / 1972 / Insulin : the structure in the cry reflection in chemistry and biology / Adv Protein Chem 26:279~402
Brandenburg, D. / 1971 / Semisynthetic insulin analogues / Biochem J 125:51~52
Chan, W. W. C. / 1968 / A method for the Complete S-sulfonation of cysteine residues in proteins / Biochemistry 7:4247~4254
Chang, S. G. / 1998 / Human insulin production from a novel mini-proinsulin which has high receptor-binding activity / Biochem J 329:631~635
Choi, K. D. / 1997 / The role of highly conserved tetrapeptide sequence of C-peptide in the folding of proinsulin / Bull Korean Chem Soc 18:798~800
Brandenburg, D. / 1971 / Semisynthetic insulin analogues / Biochem J 125:51~52
Chan, W. W. C. / 1968 / A method for the Complete S-sulfonation of cysteine residues in proteins / Biochemistry 7:4247~4254
Chang, S. G. / 1998 / Human insulin production from a novel mini-proinsulin which has high receptor-binding activity / Biochem J 329:631~635
Choi, K. D. / 1997 / The role of highly conserved tetrapeptide sequence of C-peptide in the folding of proinsulin / Bull Korean Chem Soc 18:798~800
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