Abstract: Provided herein are mutants of estrogen receptor alpha ligand binding domain (ER-LBD), and chimeric proteins including such mutant ER-LBD. Also provided are methods of modulating transcription and modulating localization of such chimeric proteins.

Abstract: Provided herein are mutants of estrogen receptor alpha ligand binding domain (ER-LBD), and chimeric proteins including such mutant ER-LBD. Also provided are methods of modulating transcription and modulating localization of such chimeric proteins.

Abstract: The invention provides compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein the variables are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12D mutant of Kirsten rat sarcoma (K-Ras) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.

Abstract: Compounds of formula I as defined herein, or pharmaceutically acceptable salts, solvates or derivatives thereof, are potent inhibitors of angiogenesis and accordingly are of use in the treatment and prevention of various angiogenesis-related disorders such as macular degeneration and diabetic retinopathy.

Abstract: Peptidomimetic macrocycles that comprise all-D configuration ?-amino acids and bind mouse double minute 2 (MDM2 aka E3 ubiquitin-protein ligase) and MDMX (aka MDM4) are described. These all-D configuration ?-amino acid 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 peptidomimetic macrocycles may be useful in anticancer therapies, particularly in combination with chemotherapy or radiation therapy.

Abstract: Compounds of formula I as defined herein, or pharmaceutically acceptable salts, solvates or derivatives thereof, are potent inhibitors of angiogenesis and accordingly are of use in the treatment and prevention of various angiogenesis-related disorders such as cancer.

Abstract: A compound of formula (I) or a salt, solvate or prodrug thereof: wherein R1 and R4 are independently selected from C1-C5 alkyl, C1-C5 haloalkyl, C1-C5 alkenyl, C1-C5 haloalkenyl, C1-C5 alkynyl, C1-C5 haloalkynyl, C1-C5 alkoxy or C1-C5 haloalkoxy; R2 is an optionally substituted heteroaryl selected from optionally substituted tetrazolyl or optionally substituted imidazopyridinyl; and R3 is selected from H or optionally substituted alkyl.