Bicyclerd Limited

Bicycletx Limited

Bicycle Therapeutics Limited

Daniel Paul Teufel

Edward Walker

Catherine Lucy Stace

Silvia Pavan

John Tite

Gavin Bennett

Leonardo Baldassarre

Gemma Elizabeth Mudd

Gregory Paul Winter

Katerine Van Rietschoten

David Loakes

Christian Heinis

Elise Bernard

Paul John Beswick

Liuhong Chen

Lutz Riechmann

Michael Skynner

Marina Vaysburd

Gabriela Ivanova-Berndt

Paul Gregory Winter

Punit Upadhyaya

Leonardo Baldassare

John Paul Tite

Lutz Reichmann

BICYCLIC PEPTIDE LIGANDS SPECIFIC FOR MT1-MMP

The present invention relates to polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of prostrate-specific membrane antigen (PSMA). The invention also includes drug conjugates comprising said peptides, conjugated to one or more effector and/or functional groups, to pharmaceutical compositions comprising said peptide ligands and drug conjugates and to the use of said peptide ligands and drug conjugates in preventing, suppressing or treating a disease or disorder mediated by PSMA.

Bicyclic peptide ligands specific for PSMA

The present invention relates to polypeptides which are covalently bound to non-aromatic molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of membrane type 1 metalloprotease (MT1-MMP), such as the collagen binding site of MT1-MMP. The invention also describes drug conjugates comprising said peptides, conjugated to one or more effector and/or functional groups which have utility in imaging and targeted cancer therapy.

Bicyclic peptide ligands specific for MT1-MMP

The present invention relates to polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of membrane type 1 metalloprotease (MT1-MMP). The invention also describes drug conjugates comprising said peptides, conjugated to one or more effector and/or functional groups which have utility in imaging and targeted cancer therapy.

The invention describes peptide ligands specific for human plasma Kallikrein.

Modulation of structured polypeptide specificity

A peptide ligand specific for EphA2 comprising a polypeptide comprising three residues selected from cysteine, L-2,3-diaminopropionic acid (Dap), N-beta-alkyl-L-2,3-diaminopropionic acid (N-AlkDap) and N-beta-haloalkyl-L-2,3-diaminopropionic acid (N-HAlkDap), with the proviso that at least one of said three residues is selected from Dap, N-AlkDap or N-HAlkDap, the said three residues being separated by at least two loop sequences, and a molecular scaffold, the peptide being linked to the scaffold by covalent alkylamino linkages with the Dap or N-AlkDap or N-HAlkDap residues of the polypeptide and by thioether linkages with the cysteine residues of the polypeptide when the said three residues include cysteine, such that two polypeptide loops are formed on the molecular scaffold.

Peptide ligands for binding to EphA2

The present invention provides compounds, compositions thereof, and methods of using the same.

Bicyclic peptide ligands with detectable moieties and uses thereof

A compound comprising at least one looped peptide structure attached via at least one alkylamino linkage to a scaffold. Preferably the looped peptide structure is a Bicycle structure comprising two peptide loops attached to the scaffold via two alkylamino linkages and one thioether linkage, one of the linkages being common to both loops. Also provided is a method of making a compound comprising at least one looped peptide structure attached via at least one alkylamino linkages to a scaffold, the method comprising: providing a peptide having at least two residues selected from cysteine, diaminopropionic acid, D-N-Alkyldiaminopropionic acid and &#x3b2;-N-Alkyldiaminopropionic acid, provided that at least one of the residues is diaminopropionic acid, D-N-Alkyldiaminopropionic acid and &#x3b2;-N-Alkyldiaminopropionic acid; providing a scaffold molecule having at least two reactive sites for forming alkylamino or thioether linkages with the said at least two residues; and forming said linkages between the peptide and the scaffold molecule.

Peptide derivatives having novel linkage structures

The present invention relates to polypeptides which are covalently bound to aromatic molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of the Eph receptor tyrosine kinase A2 (EphA2). The invention also includes drug conjugates comprising said peptides, conjugated to one or more effector and/or functional groups, to pharmaceutical compositions comprising said peptide ligands and drug conjugates and to the use of said peptide ligands and dmg conjugates in preventing, suppressing or treating a disease or disorder characterised by overexpression of EphA2 in diseased tissue (such as a tumour).

Bicyclic peptide ligands specific for EphA2

Compounds for treating cancer

Bicyclic peptide ligands and uses thereof

The present invention relates to drug conjugates comprising bicyclic peptides specific for MT1-MMP conjugated to one or more effector and/or functional groups which have utility in targeted cancer therapy.

Bicyclic peptide-toxin conjugates specific for MT1-MMP

Growing community of inventors

Cambridge, United Kingdom

Daniel Paul Teufel