刘刚
1.组合化学与药物先导化合物的发现与优化。 2.多肽与多肽模拟物。
个性化签名
- 姓名:刘刚
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学术头衔:
博士生导师
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学科领域:
药物化学
- 研究兴趣:1.组合化学与药物先导化合物的发现与优化。 2.多肽与多肽模拟物。
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成果数
12
【期刊论文】Anti-epitope antibody, a novel site-directed antibody against human acetylcholinesterase1
刘刚, Xing-mei ZHANG, Gang LIU, Man-ji SUN
Acta Pharmacol Sin 2004 Apr; 25 (4): 431-435,-0001,():
-1年11月30日
AIM: To construct synthetic antigens using the epitope of human brain acetylcholinesterase (hbAChE) for induction and detection of the specific antibody against the epitope, and to analyse the immunogenicity of the antibody. METHODS: The epitope (RTVLVSMNYR, amino acids 143-152) of hbAChE was chemically synthesized, coupled with the carrier protein keyhole limpet hemocyanin (KLH) to construct an artificial immunogen (KLH-epitope), and injected into rabbits to raise antibody. The epitope conjugated with bovine serum albumin (BSA) was used as the detection antigen. The specificity of the antibody was tested by enzyme-linked immunosorbent assay (ELISA) and Western blotting. The immunoreaction between the anti-recombinant human butyrylcholinesterase (rhBChE) polyclonal antibody and the biotinylated-epitope was examined by indirect ELISA. RESULTS: The erythrocyte AChE, the hbAChE, rhBChE and the BSA-epitope all immunoreacted with the anti-epitope antibody against the epitope (143-152) of hbAChE, whereas the torpedo AChE did not. CONCLUSION: The hbAChE, the human erythrocyte AChE and hBChE share the conservative antigenic epitope RTVLVSMNYR, hence they can all immunoreact with the anti-epitope antibody. Since the epitope of hbAChE is less similar with the aligned amino acid sequences of AChE of Torpedo californica or Torpedo marmorata, there is not any immunoreactivity between them. The R, M, and N residues in the epitope seem to be necessary radicals for the conservation of antigenicity.
acetylcholinesterase, butyrylcholinesterase, epitopes, antibodies, enzyme-linked mmunosorbent assay, Western blotting
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【期刊论文】Solid-Phase Synthesis of Muramyl Dipeptide MDP Derivatives Using a Multipin Method
刘刚, Gang Liu, * Shuo-De Zhang, Shu-Quan Xia and Zhen-Kai Ding
Bioorganic & Medicinal Chemistry Letters 10(2000)1361-1363,-0001,():
-1年11月30日
Solid-phase synthetic method of muramyl dipeptide derivatives is reported. A diverse library of muramyl dipeptides could be potentially synthesized by acylation, reductive alkylation, sulfonamide formation, urea formation, N-alkylation, amine addition, or component Ugi reactions based on this method for drug screening.
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【期刊论文】Design and Solid-Phase Synthesis of Multiple Muramyl Dipeptide (MMD)
刘刚, Shuo De ZHANG, Gang LIU*, Su Quan XIA
Chinese Chemical Letters Vol. 12, No.10, pp 887-888, 2001,-0001,():
-1年11月30日
As a non-specific modulator of macrophage, multiplied muramyl dipeptide (MMD) is solid-phase synthesized by application of standard Fmoc chemistry strategy. Tam's multiple antigen system (MAS) is used as our four branched-linker on Lysine.
Multiplied muramyl dipeptide,, multiple antigen system,, macrophage,, solid-phase synthesis
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【期刊论文】Design and Synthesis of Muramyl Dipeptide Cyclic Analogue
刘刚, Suo De ZHANG, Gang LIU*, Su Quan XIA, Ping WU
Chinese Chemical Letters Vol. 13, No.1, pp 17-18, 2002,-0001,():
-1年11月30日
A new conformationally restricted cyclic analogue of muramyl dipeptide was designed and manually synthesized by our "Meshed-Bag Gathered-Bunch" method with a combination of Fmoc, allyl and N-1-(4,4-dimethyl-2,6-dioxocyclo-hexylidene)ethyl chemical protection strategy.
Muramyl dipeptide,, ", Meshed-Bag Gathered-Bunch", method,, cyclic peptides,, solidphase synthesis.,
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刘刚, Gang Liu, † Yemei Fan, † James R. Carlson, ‡ Zhan-Gong Zhao, †, # and Kit S. Lam*
J. Comb. Chem. 2000, 2, 467-474 467,-0001,():
-1年11月30日
In this report we demonstrate that a 1,5-dialkylamino-2,4-dinitrobenzene small molecule library can be generated by a highly efficient solution-phase synthesis method. From this 2485-member library, a series of novel compounds with antibacterial activity were isolated. The significance of this report is that the synthetic scheme is extremely simple, with minimal number of liquid handling steps, and the solvents and reagents left in the final library preparation are fully compatible with cell-based assays.
