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1.发明申请公开(公告)号：US20150276755A1
公开(公告)日：2015-10-01
申请号：US14438469
申请日：2013-10-25
Applicant: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH
Inventor： Farid Ghadessy , Chandra Shekhar Verma , David Philip Lane , Jia Wei Siau , Thomas Leonard Joseph , Adelene Yen Ling Sim
CPC classification number: G01N33/6845 , C12Q1/6883 , C12Q2600/156 , G01N2333/4748 , G01N2333/9015 , G01N2500/02
Abstract: The present disclosure provides a method of determining resistance of a biological molecule to inhibition of its interaction with a target molecule by an inhibitor of the biological molecule, the method comprising the steps of: a) co-compartmentalizing a gene encoding the biological molecule with the target molecule, or a gene encoding the biological molecule with a gene encoding the target molecule into an aqueous droplet disposed within a water-in-oil emulsion, and b) assaying for a complex comprising the biological molecule and the target molecule upon expression of the gene encoding the biological molecule and the gene encoding the target molecule, wherein detection of the complex in the presence of the inhibitor indicates that the biological molecule is resistant to inhibition of its interaction with the target molecule by the inhibitor. Also provided are mutated HDM2 ubiquitin ligase polypeptides exhibiting resistance to Nutlin inhibition of p53 binding.
Abstract translation: 本公开提供了一种确定生物分子对生物分子的抑制剂与靶分子的相互作用的抗性的方法，所述方法包括以下步骤：a）将编码生物分子的基因与 目标分子或编码具有编码靶分子的基因的生物分子的基因转化成布置在油包水乳液中的水滴，以及b）在表达后，测定包含生物分子和靶分子的复合物 编码生物分子的基因和编码靶分子的基因，其中在抑制剂存在下检测复合物表明生物分子对抑制剂与靶分子的相互作用的抑制具有抗性。 还提供了显示出对Nutlin抑制p53结合的抗性的突变的HDM2泛素连接酶多肽。
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公开(公告)号：US20160046672A1
公开(公告)日：2016-02-18
申请号：US14778761
申请日：2014-02-28
Applicant: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH
Inventor： Christopher John Brown , David Philip Lane , Soo Tng Quah , Dilraj Lama , Chandra Shekhar Verma
IPC: C07K7/08
CPC classification number: C07K7/08 , A61K38/00 , C07K14/4705
Abstract: The present invention relates to cross-linked peptides that are associated with human eIF4G and bind to eIF4E, uses thereof and pharmaceutical compositions comprising the peptides.
Abstract translation: 本发明涉及与人eIF4G相关并结合eIF4E的交联肽，其用途和包含该肽的药物组合物。
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Patent Agency Ranking
公开(公告)号：US20140142027A1
公开(公告)日：2014-05-22
申请号：US14090057
申请日：2013-11-26
Inventor： Roger W. BEUERMAN , Shouping Liu , Jing Li , Lei Zhou , Chandra Shekhar Verma , Donald Tan
IPC: A01N37/46
CPC classification number: A01N37/46 , A61K31/496 , A61K38/04 , A61K38/16 , C07K14/4723 , A61K2300/00
Abstract: The invention relates to multimeric forms of antimicrobial peptides, for example, defensin peptides. The multimeric forms of defensin peptides possesses antimicrobial activity and may be formulated into antimicrobial compositions, pharmaceutical compositions, eyedrop composition, contact lens solution compositions for coating medical devices and the like. The invention also relates to the use of these multimeric forms of peptides, e.g. multimeric forms of defensin peptides for inhibiting and/or reducing the growth of microorganisms in general, including in a host. The invention further relates to a method of preparing multimers of peptides derived from defensins, for example hBD3. The method includes a composition or combination comprising the multimeric antimicrobial peptides and at least one active pharmaceutical ingredient.
Abstract translation: 本发明涉及多聚体形式的抗微生物肽，例如防御素肽。 防御素肽的多聚体形式具有抗微生物活性，并且可以配制成抗微生物组合物，药物组合物，滴眼剂组合物，用于涂覆医疗装置的隐形眼镜溶液组合物等。 本发明还涉及这些多聚体形式的肽的用途，例如， 用于抑制和/或减少微生物生长的多聚体形式的防御素肽通常包括在宿主中。 本发明还涉及制备衍生自防御素例如hBD3的肽的多聚体的方法。 该方法包括包含多聚体抗微生物肽和至少一种活性药物成分的组合物或组合。
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4.发明申请公开(公告)号：US20250034211A1
公开(公告)日：2025-01-30
申请号：US18712016
申请日：2022-11-23
Applicant: Merck Sharp & Dohme LLC , MSD International GmbH , Agency for Science, Technology and Research
Inventor： Hubert Josien , Arun Chandramohan , Charles William Johannes , Christopher J. Brown , Srinivasaraghavan Kannan , Anthony William Partridge , Chandra Shekhar Verma , Lin Yan , Tsz Ying Yuen
Abstract: The crosslinked peptidomimetic macrocycles disclosed herein comprise an alkene or alkyne staple and a poly-amino acid C-terminal tail. These crosslinked peptidomimetic macrocycles have improved binding to MDM2 and MDMX (aka MDM4), are protease resistant, cell permeable without inducing membrane disruption, and intracellularly activate p53 by binding MDM2 and MDMX thereby antagonizing MDM2 and MDMX binding to p53. These peptidomimetic macrocycles may be useful in anticancer therapies, particularly in combination with chemotherapy or radiation therapy.
