- Novel chemical probes for the investigation of nonribosomal peptide assembly
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Chemical probes were devised and evaluated for the capture of biosynthetic intermediates involved in the bio-assembly of the nonribosomal peptide echinomycin. Putative intermediate peptide species were isolated and characterised, providing fresh insights
- Ho, Y. T. Candace,Leng, Daniel J.,Ghiringhelli, Francesca,Wilkening, Ina,Bushell, Dexter P.,K?stner, Otto,Riva, Elena,Havemann, Judith,Passarella, Daniele,Tosin, Manuela
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Read Online
- Preparation of novel polymer assemblies, "lactosome", composed of poly(L-lactic acid) and poly(sarcosine)
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Novel amphiphilic block polymers composed of poly(L-lactic acid) (PLLA) and poly(sarcosine) (PS) were synthesized by successive polymerizations of lactide and sarcosine N-carboxy anhydride (NCA). The degree of polymerization of each block was controlled b
- Makino, Akira,Yamahara, Ryo,Ozeki, Eiichi,Kimura, Shunsaku
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Read Online
- Development of a High-Affinity Antibody-Binding Peptide for Site-Specific Modification
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Immunoglobulin G (IgG)-binding peptides such as 15-IgBP are convenient tools for the site-specific modification of antibodies and the preparation of homogeneous antibody–drug conjugates. A peptide such as 15-IgBP can be selectively crosslinked to the fragment crystallizable region of human IgG in an affinity-dependent manner via the ?-amino group of Lys8. Previously, we found that the peptide 15-Lys8Leu has a high affinity (Kd=8.19 nM) due to the presence of the γ-dimethyl group in Leu8. The primary amino group required for the crosslinking to the antibodies has, however, been lost. Here, we report the design and synthesis of a novel unnatural amino acid, 4-(2-aminoethylcarbamoyl)leucine (Aecl), which possesses both the γ-dimethyl fragment and a primary amino group. A peptide containing Aecl8 (15-Lys8Aecl) was synthesized and showed a binding affinity ten times higher (Kd=24.3 nM) than that of 15-IgBP (Kd=267 nM). Fluorescein isothiocyanate (FITC)-labeled 15-Lys8Aecl with an N-hydroxy succinimide ester at the side chain of Aecl8 (FITC-15-Lys8Aecl(OSu)) successfully labeled an antibody (trastuzumab, Herceptin) with the fluorophore. This peptide scaffold has both strong binding affinity and crosslinking capability, and could be a useful tool for the selective chemical modification of antibodies with molecules of interest such as drugs.
- Muguruma, Kyohei,Osawa, Rento,Fukuda, Akane,Ishikawa, Naoto,Fujita, Konomi,Taguchi, Akihiro,Takayama, Kentaro,Taniguchi, Atsuhiko,Ito, Yuji,Hayashi, Yoshio
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Read Online
- Design, synthesis and anticancer profile of new 4-(1H-benzo[d]imidazol-1-yl)pyrimidin-2-amine-linked sulfonamide derivatives with V600EBRAF inhibitory effect
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A new series of 4-(1H-benzo[d]imidazol-1-yl)pyrimidin-2-amine linked sulfonamide derivatives 12a–n was designed and synthesized according to the structure of well-established V600EBRAF inhibitors. The terminal sulfonamide moiety was linked to the pyrimidine ring via either ethylamine or propylamine bridge. The designed series was tested at fixed concentration (1 μM) against V600EBRAF, finding that 12e, 12i and 12l exhibited the strongest inhibitory activity among all target compounds and 12l had the lowest IC50 of 0.49 μM. They were further screened on NCI 60 cancer cell lines to reveal that 12e showed the most significant growth inhibition against multiple cancer cell lines. Therefore, cell cycle analysis of 12e was conducted to investigate the effect on cell cycle progression. Finally, virtual docking studies was performed to gain insights for the plausible binding modes of vemurafenib, 12i, 12e and 12l.
- Abdel-Maksoud, Mohammed S.,Mohamed, Ahmed A. B.,Hassan, Rasha M.,Abdelgawad, Mohamed A.,Chilingaryan, Garri,Selim, Samy,Abdel-Bakky, Mohamed S.,Al-Sanea, Mohammad M.