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刘刚, Suo-De Zhang, † Gang Liu, *, ‡ Shu-Quan Xia, † Ping Wu, † and Liang Zhang‡
J. Comb. Chem. 2002, 4, 131-137,-0001,():
-1年11月30日
A new "Meshed-Bag Gathered-Bunch"technology for the solid-phase synthesis of chemical libraries was developed. Using such technology, we synthesized muramyl dipeptide mimetics including derivatives at the N- and C-terminus, cyclic muramyl dipeptide mimetics, muramyl dipeptide and Tuftsin's analogue conjugates. The advantages of such a method include ease of manufacture, low unit cost of production, the physical encoding method, and the compatibility with both parallel and "split-mix"approaches.
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【期刊论文】Multistep Parallel Synthesis of Substituted 5-Aminobenzimidazoles in Solution Phase
刘刚, Li Li, † Gang Liu, *, † Zhanguo Wang, † Yunyun Yuan, † Chunxu Zhang, ‡ Hongyu Tian, ‡ Xianghong Wu, † and Jing Zhang†
J. Comb. Chem. 2004, 6, 811-821,-0001,():
-1年11月30日
An efficient solution-phase parallel synthesis of multisubstituted 5-aminobenzimidazoles is described. The two fluorine atoms of 1,5-difluoro-2,4-dinitrobenzene (DFDNB) are sequentially and quantitatively replaced by nucleophiles. Simultaneous reduction of aromatic m-dinitro groups by Pd-C/HCOONH4 results in 2,4,5- benzenetriamines, which are continuously condensed with aldehydes to successfully construct the benzimidazole ring without additional oxidants. The free aromatic amino group is further modified by anhydrides, isocyanates, isothiocyanates, and sulfonyl chlorides. All the reactions involved here are highly effective in giving the desired products at room temperature. Four diversity points are introduced in the final products.
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刘刚, Scott R. Nagy, ‡ Gang Liu, § Kit S. Lam, § and Michael S. Denison*, ‡
Biochemistry 2002, 41, 861-868,-0001,():
-1年11月30日
The Ah receptor is a ligand-dependent transcription factor that mediates the biological and toxic effects of polycyclic aromatic hydrocarbons and halogenated aromatic hydrocarbons such as 2,3,7,8- tetrachlorodibenzo-p-dioxin (TCDD, dioxin). Recent evidence also suggests a role for the AhR in normal physiology and development. Although a variety of structurally diverse chemicals are reported to bind to and activate the AhR, the full spectrum of structural chemical classes that can interact with the AhR remains to be elucidated. Large-scale analysis of the ligand binding specificity of the AhR requires the use of a high-throughput AhR bioassay system for chemical screening. We have utilized a recombinant mouse hepatoma cell line (H1G1.1c3) containing a stably integrated TCDD- and AhR-responsive enhanced green fluorescent protein (EGFP) reporter gene to screen a 1,5-dialkylamino-2,4-dinitrobenzene combinatorial chemical library consisting of 155 parental amines and up to 12 090 combinatorial products in less than 7 days for novel AhR agonists. These analyses have identified numerous parental amines as relatively potent inducers of EGFP (with EC50s between 8 and 1000
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【期刊论文】Solid-phase synthesis and antibacterial evaluations of N-demethylvancomycin derivatives
刘刚, Nian-Huan Yao, a Gang Liu, a, * Wen-Yi He, a Changqun Niu, b James R. Carlsonc and Kit S. Lamc
Bioorganic & Medicinal Chemistry Letters 15(2005)2325-2329,-0001,():
-1年11月30日
Twenty-five N-demethylvancomycin derivatives were synthesized on solid-support and their structures were determined by LC-MS/MS. Biological evaluation of these compounds indicated that bulky hydrophobic substituent on vancosamine of N-demethylvancomycin can increase antibacterial activity against vancomycin-resistant Enterococcus faecalis.
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刘刚, Nian-Huan Yao, † Wen-Yi He, † Kit S. Lam, ‡ and Gang Liu*, †
J. Comb. Chem. 2005, 7, 123-129,-0001,():
-1年11月30日
The molecular target of vancomycin, a commonly used glycopeptide antibiotic, is the D-Ala-D-Ala dipeptide subunit on the bacterial cell wall. The molecular basis of interaction between vancomycin and D-Ala-D-Ala in solution is well-known. However, there is no structural data on vancomycin, and its interaction with D-Ala-D-Ala when the drug is tethered to a solid support. In this Article, vancomycin was directly coupled onto TentaGel or PEGA resin through its C terminus. High-resolution magic angle spinning NMR studies indicated that conformation of PEGA bead-bound vancomycin is identical to that of the free drug. Broadening and shifts of the same proton resonances were observed in solution-phase vancomycin or PEGA-bound vancomycin when complexed with Ac2-L-Lys-D-Ala-D-Ala. This study demonstrates that bead-bound molecules can behave the same as solution-phase molecules in terms of molecular interaction with its target molecule, thus validating the on-bead screening approach of the "one-bead-one-compound" combinatorial library method.
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