250290-80-3Relevant academic research and scientific papers
Stability of His-Phe-Arg-Trp-Pro-Gly-Pro to Leucine Aminopeptidase, Carboxypeptidase Y, and Rat Nasal Mucus, Blood, and Plasma
Shevchenko,Dulov,Andreeva,Nagaev,Shevchenko,Radilov,Myasoedov
, p. 153 - 161 (2016)
The His-Phe-Arg-Trp-Pro-Gly-Pro [ACTH-(6-9)-PGP] peptide was synthesized. Proteolysis of ACTH-(6-9)-PGP and semax (Met-Glu-His-Phe-Pro-Gly-Pro) in the presence of leucine aminopeptidase and carboxypeptidase Y was studied. If the proteolysis of ACTH-(6-9)-PGP is mainly defined by aminopeptidases, the basic metabolite is Trp-Pro-Gly-Pro. Identification of major metabolites of ACTH-(6-9)PGP when incubated with the enzymes in vitro made it possible to evaluate proteolysis pathways of the peptide and prepare necessary amounts of its metabolites for using them as standards. Kinetics of ACTH-(6-9)PGP degradation in the presence of enzyme systems of nasal mucus, blood, and plasma were also explored. It was found that proteolysis of ACTH-(6-9)-PGP in rat blood and plasma occurs mainly under the effect of enzymes whose action is similar to leucine aminopeptidase.
2'-Nitrobenzhydryl Polystyrene Resin: A New Photosensitive Polymeric Support for Peptide Synthesis
Ajayaghosh, A.,Pillai, V. N. Rajasekharan
, p. 5714 - 5717 (1987)
2'-Nitrobenzhydryl polystyrene resin (NBH-resin) was prepared from the commercially available styrene-divinylbenzene cross-linked polymer by a two-step polymer analogous reaction.This resin was employed as a photolytically cleavable polymeric protective support for carboxyl function in amino acids under neutral conditions.The 2'-nitrobenzhydryl resin possesses good stability in 4 N HCl-dioxane required for the deprotection of the temporary Nα-tert-butyloxycarbonyl protecting group.The advantage of the new resin over the already reported benzhydryl resin is its increased acid stability during the Nα deblocking, which permits the peptide synthesis with the commonly available Boc-amino acids.The applicability of this resin is illustrated with the solid-phase synthesis of some model peptides.
Leonurine derivative and application thereof in preparing medicine for preventing or treating ischemic cerebrovascular diseases
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Paragraph 0116-0118, (2021/03/30)
The invention provides a leonurine derivative and application of the leonurine derivative in preparation of a medicine for preventing or treating ischemic cerebrovascular diseases. The leonurine derivative has a structure as shown in a general formula (I), wherein X is selected from O or NH; Y is selected from any one of natural amino acid, substituted amino acid or amino alcohol; Z is selected from H, proline and any substituted proline. Pharmacological experiments prove that the leonurine derivative provided by the invention has the effects of neuroprotection, cerebral infarction area reduction and animal neurobehavioral scoring, and is good in safety, so that the leonurine derivative has important significance for developing novel medicines for preventing or treating ischemic cerebrovascular diseases.
Design, synthesis, and biological evaluation of novel stachydrine derivatives as potent neuroprotective agents for cerebral ischemic stroke
Zhang, Liang,Li, Feng,Hou, Chenhui,Zhu, Sifeng,Zhong, Lili,Zhao, Jianchun,Song, Cai,Li, Wenbao
, p. 2529 - 2542 (2020/05/25)
Stachydrine is a natural product with multiple protective biological activities, including those involved in preventing cancer, ischemia, and cardiovascular disease. However, its use has been limited by low bioavailability and unsatisfactory efficacy. To address this problem, a series of stachydrine derivatives (A1/A2/A3/A4/B1/B2/B3/B4) were designed and synthesized, and biological studies were carried out in vitro and in vivo. When compared with stachydrine, Compound B1 exhibited better neuroprotective effects in vitro, and significantly reduced infarction size in the model of the middle cerebral artery occlusion rat model. Therefore, Compound B1 was selected for further research on ischemic stroke. [Figure not available: see fulltext.].
