Leland Stanford Junior University

Uti Limited Partnership

Lina Cui

Jianghong Rao

Chang-Chun Ling

Adam Shuhendler

Ping Zhang

Ramprasad Ghosh

Aixia Wang

Provided are embodiments of a small molecule tracer for positron emission tomography (PET) imaging of the enzyme activity of PARP-1 that is responsible for DNA-damage sensing and critically involved in radiation therapy and some chemotherapy response mechanisms. These PARP-1 tracers are derivatives of nicotinamide adenine dinucleotide (NAD), which is the natural substrate for PARP-1. Provided are NAD derivatives that include a linker moiety to which may be attached a label moiety such as a PET detectable fluorine to generate a 6N-(triazo-PEG2-F)-NAD. Especially advantageous for use in PET and MRI scanning detection systems is the attachment of a chelating agent that allows for the formation of a chelator-metal ion complex.

Probe for imaging PARP-1 activity

The present application provides an amphiphilic cyclodextrin-based compound of the formula I: R-G-D-A (I) wherein R is one or more hydrophilic groups; G is one or more linkers; D is a cyclodextrin, and A is one or more aliphatic groups. In certain embodiments, the hydrophilic group is a sugar such as lactose, the linker comprises &#x2014;(CHR'CHO)&#x2014; where R&#x2032; is H or is an alkyl group substituted with &#x2014;(CHR&#x2032;CHO)&#x2014; where n is 1 to 20, typically n=4; the cyclodextrin is a &#x3b2;-cyclodextrin comprising 7 subunits, and the aliphatic groups are Calkyl groups. The compound can be used to enhance water solubility, bioavailability, cellular uptakes of active ingredients used in medicines, cosmetics and foods and other products, for detection, removal and immobilization of pathogenic organisms, toxins, and autoantibodies, and biomarkers on solid matrix, or for molecular biological techniques, such as ELISA, for example.

Amphiphilic cyclodextrin-based glycodendrimers

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Mountain View, CA, United States of America

Lina Cui