Abstract: Cancer cells can develop resistance to endocrine therapies, such as Tamoxifen, through acquisition of the Y537S mutation. Cells transfected with the Y537S mutation showed significant increases in mitochondrial mass and membrane potential, consistent with an increase in mitochondrial biogenesis. Certain biomarkers are identified that have prognostic value of endocrine therapy resistance. The mechanism resulting in this resistance, however, leaves these treatment-resistant cells vulnerable to therapeutics that inhibit mitochondrial biogenesis. Numerous mitochondrial biogenesis inhibitors are disclosed, as well as methods for reducing or eliminating endocrine treatment resistance, improving the effectiveness of an endocrine therapy, and for treating cancer.

Abstract: The present disclosure provides, in part, modulators of prostate-specific G-protein receptor (OR51E2/PSGR) and methods of treating, preventing, and diagnosing prostate cancer using the same.

Abstract: Disclosed herein are “ketone body-HMB” or “KB-HMB” compositions including a combination of: (1) hydroxymethyl butyrate; (2) a ketone body component such as beta-hydroxybutyrate (BHB) and/or acetoacetate; and (3) optionally a dietetically or pharmaceutically acceptable carrier. Also disclosed herein are methods of using such compositions for producing desired physiological effects, such as fat loss, in a mammal. The compositions beneficially enhance fat loss through ketosis while also reducing or eliminating muscle wasting and/or promoting muscle formation.

Abstract: The invention provides methods for activating a repressed allele within an imprinting control region, thereby treating an imprinting associated disorder.

Abstract: A 3-[4,4-bis(4-nitrophenyl)-2,5-dioxoimidazolidin-1-yl]propanoic acid compound, its synthesis, and its use as an antimicrobial agent.

Abstract: Bifunctional compounds, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (Raf, such as c-Raf, A-Raf, and/or B-Raf), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds Raf, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The hetero-bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

Abstract: Disclosed are bioavailable solid state (17-?)-Hydroxy-4-Androsten-3-one esters suitable for pharmaceutical uses and administration to mammals in need of (17-?)-Hydroxy-4-Androsten-3-one. Pharmaceutical compositions and the dosage forms of the bioavailable solid state (17-?)-Hydroxy-4-Androsten-3-one esters can be used to treat any condition associated with testosterone deficiency, including complete absence of endogenous testosterone in male or female subjects.

Abstract: Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for eye conditions associated with angiogenesis, for example, intraocular pressure, ocular hypertension, and glaucoma.

Abstract: The invention relates to the use of at least one inhibitory structural analog or inhibitory functional analog of a coenzyme (such as thiamine for example) of an enzyme group, the enzyme members of which catalyze anabolic and/or catabolic and/or energy-releasing metabolic reactions that are of essential significance for the functionality of the overall metabolism of cells, in particular mammalian cells. The invention is used to treat patients in order to produce a general successive (in particular also continuous) slowing down of the metabolic processes of endogenous cells and exogenous cells in the body of the patient and thus achieve a slowing down of disease-causing processes in particular.

Abstract: The present disclosure relates to methods of treating, preventing, reducing the risk of, or delaying the onset of microbial infections in humans and animals that are caused by or involves one or more microorganisms which are capable of being used as biological weapons, the method including administering a pyrrolocytosine compound or a tautomer thereof or a pharmaceutically acceptable salt of the compound or tautomer.

Abstract: Provided are pharmaceutical compositions and methods of treating or preventing edema, using an anti-T cell agent, an anti-TGF-?1 agent, or an anti-angiotensin agent, preferably a combination of at least two such agents. The pharmaceutical compositions can be formulated for systemic or local administration, and are preferably administered topically.

Abstract: A pharmaceutical composition exhibiting anti-tumor activity is provided. The pharmaceutical composition comprises para-toluenesulfonamide (PTS) and a pharmaceutically acceptable carrier. The pharmaceutical composition is used for treating squamous-cell carcinoma. The present invention further provides a method for treating a patient suffering from cancer and a method for inhibiting tumor growth.

Abstract: Methods of treating patients suffering from or exhibiting symptoms of mental, behavioral, and/or cognitive disorders with azelastine or a pharmaceutically acceptable salt of azelastine are disclosed.

Abstract: The invention is directed to roles for low doses of PARP-1 inhibitors and synergistic combinations thereof to treat disease.

Abstract: The technology described herein is directed to methods and compositions for inhibition of ClbP and the treatment and/or prevention of cancer, e.g., colorectal cancer, a urinary tract cancer, a squamous cell carcinoma, an oral squamous cell carcinoma, or a head-and-neck cancer.

Abstract: The invention relates to a pharmaceutically acceptable acid addition salt of: (i) S-pindolol; and (ii) an organic acid, wherein the organic acid has: a pKal of greater than or equal to 2.5; and a chemical formula of CxHy(CO2H)z, where x is from 1 to 10, y is from 2 to 20 and z is 1 or 2. The pharmaceutically acceptable acid addition salt is useful in treating conditions such as cachexia, sarcopenia, a neuromuscular disorder and muscle weakness.

Abstract: The present disclosure generally relates to pharmaceutical compositions and combinations comprising an androgen receptor N-terminal domain inhibitor or an inhibitor and a second therapeutically active agent, such as an CDK4/6 inhibitor, a Pin1 inhibitor (inhibitor of peptidyl-prolyl cis/trans isomerases), or an antiandrogen. In particular, the present disclosure relates to pharmaceutical compositions and combinations useful for treatment of various cancers, for example breast cancer and prostate cancer. Further, the present disclosure relates administering an androgen receptor N-terminal domain inhibitor in combination with radiation therapy for treatment of various cancers.

Abstract: Disclosed herein are methods for treating estrogen sensitive disease, specifically toward endometrial cancers, and compositions used to treat the estrogen sensitive disease. Methods for treating estrogen sensitive diseases comprise administering to a patient an effective amount of a cannabis extract in the presence of an elevated level of estrogen wherein the estrogen is endogenous estrogen or further comprises exogenous estrogen and wherein the methods may further comprise the addition of a chemotherapeutic agent.

Abstract: The present invention is directed to topical ophthalmic compositions of a lipophilic compound and an oligomeric or polymeric carrier wherein the compositions are useful in the treatment and prevention of macular degeneration. The invention also includes methods of treating macular degeneration by using a topical ophthalmic composition of a lipophilic compound and an oligomeric or polymeric carrier.

Abstract: Provided herein are compositions (e.g., pharmaceutical compositions) comprising deuterated testosterone, deuterated methyltestosterone, or derivatives thereof. The provided compositions and related methods may be useful for treating and/or preventing various diseases and conditions, such as hypogonadism, delay of growth and puberty, weight loss associated with HIV-associated wasting, vulvar dystrophies, micropenis, breast cancer, and sexual disorders.