METHOD FOR PRODUCING RECOMBINANT PEPTIDE AND RESULTANT PEPTIDE
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Paragraph 0046; 0050; 0051, (2020/01/07)
PROBLEM TO BE SOLVED: To provide peptides with reproductive- and sexual-function stimulating activity. SOLUTION: The peptides are represented by general formula: A-Thr-Lys-Pro-B-C-D-X (where A is 0, Met, Met(O), Thr, Ala, His, Phe, Lys, or Gly; B is 0, Gly, Asp, Trp, Gln, Asn, Tyr, Pro, or Arg; C is 0, Arg, Phe, Tyr, Gly, His, Pro, or Lys; D is 0, Val, Gly, Tyr, Trp, Phe, or His; and X is OH, OCH3, or NH2; where 0 represents absence of the amino acid residue; provided that if A≠0 then B ≠0 and/or C≠0 and/or D≠0, if B≠0 then C≠0 and/or D≠0, and peptides Phe-Thr-Lys-Pro-Gly, Thr-Lys-Pro-Pro-Arg and Thr-Lys-Pro-Arg-Gly are excluded). SELECTED DRAWING: Figure 1 COPYRIGHT: (C)2020,JPO&INPIT
Synthesis of cytotoxic cyanobactin, Wewakazole B
Nayani, Kiranmai,Anwar Hussaini
supporting information, p. 1166 - 1169 (2017/03/02)
We report herein the synthesis of cytotoxic cyanobactin, Wewakazole B through an efficient solution-phase approach. The key steps of the synthesis are the macrocyclic lactamization of linear dodecapeptide and construction of two hexapeptides with three di
PYRROLIDINE CARBOXAMIDO DERIVATIVES AND METHODS FOR PREPARING AND USING THE SAME
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Page/Page column 55-56, (2017/01/26)
Pyrrolidine carboxamido derivatives, optical isomers thereof, and salts thereof that are able to prevent, improve, and/or treat inflammatory conditions, including inflammatory bowel disease, and methods for preparing and using the same are provided.
Aggregation propensity of amyloidogenic and elastomeric dipeptides constituents
Kumar, Vikas,Krishna, K. Vijaya,Khanna, Shruti,Joshi, Khashti Ballabh
supporting information, p. 5369 - 5376 (2016/08/05)
This study demonstrates the self-assembly of N- and C-terminal protected dipeptides Phe–Gly and Pro–Gly which were derived from amyloidogenic and elastomeric peptide sequences. These constituents afforded nanostructured supramolecular ensembles through va
Method for producing a recombinant peptide and resultant peptide
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Page/Page column 157, (2016/09/12)
The invention relates to peptides with the following general formula: [in-line-formulae]A-Thr-Lys-Pro-B-C-D-X, where:[/in-line-formulae] A—0, Met, Met (O), Thr, Ala, His, Phe, Lys, Gly B—0, Gly, Asp, Trp, Gln, Asn, Tyr, Pro, Arg C—0, Arg, Phe, Tyr, Gly, His, Pro, Lys D—0, Val, Gly, Tyr, Trp, Phe, His X—OH, OCH3, NH2, where 0 is no amino acid residue, provided that if A≠0, then B and/or C and/or D≠0, if B≠0, then C and/or D≠0, excluding the peptides Phe-Thr-Lys-Pro-Gly (SEQ ID NO: 1), Thr-Lys-Pro-Pro-Arg (SEQ ID NO: 2), Thr-Lys-Pro-Arg-Gly (SEQ ID NO: 3).
Synthesis, docking and anticancer activity studies of D-proline- incorporated wainunuamide
Himaja,Ranjitha,Mali, Sunil V.
, p. 1049 - 1055 (2013/03/13)
D-proline-incorporated wainunuamide - a cyclic octapeptide was synthesized and characterized by FTIR, 1H and 13C NMR and Mass spectral analysis. Molecular docking studies were carried out for the designed cyclic octapeptide and the results showed greater affinity for HPV18-2IOI receptor (HeLa cancer cell line). The synthesized cyclic octapeptide exhibited potent anticancer activity against HeLa cancer cells. Indian Academy of Sciences.