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- Anticancer profile and anti-inflammatory effect of new N-(2-((4-(1,3-diphenyl-1H-pyrazol-4-yl)pyridine sulfonamide derivatives
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A new series of N-(2-((4-(1,3-diphenyl-1H-pyrazol-4-yl)pyridine sulfonamide derivatives 11a-o were designed and synthesized based on our previous works. The new series was tested for its anticancer and anti-inflammatory effects. The anticancer profile of
- Abdel-Maksoud, Mohammed S.,Mohamed Hassan, Rasha,Abdel-Sattar El-Azzouny, Aida,Nabil Aboul-Enein, Mohamed,Oh, Chang-Hyun
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- Triazine-Based Janus G-C Nucleobase as a Building Block for Self-Assembly, Peptide Nucleic Acids, and Smart Polymers
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This communication reports on the utility of a triazine-based self-assembling system, reminiscent of a Janus G-C nucleobase, as a building block for developing (1) supramolecular polymers, (2) peptide nucleic acids (PNAs), and (3) smart polymers. The strategically positioned self-complementary triple H-bonding arrays DDA and AAD facilitate efficient self-assembly, leading to a linear supramolecular polymer.
- Meena, Chhuttan L.,Singh, Dharmendra,Kizhakeetil, Bhavya,Prasad, Manasa,George, Malini,Tothadi, Srinu,Sanjayan, Gangadhar J.
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p. 3186 - 3195
(2021/02/16)
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- Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting V600EBRAF
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Several pyrrolo[2,3-b]pyridine-based B-RAF inhibitors are well known and some of them are currently FDA approved as anticancer agents. Based on the structure of these FDA approved V600EB-RAF inhibitors, two series of pyrrolo[2,3-b]pyridine scaffold were designed and synthesized in attempt to develop new potent V600EB-RAF inhibitors. The 38 synthesized compounds were biologically evaluated for their V600EB-RAF inhibitory effect at single dose (10 μM). Compounds with high percent inhibition were tested to determine their IC50 over V600EB-RAF. Compounds 34e and 35 showed the highest inhibitory effect with IC50 values of 0.085 μM and 0.080 μM, respectively. Headed for excessive biological evaluation, the synthesized derivatives were tested over sixty diverse human cancer cell lines. Only compound 35 emerged as a potent cytotoxic agent against different panel of human cancer cell lines.
- Abdel-Maksoud, Mohammed S.,Ali, Eslam M. H.,Ammar, Usama M.,Mersal, Karim I.,Oh, Chang-Hyun,Yoo, Kyung Ho
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- Imidazothiazole-based potent inhibitors of V600E-B-RAF kinase with promising anti-melanoma activity: biological and computational studies
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A series of imidazothiazole derivatives possessing potential activity against melanoma cells were investigated for molecular mechanism of action. The target compounds were tested against V600E-B-RAF and RAF1 kinases. Compound 1zb is the most potent agains
- Anbar, Hanan S.,El-Gamal, Mohammed I.,Jeon, Hong R.,Kwon, Dow,Lee, Bong S.,Oh, Chang-Hyun,Tarazi, Hamadeh
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p. 1712 - 1726
(2020/10/02)
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- A CONJUGATE OF A TUBULYSIN ANALOG WITH BRANCHED LINKERS
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The present invention relates to the conjugation of a tubulysin analog compound to a cell-binding molecule with branched/side-chain linkers for having better delivery of the conjugate compound and targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of a tubulysin analog molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and autoimmune disease.
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Paragraph 000602; 000603
(2021/03/02)
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- SYNTHETIC INNATE IMMUNE RECEPTOR LIGANDS AND USES THEREOF
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An adjuvant formulation includes a monophosphoryl Lipid A (MPLA) analogue, a Pam3CSK4 analogue, or a muramyldipeptide (MDP) analogue, or combinations thereof. The adjuvant may be formulated in soluble form or in a nanoparticle, such as polylactic glycolic acid nanoparticles. A vaccine formulation comprises the adjuvant formulation and an immunogen. Methods of vaccinating an animal include delivering the vaccine formulation to the animal.
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Paragraph 0055; 0092
(2020/06/10)
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- A CONJUGATE OF A TUBULYSIN ANALOG WITH BRANCHED LINKERS
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The present invention relates to the conjugation of a tubulysin analog compound to a cell-binding molecule with branched/side-chain linkers for having better delivery of the conjugate compound and targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of a tubulysin analog molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and autoimmune disease.