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公开(公告)号：US20250042961A1
公开(公告)日：2025-02-06
申请号：US18716399
申请日：2022-12-05
Applicant: MERCK SHARP & DOHME LLC , MSD International GMBH , Agency for Science, Technology and Research
Inventor： Hubert Josien , Arun Chandramohan , Charles William Johannes , Christopher J. Brown , Srinivasaraghavan Kannan , Anthony William Partridge , Chandra Shekhar Verma , Lin Yan , Tsz Ying Yuen
IPC: C07K14/47 , A61K31/203 , A61K31/4745 , A61K31/475 , A61K31/495 , A61K31/675 , A61K31/7048 , A61K31/7068 , A61K33/243 , A61K38/00 , A61K38/12 , A61K38/14 , A61K39/395
Abstract: Disclosed are p53 peptidomimetic macrocycles, each p53 peptidomimetic macrocycle comprising an i, i+4 olefin staple and a polypeptide tail covalently linked to the p53 peptidomimetic macrocycle; an i, i+7 olefin staple and a polypeptide tail covalently linked to the p53 peptidomimetic macrocycle; or, an i, i+7 di-alkyne staple and optionally a polypeptide tail covalently linked to the p53 peptidomimetic macrocycle; wherein the p53 peptidomimetic macrocycle comprises all D-configuration amino acids and the polypeptide tail comprises three to nine amino acids, each amino acid of the polypeptide tail independently having a D-configuration or an L-configuration. The p53 peptidomimetic macrocycles are protease resistant, cell permeable without inducing membrane disruption, and intracellularly activate p53 by binding MDM2 and MDMX, thereby antagonizing MDM2 and MDMX binding to p53. These p53 peptidomimetic macrocycles may be useful in anticancer therapies, particularly in combination with chemotherapy or radiation therapy.
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公开(公告)号：US09220264B2
公开(公告)日：2015-12-29
申请号：US14090057
申请日：2013-11-26
Inventor： Roger W. Beuerman , Shouping Liu , Jing Li , Lei Zhou , Chandra Shekhar Verma , Donald Tan
CPC classification number: A01N37/46 , A61K31/496 , A61K38/04 , A61K38/16 , C07K14/4723 , A61K2300/00
Abstract: The invention relates to multimeric forms of antimicrobial peptides, for example, defensin peptides. The multimeric forms of defensin peptides possesses antimicrobial activity and may be formulated into antimicrobial compositions, pharmaceutical compositions, eyedrop composition, contact lens solution compositions for coating medical devices and the like. The invention also relates to the use of these multimeric forms of peptides, e.g. multimeric forms of defensin peptides for inhibiting and/or reducing the growth of microorganisms in general, including in a host. The invention further relates to a method of preparing multimers of peptides derived from defensins, for example hBD3. The method includes a composition or combination comprising the multimeric antimicrobial peptides and at least one active pharmaceutical ingredient.
Abstract translation: 本发明涉及多聚体形式的抗微生物肽，例如防御素肽。 防御素肽的多聚体形式具有抗微生物活性，并且可以配制成抗微生物组合物，药物组合物，滴眼剂组合物，用于涂覆医疗装置的隐形眼镜溶液组合物等。 本发明还涉及这些多聚体形式的肽的用途，例如， 用于抑制和/或减少微生物生长的多聚体形式的防御素肽通常包括在宿主中。 本发明还涉及制备衍生自防御素例如hBD3的肽的多聚体的方法。 该方法包括包含多聚体抗微生物肽和至少一种活性药物成分的组合物或组合。
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公开(公告)号：US20150246946A1
公开(公告)日：2015-09-03
申请号：US14432729
申请日：2013-10-01
Applicant: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH
Inventor： Thomas Leonard Joseph , Chandra Shekhar Verma , David Phillip Lane , Christopher John Brown
CPC classification number: C07K7/06 , A61K38/00 , A61K38/08 , A61K38/10 , A61K45/06 , C07K7/08 , A61K2300/00
Abstract: By using a phage display derived peptide as an initial template, compounds have been developed that are highly specific against Mdm2/Mdm4. These compounds exhibit greater potency in p53 activation and protein-protein interaction assays than a compound derived from the p53 wild-type sequence. Unlike nutlin, a small molecule inhibitor of Mdm2/Mdm4, the phage derived compounds can arrest cells resistant to p53 induced apoptosis over a wide concentration range without cellular toxicity, suggesting they are highly suitable for cyclotherapy.
Abstract translation: 通过使用噬菌体展示衍生肽作为初始模板，开发了对Mdm2 / Mdm4具有高度特异性的化合物。 与来自p53野生型序列的化合物相比，这些化合物在p53活化和蛋白质 - 蛋白质相互作用测定中表现出更大的效力。 与Mdm2 / Mdm4的小分子抑制剂nutlin不同，噬菌体衍生的化合物可以在宽的浓度范围内阻止对p53诱导的细胞凋亡的细胞，而无细胞毒性，表明它们非常适合于环境疗法。
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