6obx

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Montbretin A analogue M10-MbA in complex with Human pancreatic alpha-amylaseMontbretin A analogue M10-MbA in complex with Human pancreatic alpha-amylase

Structural highlights

6obx is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 1.3Å
Ligands:, , , , ,
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

AMYP_HUMAN

Publication Abstract from PubMed

Simplified analogues of the potent human amylase inhibitor montbretin A were synthesised and shown to bind tightly, K I = 60 and 70 nM, with improved specificity over medically relevant glycosidases, making them promising candidates for controlling blood glucose. Crystallographic analysis confirmed similar binding modes and identified new active site interactions.

Synthesis of montbretin A analogues yields potent competitive inhibitors of human pancreatic alpha-amylase.,Tysoe CR, Caner S, Calvert MB, Win-Mason A, Brayer GD, Withers SG Chem Sci. 2019 Oct 18;10(48):11073-11077. doi: 10.1039/c9sc02610j. eCollection, 2019 Dec 28. PMID:32206255[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

See Also

References

  1. Tysoe CR, Caner S, Calvert MB, Win-Mason A, Brayer GD, Withers SG. Synthesis of montbretin A analogues yields potent competitive inhibitors of human pancreatic alpha-amylase. Chem Sci. 2019 Oct 18;10(48):11073-11077. doi: 10.1039/c9sc02610j. eCollection, 2019 Dec 28. PMID:32206255 doi:http://dx.doi.org/10.1039/c9sc02610j

6obx, resolution 1.30Å

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OCA