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Page/Page column 12; 217
(2019/07/17)
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- COMBINATION THERAPIES FOR TREATING MUSCULAR DYSTROPHY
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The present disclosure relates to methods of treating Duchenne's Muscular Dystrophy by administering an antisense oligonucleotide that induces exon skipping and a non-steroidal anti- inflammatory compound.
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Page/Page column 84-85
(2019/04/26)
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- COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR
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The present disclosure relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.
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Paragraph 0658-0664
(2018/04/20)
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- A cedar Joan maleic acid salt preparation method
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The invention provides a pixantrone maleate synthesis method which has the advantages of high yield, low impurity content, simple process and easiness in large-scale production. In the method, pyridine-3,4-dicarboxylic acid is used as a starting raw material which reacts with acetic anhydride to obtain pyridine-3,4-dicarboxylic anhydride; the pyridine-3,4-dicarboxylic anhydride conducts an Friedel-Crafts acylation reaction with 1,4-difluorobenzene, and the obtained mixture is subjected to catalytic cyclization to obtain a key intermediate; the intermediate reacts with amino-protected ethylenediamine to obtain protecting group-containing pixantrone; and after that, deprotection and salifying are performed to obtain the target product. In the Friedel-Crafts acylation reaction of the method, an n-hexane solution of sulfuric acid is used as a catalyst, thus the use is convenient, the aftertreatment is simple, and the potential risk in production is eliminated; the Cbz or Fmoc protected ethylenediamine reacts with substituted anthraquinone and then the protecting group is removed through catalytic hydrogenation to obtain pixantrone; the process effectively inhibits side reactions and reduces the impurity content; and meanwhile, the aftertreatment is simplified, and the yield increase is facilitated.
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Paragraph 0052; 0053; 0054
(2017/08/25)
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- Geldanamycin derivative and its preparation and use
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The invention relates to novel geldanamycin derivatives, a preparation method of the geldanamycin derivatives, uses of the geldanamycin derivatives in the preparation of cell killers with cell killing activities, cell proliferation inhibitors and anti-tum
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Paragraph 0049; 0053; 0054
(2018/11/03)
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- Broad-spectrum antiproliferative activity of a series of 6-(4-fluorophenyl)-5-(2-substituted pyrimidin-4-yl)imidazo[2,1-b]thiazole derivatives
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This article described the synthesis and in vitro antiproliferative activities a series of 6-(4-fluorophenyl)-5-(2-substituted pyrimidin-4-yl)imidazo[2,1-b]thiazole derivatives. The nine target compounds were tested for in vitro antitumor effect against a
- Abdel-Maksoud, Mohammed S.,El-Gamal, Mohammed I.,Gamal El-Din, Mahmoud M.,Kwak, Seong-Shin,Kim, Hyun-Il,Oh, Chang-Hyun
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p. 824 - 833
(2016/04/20)
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- FGF21 DERIVATIVES AND USES THEREOF
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The invention relates to a derivative of a FGF21 protein having a cysteine residue at a position corresponding to position 167, 169, 170, 171, 172, 173, 174, 175 and in particular position 180 or position 181 of mature human FGF21 and derivatives thereof having a side chain attached to this cysteine. The FGF21 derivatives of the invention display high potency towards the FGF receptors. The invention also relates to pharmaceutical compositions comprising such FGF21 derivatives and pharmaceutically acceptable excipients, as well as the medical use of the FGF21 derivatives.
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Page/Page column 52
(2016/07/27)
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- HYDRAZINYL-PYRROLO COMPOUNDS AND METHODS FOR PRODUCING A CONJUGATE
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The present disclosure provides conjugate structures and hydrazinyl-pyrrolo compound structures used to produce these conjugates. The disclosure also encompasses methods of production of such conjugates, as well as methods of using the same. Aspects of the present disclosure include a pharmaceutical composition. The pharmaceutical composition includes a conjugate as described herein and a pharmaceutically acceptable excipient. Aspects of the present disclosure include a method of delivering a conjugate to a subject. The method includes administering to the subject an effective amount of a conjugate as described herein. Aspects of the present disclosure include a method of treating a condition in a subject.
