Abstract:
:Targeting overexpressed receptors on the cancer cells with radiolabeled peptides has become very important in nuclear oncology in the recent years. Peptides are small and have easy preparation and easy radiolabeling protocol with no side-effect and toxicity. These properties made them a valuable tool for tumor targeting. Based on the successful imaging of neuroendocrine tumors with 111 In-octreotide, other receptor-targeting peptides such as bombesin (BBN), cholecystokinin/gastrin analogues, neurotensin analogues, glucagon-like peptide-1, and RGD peptides are currently under development or undergoing clinical trials. The most frequently used radionuclides for tumor imaging are 99m Tc and 111 In for single-photon emission computed tomography and 68 Ga and 18 F for positron emission tomography imaging. This review presents some of the 99m Tc-labeled peptides, with regard to their potential for radionuclide imaging of tumors in clinical and preclinical application.
journal_name
Chem Biol Drug Desjournal_title
Chemical biology & drug designauthors
Rezazadeh F,Sadeghzadeh Ndoi
10.1111/cbdd.13413subject
Has Abstractpub_date
2019-03-01 00:00:00pages
205-221issue
3eissn
1747-0277issn
1747-0285journal_volume
93pub_type
杂志文章,评审abstract::The activation mechanism of G-protein-coupled receptors triggered upon binding of a ligand represents a very important 'conformational switch' in the biological array of signal transduction. However, the molecular and functional details for this activation switch remain unknown. Random saturation mutagenesis data on t...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/j.1747-0285.2008.00630.x
更新日期:2008-03-01 00:00:00
abstract::The flavonoid baicalein has been proven effective in animal models of parkinson's disease; however, the potential biological targets and molecular mechanisms underlying the antiparkinsonian action of baicalein have not been fully clarified. In the present study, the potential targets of baicalein were predicted by in ...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12127
更新日期:2013-06-01 00:00:00
abstract::Electron transport and respiratory pathways are active in both latent and rapidly growing mycobacteria and remain conserved in all mycobacterial species. In mycobacteria, menaquinone is the sole electron carrier responsible for electron transport. Menaquinone biosynthesis pathway is found to be essential for the growt...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/j.1747-0285.2010.00987.x
更新日期:2010-07-01 00:00:00
abstract::A low-dimensional method, based on the use of multiple fusion-based similarity measures, is described for graphically depicting and characterizing relationships among molecules in compound databases. The measures are used to construct multi-fusion similarity maps that characterize the relationship of a set of 'test' m...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/j.1747-0285.2007.00579.x
更新日期:2007-11-01 00:00:00
abstract::The novel naphthoquinone adduct 12,13-Dihydro-N-methyl-6,11,13-trioxo-5H-benzo[4,5]cyclohepta[1,2-b]naphthalen-5,12-imine (hereafter called TU100) was synthesized as a potential chemotherapeutic agent. TU100 arrests tissue culture cells in S and G2/M phases of the cell cycle, followed by rapid induction of apoptosis. ...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/j.1747-0285.2011.01214.x
更新日期:2011-11-01 00:00:00
abstract::Malfunction or overexpression of ErbB receptors (epidermal growth factor receptors) is associated with occurrence and severity of several types of cancer. Initiation of signal cascades by ErbB2 (also known as human epidermal growth factor receptor 2/neu) in breast cancer has been blocked by monoclonal antibodies such ...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12062
更新日期:2013-04-01 00:00:00
abstract::A series of novel naphthalimide derivatives with 4-[4-(3,3-diphenylallyl)piperazin-1-yl]benzoic acid as side chain were designed and synthesized. Their antitumor activities were evaluated against a variety of cancer cell lines in vitro. Preliminary results showed that most of the derivatives had cytotoxic activity com...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/j.1747-0285.2011.01232.x
更新日期:2011-12-01 00:00:00
abstract::Previous reports describe modulators of X-linked inhibitor of apoptosis (XIAP)-caspase interaction designed from the AVPI N-terminal peptide sequence of second mitochondria-derived activator of caspase. A fragment-based drug design strategy was initiated to identify therapeutic non-peptidomimetic antagonists of X-link...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/j.1747-0285.2009.00862.x
