Duocarmycins

A group of pyrroloindole compounds often with additional spirocyclic unit(s) and their analogs originally isolated from STREPTOMYCES. They bind DNA minor grooves with adenine-N3 alkylation activity.

Also Known As:

Networked: 63 relevant articles (0 outcomes, 4 trials/studies)

Bio-Agent Context: Research Results

Experts

1.	Tietze, Lutz F: 10 articles (01/2019 - 10/2006)
2.	Pors, Klaus: 7 articles (01/2022 - 01/2013)
3.	Pruijn, Frederik B: 7 articles (01/2017 - 03/2011)
4.	Tercel, Moana: 7 articles (01/2017 - 03/2011)
5.	Loadman, Paul M: 6 articles (01/2022 - 01/2013)
6.	Schuberth, Ingrid: 6 articles (01/2013 - 10/2006)
7.	Ingelman-Sundberg, Magnus: 5 articles (01/2015 - 06/2013)
8.	Johansson, Inger: 5 articles (01/2015 - 06/2013)
9.	Saito, H: 5 articles (10/2000 - 02/2000)
10.	Patterson, Laurence H: 4 articles (01/2021 - 01/2013)

Related Diseases

1.	Neoplasms (Cancer) 01/01/2023 - "In orthotopic and pseudometastatic mouse models, weekly intravenous treatments with 1 mg/kg vobra duo for 3 weeks delayed tumor growth compared with animals treated with an irrelevant (anti-CD20) duocarmycin-ADC. " 07/01/2014 - "CYP2W1 has proven to metabolize duocarmycin analogs into cytotoxic substances, compounds that in xenografts of CRC cells expressing CYP2W1 completely inhibit tumor growth. " 08/08/2013 - "CYP2W1 was also shown to sensitize proliferating cells to several compounds, demonstrating its potential as a target for tumor selective activation of duocarmycin bioprecursors. " 01/01/2021 - "The duocarmycins belong to a class of agent which has great potential for use in cancer therapy. " 01/01/2021 - "How can the potential of the duocarmycins be unlocked for cancer therapy?"
2.	Pancreatic Neoplasms (Pancreatic Cancer) 04/26/2023 - "They were well tolerated in vivo in mice, indicating low systemic release of their duocarmycin cargo, and in vivo anti-tumor efficacy trials in mouse models of breast and pancreatic cancer gave promising indications of effective tumoral drug release, presumably by in situ bioreductive activation. "
3.	Sarcoma 180 07/01/2000 - "A series of A-ring pyrrole derivatives of duocarmycin bearing beta-(5',6',7'-trimethoxy-2'-indolyl)acryloyl group were synthesized, and evaluated for in vitro anticellular activity against HeLa S3 cells and in vivo antitumor activity against murine sarcoma 180 in mice. " 05/01/2000 - "A series of the C7-substituted A-ring pyrrole derivatives of duocarmycin were synthesized, and evaluated for in vitro anticellular activity against HeLa S3 cells and in vivo antitumor activity against murine sarcoma 180 in mice. " 10/01/1999 - "A series of A-ring pyrrole compounds of duocarmycin bearing 5-membered heteroarylacryloyl groups (thienylacryloyl and pyrrolylacryloyl) and heteroarylcarbonyl groups were synthesized and evaluated for in vitro anticellular activity against HeLa S3 cells and in vivo antitumor activity against murine sarcoma 180 in mice. " 07/29/1999 - "A series of 3-substituted A-ring pyrrole compounds of duocarmycin were synthesized and evaluated for in vitro anticellular activity against HeLa S(3) cells and in vivo antitumor activity against murine sarcoma 180 in mice. " 02/25/1999 - "A series of A-ring pyrrole compounds of duocarmycin bearing 4'-methoxy-beta-heteroarylacryloyl groups were synthesized and evaluated for in vitro anticellular activity against HeLa S3 cells and in vivo antitumor activity against murine sarcoma 180 in mice. "
4.	Hypoxia (Hypoxemia) 01/01/2017 - "A new series of nitro analogues of the duocarmycins was prepared and evaluated for hypoxia-selective anticancer activity. " 10/04/2011 - "Preparation and antitumour properties of the enantiomers of a hypoxia-selective nitro analogue of the duocarmycins." 08/15/2011 - "The effect of sulfonate leaving groups on the hypoxia-selective toxicity of nitro analogs of the duocarmycins." 01/01/2017 - "Influence of a Basic Side Chain on the Properties of Hypoxia-Selective Nitro Analogues of the Duocarmycins: Demonstration of Substantial Anticancer Activity in Combination with Irradiation or Chemotherapy." 09/01/2014 - "The method is sensitive enough to detect adducts at physiologically relevant concentrations, and could have application in the development of nitro analogues of the duocarmycins as hypoxia-activated anticancer prodrugs."
5.	Carcinoma (Carcinomatosis) 01/01/1993 - "Analysis of DNA fragmentation in human uterine cervix carcinoma HeLa S3 cells treated with duocarmycins or other antitumor agents by pulse field gel electrophoresis." 01/01/2016 - "SYD985, a Novel Duocarmycin-Based HER2-Targeting Antibody-Drug Conjugate, Shows Antitumor Activity in Uterine Serous Carcinoma with HER2/Neu Expression." 12/01/1994 - "Duocarmycin A (DUMA) and DU-86, a semisynthetic derivative of duocarmycins (DUMs) and a possible active form of KW-2189, both showed potent cell growth-inhibitory and cell-killing activities against human uterine cervix carcinoma HeLa S3 cells. "

Related Drugs and Biologics

1.	Prodrugs
2.	Immunoconjugates (Immunoconjugate)
3.	Cytochrome P-450 Enzyme System (Cytochrome P450)
4.	Aldehyde Dehydrogenase 1 Family
5.	Vascular Endothelial Growth Factor Receptor-2 (Vascular Endothelial Growth Factor Receptor 2)
6.	hydroxide ion
7.	Aligeron (AS 2)
8.	Pyrroles
9.	DNA (Deoxyribonucleic Acid)
10.	Phosphates (Orthophosphate)

Related Therapies and Procedures

1.	Therapeutics
2.	Drug Therapy (Chemotherapy)