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Paragraph 00714; 00715
(2015/06/11)
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- Comparison of alternative nucleophiles for Sortase A-mediated bioconjugation and application in neuronal cell labelling
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The Sortase A (SrtA) enzyme from Staphylococcus aureus catalyses covalent attachment of protein substrates to pentaglycine cross-bridges in the Gram positive bacterial cell wall. In vitro SrtA-mediated protein ligation is now an important protein engineering tool for conjugation of substrates containing the LPXTGX peptide recognition sequence to oligo-glycine nucleophiles. In order to explore the use of alternative nucleophiles in this system, five different rhodamine-labelled compounds, with N-terminal nucleophilic amino acids, triglycine, glycine, and lysine, or N-terminal non-amino acid nucleophiles ethylenediamine and cadaverine, were synthesized. These compounds were tested for their relative abilities to function as nucleophiles in SrtA-mediated bioconjugation reactions. N-Terminal triglycine, glycine and ethylenediamine were all efficient in labelling a range of LPETGG containing recombinant antibody and scaffold proteins and peptides, while reduced activity was observed for the other nucleophiles across the range of proteins and peptides studied. Expansion of the range of available nucleophiles which can be utilised in SrtA-mediated bioconjugation expands the range of potential applications for this technology. As a demonstration of the utility of this system, SrtA coupling was used to conjugate the triglycine rhodamine-labelled nucleophile to the C-terminus of an Im7 scaffold protein displaying Aβ, a neurologically important peptide implicated in Alzheimer's disease. Purified, labelled protein showed Aβ-specific targeting to mammalian neuronal cells. Demonstration of targeting neuronal cells with a chimeric protein illustrates the power of this system, and suggests that SrtA-mediated direct cell-surface labelling and visualisation is an achievable goal. This journal is the Partner Organisations 2014.
- Baer, Samuel,Nigro, Julie,Madej, Mariusz P.,Nisbet, Rebecca M.,Suryadinata, Randy,Coia, Gregory,Hong, Lisa P. T.,Adams, Timothy E.,Williams, Charlotte C.,Nuttall, Stewart D.
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p. 2675 - 2685
(2014/05/06)
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- Design, synthesis, and optimization of balanced dual NK1/NK 3 receptor antagonists
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In connection with a program directed at potent and balanced dual NK 1/NK3 receptor ligands, a focused exploration of an original class of peptidomimetic derivatives was performed. The rational design and molecular hybridization of a novel phenylalanine core series was achieved to maximize the in vitro affinity and antagonism at both human NK1 and NK3 receptors. This study led to the identification of a new potent dual NK1/NK3 antagonist with pKi values of 8.6 and 8.1, respectively.
- Hanessian, Stephen,Jennequin, Thomas,Boyer, Nicolas,Babonneau, Vincent,Soma, Udaykumar,Mannoury La Cour, Clotilde,Millan, Mark J.,De Nanteuil, Guillaume
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supporting information
p. 550 - 555
(2014/06/09)
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- Synthesis and preliminary investigations into norbornane-based amphiphiles and their self-assembly
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A range of norbornane based amphiphiles, which possess a rigid 'kink' in the centre of amphiphiles, were accessed via a concise four step synthesis. The self-assembly properties of these novel compounds were then investigated and the critical aggregation
- Squire, Jennifer S.,Sutti, Alessandra,Durand, Gregory,Conlan, Xavier A.,Henderson, Luke C.
