6p2u

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Structure of Mortalin-NBD with N6-propargyladenosine-5'-diphosphate

Structural highlights

6p2u 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 2Å
Ligands:MG, NO7, PO4
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

GRP75_HUMAN Implicated in the control of cell proliferation and cellular aging. May also act as a chaperone.

Publication Abstract from PubMed

Our early efforts to find a covalent inhibitor of mortalin, a member of the 70 kD heat shock protein (Hsp70) family, led us to solve the structure of the mortalin nucleotide-binding domain (NBD) in complex with N6-propargyladenosine-5'-diphosphate. The acquired structure emphasizes the ability of the nucleotide-binding pocket to accommodate modified ADP compounds. A library of ADP analogues modified at either the 2- or N6-positions of adenosine were screened against the mortalin-NBD. Competitive inhibition and binding assays of the analogues demonstrate that modifications at the 2- or N6-positions have potential to bind and inhibit mortalin uniquely compared to other Hsp70 homologs, and that modifications at the 2-position confer the greatest selectivity in binding and inhibition of the mortalin-NBD. This article is protected by copyright. All rights reserved.

2- and N6-Functionalized Adenosine-5'-diphosphate Analogues for the Inhibition of Mortalin.,Moseng MA, Nix JC, Page RC FEBS Lett. 2019 Jun 8. doi: 10.1002/1873-3468.13475. PMID:31177526[1]

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

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Citations
1 reviews cite this structure
Abrogating the Interaction Between p53 and Mortalin (Grp75/HSPA9/mtHsp70) for Cancer Therapy: The Story so far.
Elwakeel et al. (2022)
0 more
1 other articles
No citations found

References

  1. ↑ Moseng MA, Nix JC, Page RC. 2- and N6-Functionalized Adenosine-5'-diphosphate Analogues for the Inhibition of Mortalin. FEBS Lett. 2019 Jun 8. doi: 10.1002/1873-3468.13475. PMID:31177526 doi:http://dx.doi.org/10.1002/1873-3468.13475

Contents


PDB ID 6p2u

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OCA

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