New York University

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Aileron Therapeutics, Inc.

Paramjit S Arora

Brooke Bullock Lao

Ross N Chapman

Michael G Wuo

Danielle Guarracino

Richard Bonneau

Kevin Drew

Petra Tosovská

Anupam Patgiri

Dafna Bar-Sagi

Bogdan Z Olenyuk

Anna Mapp

Kamlesh Yadav

Quintin Pan

Ethel Cesarman

Laura Henchey

Katherine M Block

Stephen Joy

Brooke Bullock Lau

Ivan Grishagin

Deyun Wang

Brooke Bullock

Nicholas G Angelo

Jouliana Sadek

Monika Raj

Huabin Wu

This invention relates to macrostructures (and pharmaceutical formulations containing them) that include a parallel coiled-coil structure, wherein the parallel coiled-coil comprises a first coil of Formula I and a second coil of Formula II:T-f-g-a-b-c-d-e-f-g-a-b-c-d-e-f-g-a-b-c-d-e-T  (I)T-g'-a′-b′-c′-d′-e′-f′-g′-a′-b′-c′-d′-e′-f′-g′-a′-b′-c′-d′-e′-f′-T  (II),as described in the present application. Methods of using these macrostructures are also disclosed.

Nemo coiled coil mimics and methods of using same

This invention relates to macrostructures (and pharmaceutical formulations containing them) that include a parallel coiled-coil structure, wherein the parallel coiled-coil comprises a first coil of Formula I and a second coil of Formula II:T-f-g-a-b-c-d-e-f-g-a-b-c-d-e-f-g-a-b-c-d-e-T  (I)T-g′-a′-b′-c′-d′-e′-f′-g′-a′-b′-c′-d′-e′-f′-g′-a′-b′-c′-d′-e′-f′-T  (II),as described in the present application. Methods of using these macrostructures are also disclosed.

NEMO coiled coil mimics and methods of using same

The present invention relates to oxopiperazines that mimic helix &#x3b1;B of the C-terminal transactivation domain of HIF1&#x3b1;. Also disclosed are pharmaceutical compositions containing these oxopiperazines and methods of using these oxopiperazines (e.g., to reduce gene transcription, treat or prevent disorders mediated by interaction of HIF1&#x3b1; with CREB-binding protein and/or p300, reduce or prevent angiogenesis in a tissue, induce apoptosis, and decrease cell survival and/or proliferation).

Oxopiperazine helix mimetics for control of hypoxia-inducible gene expression

This invention relates to a macrostructure that includes an antiparallel coiled-coil structure or a parallel coiled-coil structure.

Stabilized minimal coiled-coil mimetics

The present invention relates to oligooxopiperazines for modulating the p53-Mdm2 interaction. Exemplary oligooxopiperazines include those of Formula IA, Formula IB, and Formula IC below (wherein the various substituents are as defined herein). Methods of using the oligooxopiperazines are also disclosed. 

Oxopiperazine helix mimetics as inhibitors of the p53-MDM2 interaction

This invention relates to a macrostructure that includes an antiparallel coiled-coil structure shown below or a parallel coiled-coil structure shown below and described in the present application. 

The present invention relates to oxopiperazines that mimic helix &#x3b1;B of the C-terminal transactivation domain of HIF1&#x3b1;. Also disclosed are pharmaceutical compositions containing these oxopiperazines and methods of using these oxopiperazines (e.g., to reduce gene transcription, treat or prevent disorders mediated by interaction of HIF1a with CREB-binding protein and/or p300, reduce or prevent angiogenesis in a tissue, induce apoptosis, and decrease cell survival and/or proliferation).

Oxopiperazine helix mimetics for control of Hypoxia-Inducible gene expression

The present invention relates to peptides having one or more stable, internally-constrained HBS &#x3b1;-helices, where the peptide is capable of interacting with Ras and related proteins.

Hydrogen bond surrogate macrocycles as modulators of Ras

The present invention relates to oligooxopiperazines that mimic helix &#x3b1;B of the C-terminal transactivation domain of HIF-1&#x3b1;. Also disclosed are pharmaceutical compositions containing these oligooxopiperazines and methods of using these oligooxopiperazines (e.g., to reduce gene transcription, treat or prevent disorders mediated by interaction of HIF-1&#x3b1; with CREB-binding protein and/or p300, reduce or prevent angiogenesis in a tissue, induce apoptosis, and decrease cell survival and/or proliferation).

Control of hypoxia-inducible gene expression with oligooxopiperazine nonpeptidic helix mimetics

The present invention relates to oligooxopiperazines for reactivating p53. The oligooxopiperazines comprise two or three oxopiperazine rings and substantially mimic helix &#x3b1;B of the C-terminal transactivation domain of Hypoxia-Inducible Factor 1&#x3b1;. Methods of using the oligooxopiperazines are also disclosed. Exemplary oligooxopiperazines include those of Formula I below (wherein A, R, R, R, R, and B are as defined herein). 

Oligooxopiperazines for p53 reactivation

The present invention relates to oligooxopiperazines and their use. Methods for preparing oligooxopiperazines are also disclosed.

Oligooxopiperazines and methods of making and using them

The present invention relates to peptidomimetics for reactivating p53. Methods of using the peptidomimetics are also disclosed.

Hydrogen-bond surrogate peptides and peptidomimetics for p53 reactivation

The present invention relates to ligation agents and their use in making an amide ligation product. Methods of making the ligation agents are also disclosed.

Aldehyde capture ligation technology for synthesis of amide bonds

The present invention relates to peptides having one or more stable, internally constrained &#x3b1;-helices, and that include a sequence that mimics at least a portion of the C-terminal transactivation domain of HIF-1&#x3b1;. Also disclosed are pharmaceutical compositions containing these peptides and methods of using these peptides, for example to reduce gene transcription, treat or prevent disorders mediated by interaction of HIF-1&#x3b1; with CREB-binding protein and/or p300, reduce or prevent angiogenesis in a tissue, induce apoptosis, decrease cell survival and/or proliferation, and identify potential ligands of CREB-binding protein and/or p300.

Inhibiting interaction between the HIF-1ALPHA and p300/CBP with hydrogen bond surrogate-based helices

The present invention relates to peptidomimetics having a stable, internally constrained protein secondary structure, where the peptidomimetics contain a hydrogen bond surrogate in the internal constraint, and at least one beta amino acid. Methods for promoting cell death using peptidomimetics that inhibit p53/hDM2 are also disclosed.

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Cold Spring Harbor, NY, United States of America

Paramjit S Arora