Site-specific antibody conjugation with payloads beyond cytotoxins

Q Zhou - Molecules, 2023 - mdpi.com
As antibody–drug conjugates have become a very important modality for cancer therapy,
many site-specific conjugation approaches have been developed for generating …

The analysis of key factors related to ADCs structural design

H Tang, Y Liu, Z Yu, M Sun, L Lin, W Liu… - Frontiers in …, 2019 - frontiersin.org
Antibody–drug conjugates (ADCs) have developed rapidly in recent decades. However, it is
complicated to map out a perfect ADC that requires optimization of multiple parameters …

Antibody-mediated delivery of chimeric BRD4 degraders. Part 2: improvement of in vitro antiproliferation activity and in vivo antitumor efficacy

PS Dragovich, TH Pillow, RA Blake… - Journal of Medicinal …, 2021 - ACS Publications
Heterobifunctional compounds that direct the ubiquitination of intracellular proteins in a
targeted manner via co-opted ubiquitin ligases have enormous potential to transform the …

Antibody-mediated delivery of chimeric BRD4 degraders. Part 1: exploration of antibody linker, payload loading, and payload molecular properties

PS Dragovich, TH Pillow, RA Blake… - Journal of Medicinal …, 2021 - ACS Publications
The biological and medicinal impacts of proteolysis-targeting chimeras (PROTACs) and
related chimeric molecules that effect intracellular degradation of target proteins via ubiquitin …

Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα)

PS Dragovich, P Adhikari, RA Blake… - Bioorganic & Medicinal …, 2020 - Elsevier
Chimeric molecules which effect intracellular degradation of target proteins via E3 ligase-
mediated ubiquitination (eg, PROTACs) are currently of high interest in medicinal chemistry …

PROTACs, molecular glues and bifunctionals from bench to bedside: Unlocking the clinical potential of catalytic drugs

M Maneiro, E De Vita, D Conole, CS Kounde… - Progress in medicinal …, 2021 - Elsevier
The vast majority of currently marketed drugs rely on small molecules with an 'occupancy-
driven'mechanism of action (MOA). Therefore, the efficacy of these therapeutics depends on …

[HTML][HTML] Estrogen receptor-α targeting: PROTACs, SNIPERs, peptide-PROTACs, antibody conjugated PROTACs and SNIPERs

A Negi, KK Kesari, AS Voisin-Chiret - Pharmaceutics, 2022 - mdpi.com
Targeting selective estrogen subtype receptors through typical medicinal chemistry
approaches is based on occupancy-driven pharmacology. In occupancy-driven …

Estrogen Receptor α (ERα)-targeting compounds and derivatives: Recent advances in structural modification and bioactivity

WY Guo, SMZ Zeng, GS Deora, QS Li… - Current Topics in …, 2019 - benthamdirect.com
Breast cancer is the most common cancer suffered by female, and the second highest cause
of cancer-related death among women worldwide. At present, hormone therapy is still the …

The development of sulfatase-cleavable linkers for antibody-drug conjugates

J Bargh - 2021 - repository.cam.ac.uk
Abstract Antibody-Drug Conjugates (ADCs) are a rapidly growing class of anticancer agents
comprising a small molecule cytotoxin and a monoclonal antibody (mAb). A covalent linker …

Methods for preparing antibody drug conjugates

T Pillow, P Dragovich - US Patent 11,547,762, 2023 - Google Patents
The subject matter described herein is directed to methods of preparing certain antibody-
drug conjugates (ADCs) wherein the antibody is linked to the drug through a linker, wherein …