36results about "Peptides with abnormal peptide link" patented technology

Described herein are anti-NaPi2b antibody-drug conjugates (ADCs) comprising an antibody construct that binds to human sodium-dependent phosphate transporter 2B (NaPi2b) conjugated to a camptothecin analog of Formula (I). The antibody construct of the ADC comprises an amino acid modification in the Fc that knocks out binding to Fc gamma receptors. The ADCs are useful as therapeutic agents, among others, in the treatment of cancer.

The present disclosure provides compounds and methods for preparing antibody conjugates with fluorophores, as well as methods of using these conjugates for cell imaging. In one embodiment, the conjugate can be bound to a quencher to absorb fluorescence from the fluorophore.

The present disclosure relates to a preparation method of an intermediate of camptothecin derivative. Specifically, the present disclosure relates to a preparation method of a compound as shown in formula (II), which comprises the step of reacting a compound as shown in formula (III) with a compound as shown in formula (VII) in the presence of a base. The method has high yield and mild reaction conditions, and is suitable for industrial production.

To provide a hepcidin analog having an improved in vivo half-life, as well as related pharmaceutical compositions and methods of use thereof. [Solution] In certain embodiments, the peptide analog or dimer of the present invention includes an isovaleric acid moiety conjugated to the N-terminal X1 residue. In certain embodiments, the peptide analog or dimer of the present invention includes an isovaleric acid moiety conjugated to the N-terminal Asp residue. In certain embodiments, the peptide analog or dimer of the present invention includes an isovaleric acid moiety conjugated to the N-terminal Glu residue. In certain embodiments, the peptide analog of the present invention includes an amidated C-terminal residue.

The present application discloses a kind of compound for targeting CXCR4 and purposes thereof.The compound is shown in structure of formula (I) or its isotopic variant, hydrate, ester or solvate, tautomer, stereoisomer or pharmaceutically acceptable salt.The compound of the present application connects ligand group (Ra and Rb) for targeting CXCR4 and chelating group Z by linker (L1-X-L2), which has good CXCR4 targeting and specificity, can be quickly imaged in a short time after administration, and can be used for diagnosing and treating CXCR4 overexpression diseases.

Described herein are EphA4 receptor antagonists, pharmaceutical compositions containing EphA4 antagonists, and methods and uses of treating an EphA4-based disease, disorder or pathology in an individual using EphA4 receptor antagonists.

The disclosure relates to a bioactive molecule conjugate, preparation methods and use thereof, particularly relates to a novel bioactive molecule conjugate obtained by improving coupling of the drug and the targeting moiety in an ADC or SMDC, as well as its preparation method and use in the manufacture of a medicament for the treatment of a disease associated with an abnormal cell activity.

The present invention provides a conjugate of an antibody and a functional substance excellent in desired properties while controlling a bonding ratio between the antibody and the functional substance within a specific range, or a salt thereof. More specifically, the present invention provides a regioselective conjugate of an antibody and a functional substance comprising a structural unit represented by the following Formula (I): wherein Ig represents an immunoglobulin unit comprising two heavy chains and two light chains, and is regioselectively bonded to L1 adjacent to Ig via an amino group in side chains of lysine residues in the two heavy chains, HG represents a hydrophilic group, RA represents a side chain of a valine residue, RB represents a side chain of a citrulline residue or the like, ring A represents a divalent aromatic ring group optionally having a substituent, R1 and R2 each independently represent a hydrogen atom or a monovalent group, L1 and L2 each independently represent a divalent group, D represents a functional substance, and r is 1.5 to 2.5, or a salt thereof, and substances related thereto.

The application provides an eIF4E / eIF4G interaction inhibitor and application thereof, and belongs to the technical field of biological medicine.The series of compounds with a sulfonamide-gamma-AA peptidomimetic skeleton provided by the application can simulate the conservative binding sequence of eIF4G and 4E-BP1, show obvious translation inhibition capacity in vitro, and can effectively enter cells and inhibit translation in cells by connecting a cell-penetrating peptide and a lysosomal sorting sequence, thereby playing the roles of inhibiting tumor cell proliferation and mediating programmed death (apoptosis and ferroptosis) of tumor cells.In addition, the application verifies for the first time that the sulfonamide-gamma-AA peptidomimetic skeleton inhibits eIF4E / eIF4G interaction, and solves the problem of poor intracellular effect of previously reported natural polypeptide inhibitors, thereby providing a new means for developing new tumor drugs.

