778648-12-7Relevant academic research and scientific papers
Synthesis and in vitro Evaluation of ADAM10 and ADAM17 Highly Selective Bioimaging Probes
Camodeca, Caterina,Nuti, Elisa,Tosetti, Francesca,Poggi, Alessandro,D'Arrigo, Cristina,Zocchi, Maria Raffaella,Rossello, Armando
, p. 2119 - 2131 (2018)
A disintegrin and metalloproteinase (ADAMs) are membrane-bound metalloproteases responsible for the ectodomain shedding of various transmembrane proteins and play important roles in multiple relevant biological processes. Their altered expression is involved in several pathological conditions, and in particular ADAM10 or ADAM17 overexpression is found in various forms of cancer. To better understand how they are regulated in the cellular context, it is useful to visualize the specific ADAMs pathway by means of molecular imaging techniques. For this purpose, we synthesized bioactive fluorescent probes suitable for cell imaging and that are able to specifically target ADAM10 or ADAM17. Two previously developed ADAM17- and ADAM10-selective inhibitors were chosen for conjugation, respectively, to a Cy5.5 dye and to Cy5.5 and FITC dyes. Herein we also report the synthesis of a gold-labeled compound as an additional bioimaging probe for ADAM10. The newly synthesized ligands were found to be active in vitro on human recombinant ADAM10 and/or ADAM17, showing IC50 values in the nanomolar range and a good selectivity over matrix metalloproteinases (MMPs). Finally, these newly developed probes were successfully used for ADAMs staining on different lymphoma cell lines and lymph node mesenchymal stromal cells.
Anchoring Supramolecular Polymers to Human Red Blood Cells by Combining Dynamic Covalent and Non-Covalent Chemistries
Albertazzi, Lorenzo,Meijer, E. W.,Morgese, Giulia,Palmans, Anja R. A.,Varela-Aramburu, Silvia,de Waal, Bas F. M.
, p. 17229 - 17233 (2020)
Understanding cell/material interactions is essential to design functional cell-responsive materials. While the scientific literature abounds with formulations of biomimetic materials, only a fraction of them focused on mechanisms of the molecular interactions between cells and material. To provide new knowledge on the strategies for materials/cell recognition and binding, supramolecular benzene-1,3,5-tricarboxamide copolymers bearing benzoxaborole moieties are anchored on the surface of human erythrocytes via benzoxaborole/sialic-acid binding. This interaction based on both dynamic covalent and non-covalent chemistries is visualized in real time by means of total internal reflection fluorescence microscopy. Exploiting this imaging method, we observe that the functional copolymers specifically interact with the cell surface. An optimal fiber affinity towards the cells as a function of benzoxaborole concentration demonstrates the crucial role of multivalency in these cell/material interactions.
CONJUGATES OF A CELL-BINDING MOLECULE WITH CAMPTOTHECIN ANALOGS
-
Page/Page column 191, (2021/10/30)
Provided are conjugates of camptothecin analogs with a cell-binding molecule of formula (I), wherein R1, R2, R3, R4, R5, X, L, n, m, T and ----- are defined herein. It also provides methods of making the conjugates of camptothecin analogs to a cell-binding agent, as well as methods of using the conjugates in targeted treatment of cancer, infection, and immunological disorders.
CYTOSTATIC CONJUGATES WITH INTEGRIN LIGANDS
-
Page/Page column 10; 22-23, (2020/06/01)
The present invention relates to novel pharmaceutical compounds comprising of an αvβ3 integrin antagonist, a linking unit comprising of L-Val – L-Pro – L-Asp cleavable by elastase, a polyethyleneglycol (PEG) spacer and a cytotoxic element, to processes for preparation thereof, to the use thereof for treating, preventing or managing diseases and conditions including hyperproliferative disorders such as cancer in humans and other mammals.
A CONJUGATE OF A CYTOTOXIC AGENT TO A CELL BINDING MOLECULE WITH BRANCHED LINKERS
-
, (2021/01/23)
Provided is a conjugation of cytotoxic drug to a cell-binding molecule with a side-chain linker. It provides side-chain linkage methods of making a conjugate of a cytotoxic molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and immunological disorders.
BIOTIN-CONJUGATED N-ACETYL GLYCOL SPLIT HEPARIN
-
Page/Page column 35-36, (2018/11/10)
The present invention relates to N-acetyl glycol split heparin molecules conjugated with biotin having following formula (I), wherein the meanings of the substituents are disclosed in the description. The present invention also relates to such compounds for use as medicaments, in particular for the treatment of diseases and disorders associated with heparanase activity, and to pharmaceutical compositions comprising the same.
PSMA TARGETED FLUORESCENT AGENTS FOR IMAGE GUIDED SURGERY
-
Page/Page column 55, (2019/01/07)
Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.
BONE ACTIVE NITROGEN-CONTAINING BISPHOSPHONATES WITH A NEAR INFRARED FLUORESCENT LABEL
-
Page/Page column 11; 12, (2017/04/11)
A compound of Formula (I) has the structure: wherein G is a straight, branched or cyclic alkyl group having 2 to 50 carbon atoms or an ether group, and R is a fluorescent dye. In some embodiments, G is selected from the group consisting of -(CH2)n- and -(CH2OCH2)m-, wherein n is an integer from 2 to 18, m is an integer from 2 to 18.
METAL/RADIOMETAL-LABELED PSMA INHIBITORS FOR PSMA-TARGETED IMAGING AND RADIOTHERAPY
-
Page/Page column 85, (2015/11/27)
Low-molecular weight gadolinium (Gd)-based MR contrast agents for PSMA- specific Ti-weighted MR imaging are disclosed. The (Gd)-based MR contrast agents exhibit high binding affinity for PSMA and exhibit specific Ti contrast enhancement at PSMA+ cells. Th
