Abstract:
:Much effort has been devoted to targeting agents for imaging and chemotherapy of tumors in cancer research, but there remain significant unmet needs in that area. We have reported a series of preclinical TrkC targeting agents for diagnoses and treatment of metastatic breast cancer; however, with respect to optical imaging, there are limitations to the agents already disclosed. In this work, a TrkC targeting fragment was equipped with a zwitterionic cyanine dye to give a near-infrared probe for in vivo imaging of metastatic breast tumors, with excitation and emission wavelengths of 760 and 780 nm, respectively, and facilitate the aqueous dissolution of the final design. To our delight, the newly developed probe maintained the specific targeting to TrkC+ 4T1 metastatic breast tumor cells as well as the TrkC+ metastatic breast tumor tissue. Upon injection into 4T1-tumor-bearing mice, the tumor was visualized in vivo and ex vivo through the fluorescence signal of the probe. These data seem to encourage further investigations toward developing a TrkC targeting agent for the diagnosis of metastatic breast tumors.
journal_name
Medchemcommjournal_title
MedChemCommauthors
Yang Z,Usama SM,Li F,Burgess K,Li Zdoi
10.1039/c8md00190asubject
Has Abstractpub_date
2018-08-03 00:00:00pages
1754-1760issue
10eissn
2040-2503issn
2040-2511pii
c8md00190ajournal_volume
9pub_type
杂志文章相关文献
MedChemComm文献大全abstract::A series of cyclic peptides were designed and prepared to investigate the physicochemical properties that affect oral bioavailabilty of this chemotype in rats. In particular, the ionization state of the peptide was examined by the incorporation of naturally occurring amino acid residues that are charged in differing r...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/C2MD20203D
更新日期:2012-10-01 00:00:00
abstract::A combinatorial library of 6 × 106 cyclic peptides was synthesized in the one bead-two compound format, with each bead displaying a unique cyclic peptide on its surface and a linear peptide encoding tag in its interior. Screening of the library against K-Ras identified compounds that bound K-Ras with submicromolar aff...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/C2MD20329D
更新日期:2013-02-01 00:00:00
abstract::Bile acids have emerged as strong signaling molecules capable of influencing various biological processes like inflammation, apoptosis, cancer progression and atherosclerosis depending on their chemistry. In the present study, we investigated the effect of major hydrophobic bile acids lithocholic acid (LCA) and deoxyc...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c7md00475c
更新日期:2017-10-31 00:00:00
abstract::To increase the diversity of estrogen receptor (ER) ligands having novel structures and activities, series of selenophene derivatives with a basic side chain (BSC) were synthesized and their biological activity as subtype-selective antagonists for the ER was explored. Compared with the selenophenes without a BSC, most...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c7md00163k
更新日期:2017-05-24 00:00:00
abstract::Tetrahydroisoquinoline (THIQ) is a key structural component in many biologically active molecules including natural products and synthetic pharmaceuticals. Here, we report on the use of transition-metal mediated [2 + 2 + 2] cyclotrimerisation of alkynes to generate tricyclic THIQs with potential to selectively inhibit...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c9md00201d
更新日期:2019-06-27 00:00:00
abstract::Heat shock factor 1 (HSF1) is a transcription factor that plays key roles in cancer, including providing a mechanism for cell survival under proteotoxic stress. Therefore, inhibition of the HSF1-stress pathway represents an exciting new opportunity in cancer treatment. We employed an unbiased phenotypic screen to disc...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c6md00159a
更新日期:2016-08-01 00:00:00
abstract::Herein, we present the design and synthesis of a series of novel heterocyclic derivatives of (-)-borneol and (-)-isoborneol as potent inhibitors of the influenza A virus. All compounds were tested for their toxicity against MDCK cells and for virus-inhibiting activity against the influenza virus A/Puerto Rico/8/34 (H1...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c6md00657d
更新日期:2017-03-03 00:00:00
abstract::Diabetes mellitus is a chronic, complex and multifactorial disease associated characteristically with hyperglycemia. One of the most recently approved antidiabetic drug classes for clinical use are sodium-glucose cotransporter type 2 (SGLT-2) inhibitors. SGLT-2 is a protein expressed in the kidneys, responsible for gl...