This article provides derivatives of sea hare proline-sea hare isoleucine peptide. It also provides peptide analogs, pharmaceutical compositions comprising these compounds, and methods for treating cancer with these compounds.

This invention relates to inhibitory peptides which bind to α-synuclein molecules and inhibit α-synuclein amyloidogenic aggregation, α-synuclein cytotoxicity, and spread of α-synuclein. Methods of making and using the inhibitory peptides (e.g. to treat subjects having conditions or diseases that are mediated by α-synuclein, such as Parkinson's disease, dementia with Lewy bodies, or MSA) are described.

The document describes compounds and novel targeted ligands that can be linked to therapeutic compounds useful for directing the compounds to their in vivo targets. [Solution] The targeted ligands disclosed herein are useful for targeting expression inhibitory oligomeric compounds, such as RNAi agents, to liver cells in order to regulate gene expression. When bound to therapeutic compounds, the targeted ligands disclosed herein can be used in a variety of applications, including therapeutic, diagnostic, target validation, and genome discovery applications. Compositions comprising the targeted ligands disclosed herein, when bound to expression inhibitory oligomeric compounds, can mediate the expression of target nucleic acid sequences in liver cells, such as hepatocytes, and may be useful in treating diseases or disorders that respond to inhibition of gene expression or activity in cells, tissues, or organisms.

The present invention relates to binding molecules comprising a TRIM21 binding moiety and a protein binding moiety for selective degradation of target proteins. The present invention also relates to compositions comprising these molecules, and their uses in therapy. The present invention also relates to TRIM21 binding molecules, and their uses.

This invention relates to a granzyme B-targeting complex, a radiopharmaceutical, and their imaging applications in tumor immunotherapy, belonging to the field of nuclear medicine diagnostics. The complex is covalently modified, triggering a covalent group proximity effect by recognizing the binding of a peptide to granzyme B, achieving irreversible covalent linkage between the probe and the target protein. This significantly enhances the probe's selective retention at the target site and extends the imaging time window. After radionuclide labeling, the complex can be prepared into a radiopharmaceutical for nuclear medicine imaging; the labeling process is simple and exhibits good stability. This radiopharmaceutical allows for non-invasive, specific, and quantitative monitoring of granzyme B expression levels via PET or SPECT, reflecting the activity status of immune cells in vivo. This invention has significant clinical application value and promising prospects for the early and accurate prediction and dynamic monitoring of tumor immunotherapy efficacy.

A drug formulation comprising a ligand-drug conjugate, a lyophilized excipient, and a buffer, the formulation is subjected to pH screening to limit the buffer and lyophilized excipient used, and the lyophilization process is screened at the same time, so that the appearance, water content, impurity content, and redissolution time of the formulation can all be kept stable during storage.

The application belongs to the field of nuclear medicine and relates to a T cell immunoglobulin and mucin domain-3 targeted compound and application. 68 Ga labeled TIM-3 targeted molecular probes can realize imaging of TIM-3 positive tumors and exhibit good potential as TIM-3 targeted PET imaging agents.

The present disclosure features macrocyclic compounds capable of inhibiting Ras proteins, as well as pharmaceutical compositions and protein complexes thereof, and their use in the treatment of cancer.

The present invention discloses a five-membered fused six-membered compound, a preparation method, a pharmaceutical composition, and applications. The present invention provides a compound represented by formula (I), a pharmaceutically acceptable salt, or an isotope thereof. The compound of the present invention has an inhibitory and / or degrading effect on IRAK4. [Formula 1] TIFF2025525281000581.tif31170

The application provides a polypeptide type PROTAC molecule targeting degradation of a STING protein and application thereof in treatment of dry eye, and belongs to the technical field of biotechnology.The polypeptide type PROTAC molecule provided by the application comprises a STING targeting unit capable of specific binding with the STING protein, a connecting arm and an E3 ubiquitin ligase ligand, and can specifically degrade the STING protein.The application further provides application of the polypeptide type PROTAC molecule in preparation of a medicine for treating and / or preventing dry eye and a medicine for preventing and / or treating dry eye, has significant anti-inflammatory and tissue protection effects, can improve corneal epithelial damage, inflammatory reaction and goblet cell loss, and has excellent biocompatibility and safety, and is suitable for long-term or repeated administration on an ocular surface.

