Modular smart molecules for PSMA-targeted chemotherapy

FP Olatunji, M Pun, JW Herman, O Romero… - Molecular cancer …, 2022 - AACR
New targeted chemotherapeutics are urgently needed to minimize off-target toxicity and
reduce the high-mortality rate associated with metastatic prostate cancer. Herein, we report …

Advances in non-radioactive PSMA-targeted small molecule-drug conjugates in the treatment of prostate cancer

M Chen, L Cai, Y Xiang, L Zhong, J Shi - Bioorganic Chemistry, 2023 - Elsevier
Most patients with advanced prostate cancer (PCa) will develop metastatic castration-
resistant prostate cancer (mCRPC) after androgen deprivation therapy, at this time the tumor …

Enhancing the safety and efficacy of PSMA-based small-molecule drug conjugates by linker stabilization and conjugation to transthyretin binding ligand

TU Amin, R Emara, A Pal, H Aldawod… - Journal of Medicinal …, 2022 - ACS Publications
This work describes the enhancement of a novel antitumor therapeutic platform that
combines advantages from small-molecule drug conjugates (SMDCs) and antibody drug …

PSMA-targeted SMART molecules outfitted with SN38

EA Savoy, FP Olatunji, N Mesbahi, RK Ballard… - Bioorganic & Medicinal …, 2024 - Elsevier
Herein, we report the modular synthesis and evaluation of a prostate-specific membrane
antigen (PSMA) targeted small molecule drug conjugate (SMDC) carrying the …

[HTML][HTML] 177Lu-labeled phosphoramidate-based PSMA inhibitors: the effect of an albumin binder on biodistribution and therapeutic efficacy in prostate tumor-bearing …

CJ Choy, X Ling, JJ Geruntho, SK Beyer, JD Latoche… - Theranostics, 2017 - ncbi.nlm.nih.gov
Prostate-specific membrane antigen (PSMA) continues to be an active biomarker for small-
molecule PSMA-targeted imaging and therapeutic agents for prostate cancer and various …

Synthesis and in vitro and in vivo evaluation of urea-based PSMA inhibitors with increased lipophilicity

M Wirtz, A Schmidt, M Schottelius, S Robu, T Günther… - EJNMMI research, 2018 - Springer
Background Several radiolabeled prostate-specific membrane antigen (PSMA) inhibitors
based on the lysine-urea-glutamate (KuE) motif as the pharmacophore proved to be suitable …

Synthesis and Evaluation of ePSMA-DM1: A New Theranostic Small-Molecule Drug Conjugate (T-SMDC) for Prostate Cancer

E Murce, E Spaan, S Beekman, L van den Brink… - Pharmaceuticals, 2023 - mdpi.com
Small-molecule drug conjugates (SMDCs) are compounds in which a therapeutic payload is
conjugated to a targeting vector, for specific delivery to the tumor site. This promising …

DNA-encoded chemical libraries enable the discovery of potent PSMA-ligands with substantially reduced affinity towards the GCPIII anti-target

L Lucaroni, S Oehler, T Georgiev, M Müller… - Chemical …, 2024 - pubs.rsc.org
Prostate-specific membrane antigen (PSMA) is a tumor-associated protein that has been
successfully targeted with small organic ligands and monoclonal antibodies. Pluvicto™ is a …

PSMA-targeting imaging and theranostic agents—Current status and future perspective

S Debnath, N Zhou, M McLaughlin, S Rice… - International journal of …, 2022 - mdpi.com
In the past two decades, extensive efforts have been made to develop agents targeting
prostate-specific membrane antigen (PSMA) for prostate cancer imaging and therapy. To …

Effect of carbohydration on the theranostic tracer PSMA I&T

A Schmidt, M Wirtz, SF Färber, T Osl, R Beck… - ACS …, 2018 - ACS Publications
To investigate the effect of carbohydrate moieties on the pharmacokinetic profile of prostate-
specific membrane antigen (PSMA) inhibitors, carbohydrated derivatives of the established …