journal_title:MedChemComm
pub_type: 杂志文章,评审
doi:10.1039/c8md00183a
更新日期:2018-06-06 00:00:00
abstract::Classical aminoglycoside antibiotics are obsolete or hampered by the emergence of drug resistant bacteria. Recent discoveries of antifungal amphiphilic kanamycins offer new strategies for reviving and repurposing these old drugs. A simple structural modification turns the clinically obsolete antibacterial kanamycin in...
journal_title:MedChemComm
pub_type: 杂志文章,评审
doi:10.1039/c8md00155c
更新日期:2018-04-17 00:00:00
abstract::Recent studies point towards the possible disadvantages of using hydroxamic acid-based zinc-binding groups in HDAC inhibitors due to e.g. mutagenicity issues. In this work, we elaborated on our previously developed Tubathian series, a class of highly selective thiaheterocyclic HDAC6 inhibitors, by replacing the benzoh...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00107c
更新日期:2018-05-18 00:00:00
abstract::A library of 33 compounds was screened for potentiation of the antibiotic FR 900098 against the Francisella tularensis surrogate Francisella novicida. From the screen a highly potent 2-oxazoline adjuvant was discovered capable of potentiating FR 900098 with a 1000-fold reduction in MIC against the Francisella sub-spec...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/C6MD00365F
更新日期:2016-01-01 00:00:00
abstract::Previous studies have demonstrated that natural steroid compounds containing a peroxide bridge exhibited potential anti-hepatitis B virus activity. To continue our research, a simple and regioselective methodology, using Eosin Y as a clean photosensitized oxidation catalyst, was developed for the synthesis of a peroxi...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c6md00344c
更新日期:2016-10-19 00:00:00
abstract::Phenotypic screening is in a renaissance phase and is expected by many academic and industry leaders to accelerate the discovery of new drugs for new biology. Given that phenotypic screening is per definition target agnostic, the emphasis of in silico and in vitro follow-up work is on the exploration of possible molec...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c6md00065g
更新日期:2016-06-01 00:00:00
abstract::It was previously reported that 6β-aminomorphinan derivatives show high affinity for opiate receptors. Novel 6β-heteroarylamidomorphinanes were designed based on the MOR selective antagonist NAP. The 6β-aminomorphinanes were prepared with stereoselective Mitsunobu reaction and subsequently acylated with nicotinic acid...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/C6MD00450D
更新日期:2017-01-01 00:00:00
abstract::A new iron(iii) complex with 5,7-dichloro-2-methyl-8-quinolinol (HClMQ) as ligands, i.e., [Fe(ClMQ)2Cl] (1), was synthesized and evaluated for its anticancer activity. Compared to the HClMQ ligand, complex 1 showed a higher cytotoxicity towards a series of tumor cell lines, including Hep-G2, BEL-7404, NCI-H460, A549, ...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c6md00644b
更新日期:2017-02-01 00:00:00
abstract::Covalent probes and drugs have found widespread use as research tools and clinical agents. Covalent probes are useful because of their increased intracellular potency and because covalent labeling of cellular proteins can be tracked using click chemistry. Covalent drugs, on the other hand, can overcome drug resistance...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c5md00518c
更新日期:2016-04-01 00:00:00
abstract::Recently, there has been an emergence of significant interest in silver-based antimicrobials. Our goal was to develop a radioactive tracer for investigating the biological fate of such compounds. Purified 111Ag was incorporated into the methylated caffeine analogue, IC1 to yield the silver carbene complex designated a...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/C3MD00082F
更新日期:2013-06-01 00:00:00
abstract::Potent, selective, and cell active small molecule kinase inhibitors are useful tools to help unravel the complexities of kinase signaling. As the biological functions of individual kinases become better understood, they can become targets of drug discovery efforts. The small molecules used to shed light on function ca...