The present application relates to a kind of compound shown in general formula I or its stereoisomer, solvate, hydrate, prodrug, stable isotopic derivative and pharmaceutically acceptable salt, the compound has very high degradation activity to PRMT1 and has excellent selectivity, while having excellent drug efficacy, solubility, in vitro / in vivo pharmacokinetic properties and safety, high clinical application prospect.

The present application relates to a compound or a pharmaceutically acceptable salt and / or solvate thereof comprising one or more circulation enhancing groups, one or more target binding groups, one or more chelating groups, at one least cleavable linker and at least one branching group that is at least trivalent. The application further includes a radionuclide complex or a pharmaceutically acceptable salt and / or solvate thereof, comprising a compound of the application or a pharmaceutically acceptable salt and / or solvate thereof, and one or more radionuclides, and to compositions comprising the compound or the complexes. The present application also includes methods of using the compounds, complexes and compositions for targeting and / or killing target cells. For example, the compound includes a compound of Formula I

Compounds are provided include a. cyclic cell penetrating peptide (cCPP) and one or more linkers comprising, an amino acid component, a. polyethylene glycol component, a hydrophobic component, or a combination thereof. In embodiments, the compound includes an exocyclic peptide (EP). In embodiments, the compound does not include an exocyclic peptide.

This invention discloses an engineered strain of *Pathogenic Bacillus budapestans*, its fermentation process, and its applications. Starting with *Pathogenic Bacillus budapestans* XBD101, this invention obtains *Pathogenic Bacillus budapestans* strain FH1 by sequentially replacing the original fclC promoter with P1; strain FH2 by replacing the original gene2204 promoter of strain FH1 with P1; strain FH3 by replacing the original fclI promoter of strain FH2 with P19; and strain FH4 by replacing the original fclK promoter of strain FH3 with P6. The yield of the fcl-8 peptide derivative from strains FH1 through FH4 is significantly increased sequentially. Further fermentation optimization further increases the yield to 943.39 mg / L, a 13.56-fold increase compared to XBD101, which significantly promotes the industrialization of this type of natural product.

The invention relates to a process for preparing a tetramer of the formula (I), or salts thereof, wherein R1is hydrogen or is a link to a solid support and PROT is an ester protecting group, to a crystalline polymorph of the tetramer of formula I and its preparation and to its use as intermediate in the preparation of a GLP-1R / GIPR agonist.

The present invention addresses the problem of providing a novel cytotoxic substance, in particular, a novel cytotoxic substance suitable as a payload of a ligand-drug conjugate, and a ligand-drug conjugate containing the cytotoxic substance. The present invention relates to a dispirodiketopiperazine compound represented by formula (VIII), or to a novel ligand-drug conjugate represented by formula (I), which contains the compound as a payload.

A kind of granzyme B targeting complex, radiopharmaceutical and its imaging application in intestinal immune abnormal activity belong to the field of nuclear medicine diagnosis and treatment.The complex is covalently modified, specifically non-covalently combined with granzyme B by recognizing peptide first, and then triggers irreversible covalent connection by means of proximity effect, effectively solves the technical bottleneck of low target tissue uptake, short in vivo retention time and narrow imaging window of existing granzyme B probe, significantly improves the selective retention capacity and imaging specificity of the probe in the target site.The complex and radiopharmaceutical of the present application can specifically target granzyme B released by intestinal lesion site immune abnormal activity, realize non-invasive, dynamic, quantitative nuclear medical imaging of intestinal inflammation such as Crohn's disease, ulcerative colitis and aGVHD, and accurately evaluate the degree of intestinal immune abnormal activity and monitor the treatment effect, providing a core tool for early diagnosis and precise diagnosis and treatment of such diseases, and having important clinical transformation value and application prospect.