Antibody–drug conjugates: future directions in clinical and translational strategies to improve the therapeutic index

S Coats, M Williams, B Kebble, R Dixit, L Tseng… - Clinical Cancer …, 2019 - AACR
Since the first approval of gemtuzumab ozogamicin (Mylotarg; Pfizer; CD33 targeted), two
additional antibody–drug conjugates (ADC), brentuximab vedotin (Adcetris; Seattle …

Antibody–drug conjugates: an emerging concept in cancer therapy

RVJ Chari, ML Miller… - Angewandte Chemie …, 2014 - Wiley Online Library
Traditional cancer chemotherapy is often accompanied by systemic toxicity to the patient.
Monoclonal antibodies against antigens on cancer cells offer an alternative tumor‐selective …

Efficacy and safety of rovalpituzumab tesirine in third-line and beyond patients with DLL3-expressing, relapsed/refractory small-cell lung cancer: results from the phase …

D Morgensztern, B Besse, L Greillier… - Clinical Cancer …, 2019 - AACR
Purpose: Although extensive-stage small-cell lung cancer (SCLC) is highly responsive to
first-line therapy, virtually all patients develop resistance with short survival. Rovalpituzumab …

Antibody–drug conjugates for cancer treatment

JM Lambert, A Berkenblit - Annual review of medicine, 2018 - annualreviews.org
The concept of exploiting the specific binding properties of monoclonal antibodies as a
mechanism for selective delivery of cytotoxic agents to tumor cells is an attractive solution to …

Rational approaches, design strategies, structure activity relationship and mechanistic insights for anticancer hybrids

K Nepali, S Sharma, M Sharma, PMS Bedi… - European journal of …, 2014 - Elsevier
A Hybrid drug which comprises the incorporation of two drug pharmacophores in one single
molecule are basically designed to interact with multiple targets or to amplify its effect …

[HTML][HTML] Rovalpituzumab tesirine as a maintenance therapy after first-line platinum-based chemotherapy in patients with extensive-stage–SCLC: results from the …

ML Johnson, Z Zvirbule, K Laktionov, A Helland… - Journal of Thoracic …, 2021 - Elsevier
Abstract Introduction Rovalpituzumab tesirine (Rova-T) is an antibody-drug conjugate
targeting DLL3, an atypical Notch ligand expressed in SCLC tumors. We evaluated the …

From anthramycin to pyrrolobenzodiazepine (PBD)‐containing antibody–drug conjugates (ADCs)

J Mantaj, PJM Jackson, KM Rahman… - Angewandte Chemie …, 2017 - Wiley Online Library
Abstract The pyrrolo [2, 1‐c][1, 4] benzodiazepines (PBDs) are a family of sequence‐
selective DNA minor‐groove binding agents that form a covalent aminal bond between their …

[HTML][HTML] Use of the γ-H2AX assay to monitor DNA damage and repair in translational cancer research

A Ivashkevich, CE Redon, AJ Nakamura, RF Martin… - Cancer letters, 2012 - Elsevier
Formation of γ-H2AX in response to DNA double stranded breaks (DSBs) provides the basis
for a sensitive assay of DNA damage in human biopsies. The review focuses on the …

γH2AX as a marker of DNA double strand breaks and genomic instability in human population studies

V Valdiglesias, S Giunta, M Fenech, M Neri… - … Research/Reviews in …, 2013 - Elsevier
DNA double strand breaks (DSB) are the gravest form of DNA damage in eukaryotic cells.
Failure to detect DSB and activate appropriate DNA damage responses can cause genomic …

H2AX: functional roles and potential applications

JS Dickey, CE Redon, AJ Nakamura, BJ Baird… - Chromosoma, 2009 - Springer
Upon DNA double-strand break (DSB) induction in mammals, the histone H2A variant,
H2AX, becomes rapidly phosphorylated at serine 139. This modified form, termed γ-H2AX, is …