5-(carbamoylamino)-N-[4-(hydroxymethyl)phenyl]pentanamide

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 5-(carbamoylamino)-N-[4-(hydroxymethyl)phenyl]pentanamide
• 化学式: C₁₃H₁₉N₃O₃
• 分子量: 265.31
• InChiKey: MJGNLEMQJAYMTO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.4
• 重原子数：
  19
• 可旋转键数：
  7
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  104
• 氢给体数：
  4
• 氢受体数：
  3

文献信息

• Anti-MSR1 antibodies and methods of use thereof
  申请人：REGENERON PHARMACEUTICALS, INC.

  公开号：US11377502B2

  公开（公告）日：2022-07-05

  Provided herein are antibodies and antigen-binding fragments that bind MSR1 and methods of use thereof. According to certain embodiments, the antibodies bind human MSR1 with high affinity. In certain embodiments, the antibodies bind MSR1 without blocking, or blocking less than 90%, of modified LDL binding to MSR1. In some embodiments, the antibodies bind cell surface expressed-MSR1 and are internalized. The antibodies of the invention may be fully human antibodies. The invention includes anti-MSR1 antibodies, or antigen-binding fragments thereof, conjugated to drugs or therapeutic compounds.

  本文提供了结合 MSR1 的抗体和抗原结合片段及其使用方法。根据某些实施方案，抗体以高亲和力结合人 MSR1。在某些实施方案中，抗体结合 MSR1 而不阻断或阻断少于 90% 的修饰低密度脂蛋白与 MSR1 的结合。在某些实施方案中，抗体与细胞表面表达的 MSR1 结合并被内化。本发明的抗体可以是全人源抗体。本发明包括与药物或治疗化合物结合的抗MSR1抗体或其抗原结合片段。
• PEPTIDOMIMETIC COMPOUNDS AND ANTIBODY-DRUG CONJUGATES THEREOF
  申请人：Genentech, Inc.

  公开号：EP3082875B1

  公开（公告）日：2020-11-25
• BIOMOLECULE CONJUGATES
  申请人：CELGENE CORPORATION

  公开号：US20170360952A1

  公开（公告）日：2017-12-21

  The present invention relates to biomolecule conjugates which comprise a biomolecule wherein at least one non-natural amino acid (NNAA) is integral to the structure of the biomolecule and wherein the NNAA is a point of attachment of a linker to which a payload, particularly a cytotoxic agent, is attached. More specifically, this invention relates to conjugates of cell-binding agents and active release products comprising cytotoxic agents wherein the conjugates are produced by means of a cycloaddition reaction. Methods of production, pharmaceutical compositions and methods of use are provided.
• PROTEIN-DRUG CONJUGATES COMPRISING CAMPTOTHECIN ANALOGS AND METHODS OF USE THEREOF
  申请人：REGENERON PHARMACEUTICALS, INC.

  公开号：US20220072141A1

  公开（公告）日：2022-03-10

  Described herein are protein-drug conjugates and compositions thereof that are useful, for example, for target-specific delivery of therapeutic moieties, e.g., camptothecin analogs and/or derivatives. In certain embodiments, provided are specific and efficient methods for producing protein-drug constructs (e.g., antibody-drug conjugates) utilizing a combination of transglutaminase and 1,3-cycloaddition techniques. Camptothecin analogs, antibody-drug conjugates, and compositions which comprise glutaminyl-modified antibodies and camptothecin analog payloads and are provided.
• [EN] FC CONTAINING POLYPEPTIDES WITH ALTERED GLYCOSYLATION AND REDUCED EFFECTOR FUNCTION<br/>[FR] POLYPEPTIDES CONTENANT FC AYANT UNE GLYCOSYLATION MODIFIÉE ET UNE FONCTION EFFECTRICE RÉDUITE
  申请人：GENZYME CORP

  公开号：WO2014043361A1

  公开（公告）日：2014-03-20

  Provided are binding polypeptides (e.g., antibodies), and drug conjugates thereof, comprising an Fc domain with an altered glycosylation profile and reduced effector function. In particular embodiment, the Fc domain comprises: an asparagine residue at amino acid position 298, according to EU numbering; and a serine or threonine residue at amino acid position 300, according to EU numbering. Also provided are nucleic acids encoding the antigen-binding polypeptides, recombinant expression vectors and host cells for making such antigen-binding polypeptides. Methods of using the antigen-binding polypeptides disclosed herein to treat disease are also provided.