更新日期:2009-09-01 00:00:00
abstract::A large number of chemotherapeutic drugs, utilized in the treatment of advanced metastatic clear cell renal cell carcinoma, are typically prone to poor biocompatibility, lack of targeting specificity, and high toxicity, which mostly leads to unsatisfactory clinical outcomes. As a new drug delivery pathway, nanoliposom...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.13652
更新日期:2020-03-01 00:00:00
abstract::PCSK9, a member of the proprotein convertase family, is a key negative regulator of hepatic low-density lipoprotein receptor (LDLR) concentrations in the blood plasma and is associated with the risk of coronary artery disease (CAD). Peptide inhibitors designed to block PCSK9-LDLR interactions could reduce the risk of ...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.13612
更新日期:2019-12-01 00:00:00
abstract::A series of new 1-phenylsulphonyl-2-(1-methylindol-3-yl)-benzimidazole derivatives were designed, synthesized and evaluated as potential inhibitors of tubulin polymerization and anthropic cancer cell lines. Among them, compound 33 displayed the most potent tubulin polymerization inhibitory activity in vitro (IC50 = 1...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12932
更新日期:2017-07-01 00:00:00
abstract::Poria cocos is an edible and medicinal fungus that is widely used in Traditional Chinese Medicines as well as in modern applications. Retinoid X receptor (RXR) occupies a central place in nuclear receptor signaling, and a pharmacological RXR-dependent pathway is involved in myeloid cell function. Here, structural info...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.13610
更新日期:2020-05-01 00:00:00
abstract::High-throughput screening is utilized by pharmaceutical researchers and, increasingly, academic investigators to identify agents that act upon enzymes, receptors, and cellular processes. Screening hits include molecules that specifically bind the target and a greater number of non-specific compounds. It is necessary t...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/j.1747-0285.2010.00957.x
更新日期:2010-05-01 00:00:00
abstract::An application of molecular dynamics and molecular mechanics Poisson-Boltzmann surface area techniques to the prediction of protein kinase inhibitor selectivity is presented. A highly active and selective ERK2 inhibitor was placed in equivalent orientations in five different protein kinases (SRC, LCK, GSK3, JNK3 and A...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/j.1747-0285.2011.01140.x
更新日期:2011-08-01 00:00:00
abstract::Non-secosteroidal ligands are well-known vitamin D receptor (VDR) agonists. In this study, we described a combined QM/MM to define the protein-ligand interaction energy a strong positive correlation in both QM-MM interaction energy and binding free energy against the biological activity. The molecular dynamics simulat...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12754
更新日期:2016-08-01 00:00:00
abstract::Sensing potentially harmful bitter substances in the oral cavity is achieved by a group of (˜) 25 receptors, named TAS2Rs, which are expressed in specialized sensory cells and recognize individual but overlapping sets of bitter compounds. The receptors differ in their tuning breadths ranging from narrowly to broadly t...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12734
更新日期:2016-07-01 00:00:00
abstract::Ecdysteroids initiate the molting process in insects by binding to the ecdysone receptor (EcR), which is a promising target for identifying insect growth regulators. This paper presents an in silico/in vitro screening procedure for identifying new EcR ligands. The three-step virtual screening procedure uses a three-di...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.13772
更新日期:2021-01-01 00:00:00
abstract::This manuscript presents a method for pre-computing and storing molecular features or ''scaffolds'' that can be used for rapid clustering of diverse compound sets within the context of a relational database based on hierarchies of scaffold structures. In addition, a method for rapid structure-based profiling of a larg...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/j.1747-0285.2006.00426.x
更新日期:2006-09-01 00:00:00
abstract::CXCR4 plays a crucial role as a co-receptor with CCR5 for HIV-1 anchoring to mammalian cell membrane and is implicated in cancer metastasis and inflammation. In the current work, we study the relationship of structure and activity of AMD11070 derivatives and other inhibitors of CXCR4 using HQSAR, docking and molecular...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12377
更新日期:2015-02-01 00:00:00