journal_title:MedChemComm
pub_type: 杂志文章,评审
doi:10.1039/c7md00510e
更新日期:2017-12-08 00:00:00
abstract::The synthesis, biological evaluation and molecular modeling of a series of pyrrole compounds related to 3,5-dibromo-4-(3,4-dimethoxyphenyl)-1H-pyrrole-2-carboxylic acid that evaluates and optimizes C-4 substituents are reported. The key factor for microtubule depolymerization activity appears to be the presence of an ...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/C2MD20320K
更新日期:2013-01-01 00:00:00
abstract::Receptor mediated gene delivery to the liver offers advantages in treating genetic disorders such as hemophilia and hereditary tyrosinemia type I (HTI). Prior findings demonstrated that tethering the d-galactose head group to cationic lipids directs genes to the liver via asialoglycoprotein receptors (ASGPRs). In our ...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c7md00503b
更新日期:2017-12-06 00:00:00
abstract::The phenol of 1-(3-(1H-imidazol-1-yl)propyl)-3-(4-hydroxy-3-methoxyphenyl)thiourea was selectively carbon-11 labelled to generate [11C]PBD150 in 7.3% yield from [11C]methyl triflate (non-decay corrected; radiochemical purity ≥95%, specific activity = 5.7 Ci/µmol, n=5). Evaluation of [11C]PBD150 by small animal PET ima...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/C5MD00148J
更新日期:2015-06-01 00:00:00
abstract::We previously reported that troponoid compounds profoundly inhibit replication of herpes simplex virus (HSV)-1 and HSV-2 in cell culture, including acyclovir-resistant mutants. Synthesis of 26 alpha-hydroxylated tropolones (αHTs) led to a preliminary structure-activity relationship highlighting the potency of bi-pheny...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c9md00225a
更新日期:2019-05-30 00:00:00
abstract::Previous studies on the large-scale glycomics of more than 3500 human serum samples revealed that the serum glycoproteins of cancer patients often have more dominant and specific glycoforms, namely, branched tri- and tetra-antennary N-glycans, most cancer patient groups than normal control groups. We herein establishe...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00162f
更新日期:2018-06-29 00:00:00
abstract::Twenty-four 14-sulfonamide-tetrandrine derivatives as potential anti-cancer agents were synthesized. The synthetic derivatives were investigated for their cytotoxic activity against human cancer cell lines MDA-MB-231, PC3, WM9, HEL and K562. Initially, the IC50 values (50% inhibitory concentrations) of all of the comp...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00125a
更新日期:2018-05-04 00:00:00
abstract::Based on the scaffold of astemizole, three novel turn-on fluorescent probes (N1-N3) for human ether-a-go-go-related gene (hERG) potassium channel were developed herein. These probes have reasonable fluorescence properties, acceptable cell toxicity, and potent inhibitory activity, all of which contribute to cell imagin...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00562a
更新日期:2019-02-26 00:00:00
abstract::The potential for carbon monoxide-releasing molecules (CO-RMs) as antimicrobials represents an exciting prospective in the fight against antibiotic resistance. Trypto-CORM, a tryptophan-containing manganese(i) carbonyl, is toxic against E. coli following photo-activation. Here, we demonstrate that Trypto-CORM is toxic...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c6md00603e
更新日期:2016-12-06 00:00:00
abstract::Periodontal disease is an oral chronic immune-inflammatory disease highly prevalent worldwide that is initiated by specific oral bacterial species leading to local and systemic effects. The development of new preventive/therapeutic strategies to specifically target oral periodontopathogens without perturbing oral micr...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c9md00074g
更新日期:2019-06-10 00:00:00
abstract::Zampanolide and dactylolide are microtubule-stabilizing polyketides possessing potent cytotoxicity towards a variety of cancer cell lines. Using our understanding of the conformational preferences of the macrolide core in both natural products, we hypothesized that analogues lacking the C17-methyl group would maintain...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c9md00164f
更新日期:2019-04-09 00:00:00
abstract::Transcriptomic phenotypes defined for melanoma have been reported to correlate with sensitivity to various drugs. In this study, we aimed to define a minimal signature that could be used to distinguish melanoma sub-types in vitro, and to determine suitable drugs by which these sub-types can be targeted. By using prima...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/C6MD00466K
更新日期:2017-01-01 00:00:00
abstract::N-Acylethanolamine acid amidase (NAAA) is one of the key enzymes involved in the degradation of fatty acid ethanolamides (FAEs), especially for palmitoylethanolamide (PEA). Pharmacological blockage of NAAA restores PEA levels, providing therapeutic benefits in the management of inflammation and pain. In the current wo...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00432c
更新日期:2018-12-18 00:00:00