Nine homotrifunctional cross-linking reagents are presented. Their synthesis and chemical properties as well as their characterization by classical mechanical conformational searching techniques is reported. Mixed Low Mode and Monte Carlo searching techniques were used to exhaustively sample the OPLS2005/GBSA(water) potential energy surface of trisubstituted cyclohexane and benzene derivatives of C3 symmetry. Geometric structure, molecular length, and hydrogen-bonding patterns were analyzed. Nonaromatic compounds exhibited exclusively chair conformations at low energies, with a preference for axial or equatorial arms depending upon the presence of additional ring substituent Me groups. Increasing chain length often resulted in overall shorter molecular length due to additional chain flexibility. These results were consistent with one- and two-dimensional temperature-dependent NMR studies.
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http://dx.doi.org/10.1021/jo0709293 | DOI Listing |
Commun Biol
December 2024
Mayo Clinic, Rochester, MN, USA.
Antibody-drug conjugates (ADCs) are increasingly used in clinic for multiple indications and may improve upon the activity of parental antibodies by delivering cytotoxic payloads into target cells. This activity is predicated upon internalization to release the cytotoxic payloads intracellularly. Since binding of ADCs to their cell surface targets does not guarantee their internalization, we hypothesize that proteolysis targeting chimeras (PROTACs) could improve the activity of ADCs through forced internalization.
View Article and Find Full Text PDFAnticancer Res
January 2025
Center for Cancer Genomics and Precision Medicine, Osaka University Hospital, Osaka, Japan.
Anticancer Res
January 2025
Department of Thoracic Oncology, Osaka Habikino Medical Center, Osaka, Japan.
Background/aim: The clinical benefits of durvalumab consolidation therapy following concurrent chemoradiotherapy (CCRT) with daily low-dose carboplatin in elderly patients with unresectable, locally advanced non-small cell lung cancer (NSCLC) remain unclear.
Patients And Methods: This was a single-institution retrospective cohort study. We analyzed the medical records of consecutive patients diagnosed with NSCLC who received CCRT with daily low-dose carboplatin from April 2014 to March 2021.
PLoS One
December 2024
Hubei Province Key Laboratory of Occupational Hazard Identification and Control, Institute of Infection, Immunology and Tumor Microenvironment, School of Medicine, Wuhan University of Science and Technology, Wuhan, Hubei, China.
The effectiveness of chemotherapy involving 5-fluorouracil and cisplatin (DDP) for the treatment of colorectal cancer (CRC) is often limited due to the emergence of drug resistance. An increasing body of research highlights the crucial role of abnormally expressed microRNAs (miR/miRNAs) in fostering drug resistance in various types of cancer. The present study was the first to explore the potential roles and mechanisms of the small non-coding RNA miR-1247-3p in CRC, particularly its association with DDP resistance in CRC.
View Article and Find Full Text PDFFront Biosci (Landmark Ed)
November 2024
Department of Breast Surgery, The First People's Hospital of Foshan, 528100 Foshan, Guangdong, China.
Objective: The current study aimed to develop an experimental approach for the direct co-culture of three-dimensional breast cancer cells using single-cell RNA sequencing (scRNA-seq).
Methods: The following four cell culture groups were established in the Matrigel matrix: the untreated Michigan Cancer Foundation (MCF)-7 cell culture group, the MCF-7 cell culture plus cisplatin group, the untreated co-culture group, and the cell co-culture plus cisplatin group. For cell co-culture, MCF-7 cells, human mammary fibroblasts, and human umbilical vein endothelial cells were mixed at a ratio of 1:1:1.
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