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PDBsum entry 6h7z
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References listed in PDB file
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Key reference
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Title
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2-Aminoadipic acid-C(o)-Glutamate based prostate-Specific membrane antigen ligands for potential use as theranostics.
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Authors
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R.Nakajima,
Z.Nováková,
W.Tueckmantel,
L.Motlová,
C.Bařinka,
A.P.Kozikowski.
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Ref.
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ACS Med Chem Lett, 2018,
9,
1099-1104.
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PubMed id
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Abstract
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The design and synthesis of prostate specific membrane antigen (PSMA) ligands
derived from 2-aminoadipic acid, a building block that has not previously been
used to construct PSMA ligands, are reported. The effects of both the linker
length and of an N-substituent of our PSMA ligands were probed, and X-ray
structures of five of these ligands bound to PSMA were obtained. Among the
ligands disclosed herein, 13b showed the highest inhibitory activity for
PSMA. As ligand 13b can readily be radiolabeled since its fluorine atom
is adjacent to the nitrogen atom of its pyridine ring, the use of this and
related compounds as theranostics can be pursued.
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