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排序方式: 共有96条查询结果,搜索用时 15 毫秒
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Christos Liolios Christos Sachpekidis Antonios Kolocouris Antonia Dimitrakopoulou-Strauss Penelope Bouziotis 《Molecules (Basel, Switzerland)》2021,26(6)
Multimeric ligands consisting of multiple pharmacophores connected to a single backbone have been widely investigated for diagnostic and therapeutic applications. In this review, we summarize recent developments regarding multimeric radioligands targeting integrin αvβ3 receptors on cancer cells for molecular imaging and diagnostic applications using positron emission tomography (PET). Integrin αvβ3 receptors are glycoproteins expressed on the cell surface, which have a significant role in tumor angiogenesis. They act as receptors for several extracellular matrix proteins exposing the tripeptide sequence arginine-glycine-aspartic (RGD). Cyclic RDG peptidic ligands c(RGD) have been developed for integrin αvβ3 tumor-targeting positron emission tomography (PET) diagnosis. Several c(RGD) pharmacophores, connected with the linker and conjugated to a chelator or precursor for radiolabeling with different PET radionuclides (18F, 64Cu, and 68Ga), have resulted in multimeric ligands superior to c(RGD) monomers. The binding avidity, pharmacodynamic, and PET imaging properties of these multimeric c(RGD) radioligands, in relation to their structural characteristics are analyzed and discussed. Furthermore, specific examples from preclinical studies and clinical investigations are included. 相似文献
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Chen JH Sambol EB Kennealey PT O'Connor RB DeCarolis PL Cory DG Singer S 《Journal of magnetic resonance (San Diego, Calif. : 1997)》2004,171(1):143-150
In cell and tissue samples, water is normally three orders of magnitude more abundant than other metabolites. Thus, water suppression is required in the acquisition of NMR spectra to overcome the dynamic range problem and to recover metabolites that overlap with the broad baseline of the strong water resonance. However, the heterogeneous cellular environment often complicates water suppression and the strong coupling of water to membrane lipids interferes with the NMR detection of membrane associated lipid components. The widely used water suppression techniques including presaturation and double pulsed field gradient selective echo result in more than a 70% reduction in membrane associated lipid components in proton spectra of cells and tissues compared to proton spectra acquired in the absence of water suppression. A water suppression technique based on the combination of selective excitation pulses and pulsed field gradients is proposed to use in the acquisition of high resolution MAS NMR spectra of tissue specimens and cell samples. This pulse sequence methodology enables efficient water suppression for intact cells and tissue samples and eliminates signal loss from cellular metabolites. 相似文献
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Penelope Schobinger-Papamantellos Ch. Routsi J.K. Yakinthos 《Journal of Physics and Chemistry of Solids》1983,44(9):875-877
We have carried out neutron diffraction on a HoCo2Si2 powder sample at 4.2 K. The magnetic structure of this compound is collinear antiferromagnetic with the holmium magnetic moments parallel to the c-axis of the crystal. The magnetic moment value of holmium is 9.85 μB. The magnetic space group is I4/mm'm' (Sh410128) k = 000 The ordering temperature is tn = 12(1) K. 相似文献
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Tb5Ge4 crystallizes in the orthorhombic space group Pnma, and orders antiferromagnetically below TN = 91K. Neutron diffraction powder data at 4.2K reveal a ten-sublattice canted antiferromagnetic arrangment. The structure, which is described by the magnetic space group Pnm'a (Γ8u) with propagation vector k = 0, has three-dimensional components for the atoms in the 8(d) positions, and is almost colinear for the atoms in the 4(c) positions. The magnetic interaction in the layers formed by the Tb atoms in the (010) plane is mainly ferromagnetic, in agreement with the high paramagnetic Curie temperature of 85K. The structure is antiferromagnetically compensated through an antisymmetry center. The main axis of antiferromagnetism is parallel to z. Magnetic phase transitions have been observed by applying a magnetic field in the (010) plane. The structure is stabilized through exchange interactions via conduction electrons. Because of the low symmetry, the Hamiltonian may contain anisotropic terms that result in a canted arrangement. 相似文献
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Direct determinations of the rate constants (cm3/molec · sec) k1, k2, and k3 from 298 to 299°K are reported, using atomic resonance fluorescence in discharge flow systems: 1 One standard deviation. The rate constant k1, which has not been determined previously, was found to possess an insignificant temperature coefficient (EA = (0 ± 700) J/mole) in the range of 299 to 619°K. The present result for k2 agrees well with reinterpreted values from the one previous determination. Measurements of O atom consumption rates and Br atom production rates in the O + Br2 reaction are interpreted to give an estimate of the rate constant k4, which has not been reported previously, at 298°K: k3 has been measured at three temperatures between 299 and 602°K. The present and previous results for k3 were combined to give the following rate expression: 相似文献
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The N atoms in both of the pyrrolidine rings in the title compounds are protonated which prevents the formation of an intramolecular hydrogen bond between the phenol OH group and the ring N atom. This hydrogen bond is thought to be important for maintaining the active shape of these drugs. The positions of the pyrrolidine rings are determined by a chain of hydrogen bonds which link the N+–H through the Cl– back to portions of the same molecule. In both molecules, the carbonyl bond of the ester substituent is aligned parallel to the carbonyl bond of the central amide. The benzanilide fragment is flattened relative to the common conformation found in tabulated structures. Extensive hydrogen bonding is observed due to the presence of solvent and chloride ions. Compound1, 2,6-bis(1-pyrrolidinylmethyl)-4-(4-carboethoxybenzamido)phenol, crystallizes as the dihydrochloride methanol hydrate in the monoclinic space group C2/c with 8 molecules per unit cell and cell constants:a=20.3013,b=11.296(2),c=24.901(5)Å, =93.19(1)°, 4945 unique reflections, 2946 observed,R=0.071. Compound2, 2,6-bis[1-pyrrolidinylmethyl-4-[4-(2-carboethoxyethyl)benzamido]phenol, crystallizes as the dihydrochloride salt in the monoclinic space group P21/c with 4 molecules per unit cell anda=12.903(3),b=16.430(4),c=13.731(2)Å, =103.64(2)°, 5712 unique reflections, 2449 observed,R=0.057. 相似文献
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Cipriani P Smith CY 《Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy》2008,69(2):333-337
Thalidomide is a potent anticancer therapeutic drug whose mechanism of action has not yet been elucidated. In this report, experimental Raman spectroscopy is used to determine and characterize the vibrational frequencies of the drug. These normal modes are then compared to their quantum mechanical counterparts, which have been computed using density functional theory. Upon analysis of the spectra, we found that there was a high level of agreement between the wavenumbers. As such, this spectroscopic technique may be a viable tool for examining the way in which this drug interacts with its target molecules. 相似文献