Results 191 to 200 of about 745,289 (215)

Abstract 1319: Rapid accumulation of cytotoxic payload in tumor tissue drives BT5528 activity in tumor models

Cancer Research, 2021
Abstract BT5528 was developed as a Bicycle® toxin conjugate to deliver monomethyl auristatin E (MMAE) -payload to EphA2 overexpressing tumors. It consists of a bicyclic peptide targeting the tumor antigen EphA2, linked to the cytotoxin MMAE via a molecular spacer and cleavable linker.
Johanna Lahdenranta, Gavin Bennett, Philip Huxley, Gemma Mudd, Punit Upadhyaya, Phil Jeffrey, Nicholas Keen   +6 more
openaire   +1 more source

SO2 prodrug doped nanorattles with extra-high drug payload for "collusion inside and outside" photothermal/pH triggered - gas therapy.

Biomaterials, 2020
Recent years have witnessed the blooming of gas therapy nanoplatforms, which emerged as a promising area for cancer therapy. However, uncontrolled or inadequate generation of gas and unclear therapeutic mechanisms, which were still regarded as big ...
Qianglan Lu, Tong Lu, Min Xu, Lifang Yang, Yilin Song, Nan Li   +5 more
semanticscholar   +1 more source

Traditional Cytotoxic Agents as Antibody–Drug Conjugate (ADC) Payloads

2019
In the second half of the last century, when the antibody–drug conjugate (ADC) approach was still in its infancy, the choice of potential payloads was based on a small group of cytotoxic molecules already exploited clinically as cancer chemotherapeutic agents.
Ilona Pysz, Paolo Andriollo, David E. Thurston   +2 more
openaire   +1 more source

Systematic Variation of Pyrrolobenzodiazepine (PBD)-dimer Payload Physicochemical Properties Impacts Efficacy and Tolerability of the Corresponding Antibody-Drug Conjugates.

Journal of Medicinal Chemistry, 2020
Cytotoxic pyrrolobenzodiazepine (PBD)-dimer molecules are frequently utilized as payloads for antibody-drug conjugates (ADCs), and many examples are currently in clinical development.
Leanna R Staben, Jinhua Chen, Josefa dela Cruz-Chuh, Geoffrey Del Rosario, M. Go, Jun Guo, S. C. Khojasteh, K. Kozak, Guangmin Li, Carl Ng, Gail D Lewis Phillips, Thomas H. Pillow, Rebecca K Rowntree, J. Wai, Binqing Wei, Keyang Xu, Zijin Xu, Shang‐Fan Yu, Donglu Zhang, P. Dragovich   +19 more
semanticscholar   +1 more source

Development of immunoliposomes containing cytotoxic gold payloads against HER2-positive breast cancers

RSC Medicinal Chemistry
HER2-targeted immunoliposomes with gold payloads exhibit greater accumulation than non-targeted liposomes and free gold compounds and localize in the mitochondria and endoplasmic reticulum leading to cell death at lower nanomolar drug concentrations.
Afruja Ahad, Fatima Aftab, Alexa Michel, Jason S. Lewis, Maria Contel   +4 more
openaire   +2 more sources

Effective extracellular payload release and immunomodulatory interactions govern the therapeutic effect of trastuzumab deruxtecan (T-DXd)

Nature Communications
Trastuzumab deruxtecan (T-DXd) is an antibody-drug conjugate (ADC) targeting HER2, exhibiting significant clinical efficacy in breast cancer (BC) with varying HER2 expression, including HER2-low and HER2-ultralow.
Li-Chung Tsao, John S Wang, Xingru Ma, Sirajbir Sodhi, Joey V. Ragusa, Bushangqing Liu, Jason McBane, Tao Wang, Junping Wei, Congxiao Liu, Xiao Yang, Gangjun Lei, Ivan Spasojevic, Ping Fan, T. Trotter, Michael Morse, H. Lyerly, Z. Hartman   +17 more
semanticscholar   +1 more source

Abstract P062: The CL2A-SN38 linker-payload system conjugated to trastuzumab results in improved cellular cytotoxicity over time relative to T-DM1

Molecular Cancer Therapeutics, 2021
Abstract Background The approved antibody-drug conjugate (ADC) sacituzumab-govitecan (SG) that exploits the topoisomerase I inhibitor SN38, represents a substantial advance in the ADC field. SN38 is the first payload with low nanomolar cytotoxicity. This deviates from current design principles, which utilize ultracytotoxic payloads.
Hardeep Singh, Victor Jeffrey Leyton
openaire   +1 more source

Dumpling GNN: Hybrid GNN Enables Better ADC Payload Activity Prediction Based on the Chemical Structure

International Journal of Molecular Sciences
Antibody–drug conjugates (ADCs) are promising cancer therapeutics, but optimizing their cytotoxic payloads remains challenging. We present DumplingGNN, a novel hybrid Graph Neural Network architecture for predicting ADC payload activity and toxicity ...
Shengjie Xu, Lingxi Xie, Rujie Dai, Zehua Lyu   +3 more
semanticscholar   +1 more source

Dual-payload antibody-drug conjugates: Taking a dual shot.

European journal of medicinal chemistry
Antibody-drug conjugates (ADCs) enable the precise delivery of cytotoxic agents by conjugating small-molecule drugs with monoclonal antibodies (mAbs). Over recent decades, ADCs have demonstrated substantial clinical efficacy.
Junjie Tao, Yilin Gu, Wei Zhou, Yuxi Wang   +3 more
semanticscholar   +1 more source

Cytotoxic Payloads for Antibody – Drug Conjugates

2019
Antibody–drug conjugates (ADCs) represent one of the most promising and exciting areas of anticancer drug discovery. Five ADCs are now approved in the US and EU [i.e., ado-trastuzumab emtansine (Kadcyla™), brentuximab vedotin (Adcetris™), inotuzumab ozogamicin (Besponsa™), gemtuzumab ozogamicin (Mylotarg™) and moxetumomab pasudotox-tdfk (Lumoxiti ...
openaire   +1 more source