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PSMA 6S1X 3d printed

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PSMA 6S1X 3d printed
PSMA 6S1X 3d printed

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PSMA 6S1X

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Product Description
Prostate-specific membrane antigen (PSMA) is an excellent biomarker for the early diagnosis of prostate cancer progression and metastasis. The most promising PSMA-targeted agents in the clinical phase are based on the Lys-urea-Glu motif, in which Lys and Glu are α-(l)-amino acids. In this study, we aimed to determine the effect of β- and γ-amino acids in the S1 pocket on the binding affinity for PSMA. We synthesized and evaluated the β- and γ-amino acid analogues with ( )- or ( )-configuration with keeping α-(l)-Glu as the S1'-binding pharmacophore. The structure-activity relationship studies identified that compound 13c , a β-amino acid analogue with ( )-configuration, exhibited the most potent PSMA inhibitory activity with an IC 50 value of 3.97 nM. The X-ray crystal structure of PSMA in complex with 13c provided a mechanistic basis for the stereochemical preference of PSMA, which can guide the development of future PSMA inhibitors.
Tags
61SX PMSA
Details
What's in the box:
exsml_PSMA_6S1X_max_v4_x36_4cm
Dimensions:
4.21 x 3.2 x 2.85 cm
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1.66 x 1.26 x 1.12 inches
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Rating:
Mature audiences only.
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