Expert opinion on therapeutic patents

INTRODUCTION: Aldo-keto reductase 1C3 (AKR1C3) is a drug target for the treatment of various androgen‑dependent malignancies, including castration-resistant prostate cancer as well as hematological cancers. The enzyme plays a key role in th…

AKR1C3 is a drug target in hormonal and hormonal independent malignancies and acts as a major peripheral 17β-hydroxysteroid dehydrogenase to yield the potent androgens testosterone and dihydrotestosterone, and as a prostaglandin (PG) F synt…

INTRODUCTION: Modulation of the CB2 receptor is an interesting approach for pain and inflammation, arthritis, addictions, neuroprotection, and cancer, among other possible therapeutic applications, and is devoid of central side effects. AR…

Recent studies underscore that prostaglandin-E2 exerts mostly proinflammatory effects in chronic CNS and peripheral disease models, mainly through a specific prostanoid receptor EP2. However, very few highly characterized EP2 receptor antag…

INTRODUCTION: Steroid sulfatase (STS) converts sulfated hormones to free hormones of importance in hormone-dependent diseases such as breast cancer and endometriosis. Carbohydrate sulfatases degrade complex carbohydrates as part of normal c…

This article evaluates a patent application of the company Medivir (SE/UK) describing the synthesis of dipeptide-derived α-ketoamides containing a propylene glycine moiety in P1 as selective inhibitors of cathepsin S for the potential treat…

BACKGROUND: Luteinizing hormone-releasing hormone (LH-RH) plays a central role in the vertebrate reproduction by regulating gonadal activity. Based on its binding to pituitary LH-RH receptors, as well as to LH-RH receptors expressed on canc…

BACKGROUND: Progesterone receptor agonists are used in female contraception, hormone replacement therapy or some gynecological conditions like endometriosis. The interest for antagonists or selective progesterone receptor modulators (SPRMs)…