Carboranes in drug discovery, chemical biology and molecular imaging

A Marfavi, P Kavianpour, LM Rendina - Nature Reviews Chemistry, 2022 - nature.com
There exists a paucity of structural innovation and limited molecular diversity associated with
molecular frameworks in drug discovery and biomolecular imaging/chemical probe design …

The Rise of Boron-Containing Compounds: Advancements in Synthesis, Medicinal Chemistry, and Emerging Pharmacology

RJ Grams, WL Santos, IR Scorei, A Abad-García… - Chemical …, 2024 - ACS Publications
Boron-containing compounds (BCC) have emerged as important pharmacophores. To date,
five BCC drugs (including boronic acids and boroles) have been approved by the FDA for …

New keys for old locks: Carborane-containing drugs as platforms for mechanism-based therapies

P Stockmann, M Gozzi, R Kuhnert, MB Sárosi… - Chemical Society …, 2019 - pubs.rsc.org
Icosahedral carboranes in medicine are still an emerging class of compounds with potential
beneficial applications in drug design. These highly hydrophobic clusters are potential “new …

Glu-ureido–based inhibitors of prostate-specific membrane antigen: lessons learned during the development of a novel class of low-molecular-weight theranostic …

K Kopka, M Benešová, C Bařinka… - Journal of Nuclear …, 2017 - Soc Nuclear Med
In recent years, several radioligands targeting prostate-specific membrane antigen (PSMA)
have been clinically introduced as a new class of theranostic radiopharmaceuticals for the …

Biological determinants of PSMA expression, regulation and heterogeneity in prostate cancer

MK Bakht, H Beltran - Nature Reviews Urology, 2024 - nature.com
Prostate-specific membrane antigen (PSMA) is an important cell-surface imaging biomarker
and therapeutic target in prostate cancer. The PSMA-targeted theranostic 177Lu-PSMA-617 …

Synthesis and initial biological evaluation of boron-containing prostate-specific membrane antigen ligands for treatment of prostate cancer using boron neutron …

S Wang, C Blaha, R Santos, T Huynh… - Molecular …, 2019 - ACS Publications
Boron neutron capture therapy (BNCT) is a therapeutic modality which has been used for
the treatment of cancers, including brain and head and neck tumors. For effective treatment …

Carborane-containing amino acids and peptides: Synthesis, properties and applications

DA Gruzdev, GL Levit, VP Krasnov… - Coordination Chemistry …, 2021 - Elsevier
Derivatives of dicarba-closo-dodecaboranes and dicarba-nido-undecaboranes (carboranes)
are of increasing interest for modern medicinal chemistry and materials science. The …

Identification of alternative protein targets of glutamate-ureido-lysine associated with PSMA tracer uptake in prostate cancer cells

MK Bakht, JJ Hayward… - Proceedings of the …, 2022 - National Acad Sciences
Prostate-specific membrane antigen (PSMA) is highly overexpressed in most prostate
cancers and is clinically visualized using PSMA-specific probes incorporating glutamate …

Still NAAG'ing after all these years: the continuing pursuit of GCPII inhibitors

JJ Vornov, KR Hollinger, PF Jackson… - Advances in …, 2016 - Elsevier
Nearly two decades ago, Joe Coyle published a single-authored review with the provocative
title, The Nagging Question of the Function of N-Acetylaspartylglutamate (Coyle, 1997). In …

Synthesis of maleimide-functionalized carboranes and their utility in Michael addition reactions

VA Ol'shevskaya, VM Alpatova… - New Journal of …, 2021 - pubs.rsc.org
Carborane maleimides were prepared in good yields through the thermal cyclization of
maleamic acids prepared by the reaction of 3-amino-o-carborane with maleic or 3 …