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p. 1895 - 1905
(2013/10/08)
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- NOVEL NEUROKININ 1 RECEPTOR ANTAGONIST COMPOUNDS
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The present invention relates to a compound according to formula (A) wherein n is 1 or 2; R1 and R2 are independently hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, CD3 or halogen; R3 is hydrogen, C(=O)OR7 or C1-4 alkyl optionally substituted with hyd
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Page/Page column 65
(2013/09/12)
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- Synthesis and characterization of highly water-soluble dendrofulleropyrrolidine bisadducts with DNA binding activity
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The synthesis, characterization and DNA binding studies of a series of polycationic fullerene adducts are reported. These cationic species, exhibiting reasonably high water solubility and a heterogeneous distribution of positive charges, can efficiently c
- López, Alejandro Montellano,Scarel, Francesco,Carrero, Noelia Rubio,Vázquez, Ester,Mateo-Alonso, Aurelio,Ros, Tatiana Da,Prato, Maurizio
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supporting information
p. 4450 - 4453
(2012/10/30)
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- Dynamic interface imprinting: High-affinity peptide binding sites assembled by analyte-induced recruiting of membrane receptors
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Come together: Dynamic molecular recognition events at biological membrane receptors play a key role in cell signaling. Artificial membranes have been prepared with embedded synthetic receptors which dynamically arrange and selectively respond to external stimuli, such as, small peptide ligands. Copyright
- Gruber, Benjamin,Balk, Stefan,Stadlbauer, Stefan,Koenig, Burkhard
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supporting information
p. 10060 - 10063,4
(2012/12/12)
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- Dynamic interface imprinting: High-affinity peptide binding sites assembled by analyte-induced recruiting of membrane receptors
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Come together: Dynamic molecular recognition events at biological membrane receptors play a key role in cell signaling. Artificial membranes have been prepared with embedded synthetic receptors which dynamically arrange and selectively respond to external stimuli, such as, small peptide ligands. Copyright
- Gruber, Benjamin,Balk, Stefan,Stadlbauer, Stefan,K?nig, Burkhard
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supporting information
p. 10060 - 10063
(2013/01/15)
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- New imidazo[2,1-b]thiazole derivatives: Synthesis, in vitro anticancer evaluation, and in silico studies
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A series of 18 new imidazo[2,1-b]thiazole derivatives was synthesized. Their in vitro antiproliferative activities against A375P human melanoma cell line and NCI-60 cell line panel were tested. Compounds 15, 16, 18, 22, 26-28, and 31 showed superior poten
- Park, Jin-Hun,El-Gamal, Mohammed I.,Lee, Yong Sup,Oh, Chang-Hyun
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scheme or table
p. 5769 - 5777
(2012/01/05)
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- Selective organic functionalization of graphene bulk or graphene edges
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Graphene sheets have been functionalized with a PAMAM dendron, finding that graphene can be efficiently functionalized all over the surface, or only at the edges, depending on the reactions used in the functionalization process.
- Quintana, Mildred,Montellano, Alejandro,Del Rio Castillo, Antonio Esau,Tendeloo, Gustaaf Van,Bittencourt, Carla,Prato, Maurizio
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supporting information; experimental part
p. 9330 - 9332
(2011/10/03)
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- Photoresponsive soft nanotubes for controlled guest release
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Light, transformation, release! Self-assembly of a simple amphiphile with an azobenzene unit produced an organic nanotube with 20 nm inner diameter. The trans-to-cis photoisomerization of the azobenzene unit within the solid bilayer membranes of the nanot
- Kameta, Naohiro,Tanaka, Asuka,Akiyama, Haruhisa,Minamikawa, Hiroyuki,Masuda, Mitsutoshi,Shimizu, Toshimi
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supporting information; scheme or table
p. 5251 - 5255
(2011/07/07)
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- Synthesis of new 6-(4-Fluorophenyl)-5-(2-substituted pyrimidin-4-yl) imidazo[2,1-b] thiazole derivatives and their antiproliferative activity against melanoma cell line
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Synthesis of a new series of pyrimidinyl-imidazo[2,1-b]thiazole derivatives is described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the pyrimidinyl ring side chain was investigated.
- Park, Jin-Hun,Oh, Chang-Hyun
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experimental part
p. 2854 - 2860
(2012/04/17)
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- Parallel synthesis of an oligomeric imidazole-4, 5-dicarboxamide library
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A library of oligomeric compounds was synthesized based on the imidazole-4, 5-dicarboxylic acid scaffold along with amino acid esters and chiral diamines derived from amino acids. The final compounds incorporate nonpolar amino acids (Leu, Phe, Trp), polar amino acids (Ser, Asp, Arg), and neutral amino acids (Gly, Ala), and were designed to be useful in screening for inhibitors of protein-protein interactions. Many of the protected and deprotected oligomers show evidence of conformational isomers persistent at room temperature in aqueous solution. A total of 317 final oligomers, out of 441 targeted compounds, were obtained in high analytical purity and of sufficient quantity to submit them for high-throughput screening as part of the NIH Roadmap.
- Xu, Zhigang,DiCesare, John C.,Baures, Paul W.
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supporting information; experimental part
p. 248 - 254
(2010/08/19)
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- FATTY ACID ACETYLATED SALICYLATES AND THEIR USES
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The invention relates to Fatty Acid Acetylated Salicylate Derivatives; compositions comprising an effective amount of a Fatty Acid Acetylated Salicylate Derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a Fatty Acid Acetylated Salicylate Derivative.
