Synthesis and evaluation of 2-halogenated-1,1-bis(4-hydroxyphenyl)-2-(3-hydroxyphenyl)-ethylenes as potential estrogen receptor-targeted radiodiagnostic and radiotherapeutic agents

Hanson, Robert N.; Tongcharoensirikul, Pakamas; Barnsley, Kelton; Ondrechen, Mary Jo; Hughes, Alun; DeSombre, Eugene R.

doi:10.1016/j.steroids.2015.01.013

Cited by 2 publications

(1 citation statement)

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“…Details can be found in the references cited and [ 55 ]. The biodistribution of some radioiodinated nonsteroidal estrogens also looks very promising [ 56 ], and some work has been done to advance these and related agents for both imaging and targeted in vivo radiotherapy in preclinical breast cancer models [ 57 , 58 ]. Note is made of other recent reviews covering the development of PET imaging agents for ER [ 47 , 59 ].…”

Section: Fes a Pet Imaging Agent For Estrogen Receptors In Breastmentioning

confidence: 99%

PET Imaging Agents (FES, FFNP, and FDHT) for Estrogen, Androgen, and Progesterone Receptors to Improve Management of Breast and Prostate Cancers by Functional Imaging

Katzenellenbogen

2020

Cancers

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Many breast and prostate cancers are driven by the action of steroid hormones on their cognate receptors in primary tumors and in metastases, and endocrine therapies that inhibit hormone production or block the action of these receptors provide clinical benefit to many but not all of these cancer patients. Because it is difficult to predict which individuals will be helped by endocrine therapies and which will not, positron emission tomography (PET) imaging of estrogen receptor (ER) and progesterone receptor (PgR) in breast cancer, and androgen receptor (AR) in prostate cancer can provide useful, often functional, information on the likelihood of endocrine therapy response in individual patients. This review covers our development of three PET imaging agents, 16α-[18F]fluoroestradiol (FES) for ER, 21-[18F]fluoro-furanyl-nor-progesterone (FFNP) for PgR, and 16β-[18F]fluoro-5α-dihydrotestosterone (FDHT) for AR, and the evolution of their clinical use. For these agents, the pathway from concept through development tracks with an emerging understanding of critical performance criteria that is needed for successful PET imaging of these low-abundance receptor targets. Progress in the ongoing evaluation of what they can add to the clinical management of breast and prostate cancers reflects our increased understanding of these diseases and of optimal strategies for predicting the success of clinical endocrine therapies.

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Section: Fes a Pet Imaging Agent For Estrogen Receptors In Breastmentioning

confidence: 99%

PET Imaging Agents (FES, FFNP, and FDHT) for Estrogen, Androgen, and Progesterone Receptors to Improve Management of Breast and Prostate Cancers by Functional Imaging

Katzenellenbogen

2020

Cancers

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Discovery and Design of Radiopharmaceuticals by In silico Methods

Salahinejad

Winkler

Shiri

2022

CRP

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There has been impressive growth in the use of radiopharmaceuticals for therapy, selective toxic payload delivery, and noninvasive diagnostic imaging of disease. The increasing timeframes and costs involved in the discovery and development of new radiopharmaceuticals have driven the development of more efficient strategies for this process. Computer-aided drug design (CADD) methods and machine learning (ML) have become more effective over the last two decades for drug and materials discovery and optimization They are now fast, flexible, and sufficiently accurate to accelerate the discovery of new molecules and materials. Radiopharmaceuticals have also started to benefit from rapid developments in computational methods. Here we review the types of computational molecular design techniques that have been used for radiopharmaceuticals design. We also provide a thorough examination of success stories in the design of radiopharmaceuticals, and the strengths and weaknesses of the computational methods. We begin by providing a brief overview of therapeutic and diagnostic radiopharmaceuticals and the steps involved in radiopharmaceuticals design and development. We then review the computational design methods used in radiopharmaceutical studies – molecular mechanics, quantum mechanics, molecular dynamics, molecular docking, pharmacophore modelling, and data-driven ML. Finally, the difficulties and opportunities presented by radiopharmaceutical modelling are highlighted. The review emphasizes the potential of computational design methods to accelerate the production of these very useful clinical radiopharmaceutical agents and aims to raise awareness among radiopharmaceutical researchers about computational modelling and simulation methods that can be of benefit to this field.

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Synthesis and evaluation of 2-halogenated-1,1-bis(4-hydroxyphenyl)-2-(3-hydroxyphenyl)-ethylenes as potential estrogen receptor-targeted radiodiagnostic and radiotherapeutic agents

Cited by 2 publications

References 67 publications

PET Imaging Agents (FES, FFNP, and FDHT) for Estrogen, Androgen, and Progesterone Receptors to Improve Management of Breast and Prostate Cancers by Functional Imaging

PET Imaging Agents (FES, FFNP, and FDHT) for Estrogen, Androgen, and Progesterone Receptors to Improve Management of Breast and Prostate Cancers by Functional Imaging

Discovery and Design of Radiopharmaceuticals by In silico Methods

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