abstract::GSK3β kinase is a noteworthy target for discovery of the drugs that will be used to treat several diseases. In the effort to identify a new inhibitor lead compound, we utilized thermodynamic integration (TI)-molecular dynamics (MD) simulation and kinase assay to investigate the bindings between GSK3β kinase and five c...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12946
更新日期:2017-08-01 00:00:00
abstract::Two series of [1,2,4]triazolo[3,4-a]phthalazine and tetrazolo[5,1-a]phthalazine derivatives bearing substituted benzylpiperazine moieties have been synthesized and evaluated for their positive inotropic activity by measuring left atrium stroke volume on isolated rabbit heart preparations. The majority of the derivativ...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12101
更新日期:2013-05-01 00:00:00
abstract::Voltage-gated sodium channel NaV 1.7 serves as an attractive target for chronic pain treatment. Several venom peptides were found to selectively inhibit NaV 1.7 but with intrinsic problems. Among them, Ssm6a, a recently discovered centipede venom peptide, shows the greatest selectivity against NaV 1.7, but dissociates...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12915
更新日期:2017-06-01 00:00:00
abstract::Quinacrine-the drug based on 9-aminoacridine-failed in clinical trials for prion diseases, whereas it was active in in vitro studies. We hypothesize that aromatic nucleophilic substitution at C9 could be contributing factor responsible for this failure because of the transfer of acridine moiety from quinacrine to abun...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12918
更新日期:2017-06-01 00:00:00
abstract::A facile synthesis of a series of saccharide-binding arylboronic acid derivatives of indoloquinoline was described. The key synthetic steps were polyphosphoric acid-mediated cyclization, chlorinative aromatization, and amidation. Mass spectrometry experiments revealed these synthetic arylboronic acid derivatives of in...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/j.1747-0285.2011.01196.x
更新日期:2011-11-01 00:00:00
abstract::The facile synthesis of core-shell magnetic mesoporous silica nanoparticles (Fe3 O4 @mSiO2 NPs) was reported in aqueous phase using cetyltrimethylammonium bromide as a template under alcohol-free conditions. Compared to the conventional synthesis method for core-shell Fe3 O4 @mSiO2 NPs, the approach in this study is r...
journal_title:Chemical biology & drug design
pub_type: 信件
doi:10.1111/cbdd.12622
更新日期:2015-12-01 00:00:00
abstract::Glucokinase (GK) is the key enzyme controlling levels of blood glucose under normal physiological range, and GK activators are emerging class of drug candidates with promising hypoglycaemic activity. The current study was planned to design, synthesize and evaluate novel N-pyridin-2-yl benzamide analogues as allosteric...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.13423
更新日期:2019-03-01 00:00:00
abstract::Anthranilic diamides is a class of insecticides target at ryanodine receptors (RyRs). To discover potent insecticides targeting at RyRs, a series of novel anthranilic diamides with a diacylhydrazine bridge were designed and synthesized. Their insecticidal activities were evaluated and a preliminary structure-activity ...
journal_title:Chemical biology & drug design
pub_type: 信件
doi:10.1111/cbdd.13349
更新日期:2018-11-01 00:00:00
abstract::We report the first account of a comparative analysis of the binding affinities of nine FDA-approved drugs against subtype B as well as the South African subtype C HIV PR (C-SA). A standardized protocol was used to generate the inhibitor/C-SA PR complexes with the relative positions of the inhibitors taken from the co...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.12063
更新日期:2013-02-01 00:00:00
abstract::The design and evaluation of structural key-type fingerprints is reported that consist of only 10-30 substructures isolated from randomly generated fragment populations of different classes of active compounds. To identify minimal sets of fragments that carry substantial compound class-specific information, fragment f...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/j.1747-0285.2008.00723.x
更新日期:2008-11-01 00:00:00
abstract::Tuberculosis is the deadliest infectious disease affecting humankind with a death toll of approximately 1.7 million people in 2016. The increasing prevalence of multidrug-resistant strains of the causative pathogen, Mycobacterium tuberculosis (Mtb) which results in reduced effectiveness of the current therapies, under...
journal_title:Chemical biology & drug design
pub_type: 杂志文章
doi:10.1111/cbdd.13534
更新日期:2019-08-01 00:00:00