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Page/Page column 115
(2010/03/04)
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- POLYBASIC BACTERIAL EFFLUX PUMP INHIBITORS AND THERAPEUTIC USES THEREOF
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Disclosed are compounds having polybasic functionalities. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.
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Page/Page column 57; 58
(2009/01/24)
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- Effective methods for the biotinylation of azamacrocycles
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(Chemical Equation Presented) The biotin-(strept)avidin interaction remains a gold standard of model biological recognition events. The biotinylation of azamacrocycles permits the investigation of signal transduction between this recognition event and the
- Krivickas, Sara J.,Tamanini, Emiliano,Todd, Matthew H.,Watkinson, Michael
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p. 8280 - 8289
(2008/02/13)
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- Selective synthesis of carbamate protected polyamines using alkyl phenyl carbonates
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Utilising alkyl phenyl carbonates, an economical, practical and versatile method for selective Boc, Cbz and Alloc protection of polyamines has been developed. This method allows Boc, Cbz and Alloc protection of primary amines in the presence of secondary amines by reaction of the polyamines with the alkyl phenyl carbonates. Also, this method allows mono carbamate protection of simple symmetrical aliphatic α,ω-alkanediamines in high yields with respect to the diamine. Finally, the method allows selective carbamate protection of a primary amine located on a primary carbon in the presence of a primary amine located on a secondary or a tertiary carbon in excellent yields.
- Pittelkow, Michael,Lewinsky, Rasmus,Christensen, Jorn Bolstad
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p. 2195 - 2202
(2007/10/03)
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- Design and synthesis of peptides passing through the blood-brain barrier
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The blood-brain barrier (BBB) is a highly selective membranous barrier regulating the transport of substances in blood into the brain parenchyma. At present, delivery of biologically active peptides or peptide drugs into the brain is quite an important subject from the standpoint of chemotherapy for brain diseases H-MeTyr-Arg-MeArg-D-Leu-NH(CH2)8NH2 termed 001-C8 was first synthesized to elucidate the structural specificity of peptides for passing through the BBB. The Na-methylamino acid and D-amino acid residues were appropriately situated in this peptide to protect against the digestion by peptidase. Furthermore, a number of basic peptides were prepared as 001-C8 analogs for studying the relationship between structure and BBB permeability of peptides.
- Wakamiya, Tateaki,Kamata, Makoto,Kusumoto, Shoichi,Kobayashi, Hiroyuki,Sai, Yoshimichi,Tamai, Ikumi,Tsuji, Akira
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p. 699 - 709
(2007/10/03)
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- SYNTHESIS AND BIOLOGICAL ACTIVITIES OF NEW ANALOGUES OF β-CASOMORPHINE-5*
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Four new analogues of β-casomorphine-5 modified at the C-end by modifiers based on ethylenediamine and glycine residues have been synthesized. the opioid and analgesic activities of the peptides obtained comparison with β-casomorphine-5 and morphine are discussed.
- Sobirov, M.M.,Khalikov, Sh.Kh.,Saidov, S.S.,Kodirov, M.Z.,Zaitsev, S.V.,et al.
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p. 397 - 405
(2007/10/02)
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- Modified Amino Acids and Peptides. Part 2. A Convenient Conversion of Amino and Peptide Alcohols into Amines.
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A convenient general method for the conversion of N-protected amino and peptide alcohols into amines is described.The hydroxyl group of the alcohols was replaced by an azido group and a substituted amino group after activation through mesylation.Hydrogenation of the N-protected amino azides afforded optically active monoprotected diamines or free 1,2-diamines depending on the N-protecting group.Selective reduction of the azido group in the presence of a benzyloxycarbonyl group was performed in high yield using sodium borohydride in the presence of 10percent palladium on charcoal.
- Kokotos, George,Constantinou-Kokotou, Violetta
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p. 3117 - 3132
(2007/10/02)
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- Polymerizable ethylenically unsaturated amide compounds
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Compounds useful in making crosslinkable polymers having the formula (I): STR1 wherein R is hydrogen or methyl; R1 is cyano or STR2 wherein R2 is alkyl; Z is --X--R3 --X-- or STR3 wherein each --X-- is --O-- or --NR4
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