Abstract:
Glucosylceramide synthase inhibitors and compositions containing the same are disclosed. Methods of using the glucosylceramide synthase inhibitors in the treatment of diseases and conditions wherein inhibition of glucosylceramide synthase provides a benefit, like Gaucher disease and Fabry disease, also are disclosed.
Abstract:
The present disclosure relates generally to thienopyrimidine and thienopyridine compounds and methods of use thereof. In particular embodiments, the present disclosure provides compositions comprising thienopyrimidine and thienopyridine compounds of Formula 3: and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins.
Abstract:
The present invention relates generally to thienopyrimidine and thienopyridine class compounds and methods of use thereof. In particular embodiments, the present invention provides compositions comprising thienopyrimidine and thienopyridine class compounds and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins (e.g., for the treatment of leukemia, solid cancers and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin).
Abstract:
The present invention relates to methods, compositions, and kits for generating conjugated gold nanoparticles. In certain embodiments, the present invention provides methods of generating unsaturated conjugated gold nanoparticles by mixing naked gold nanoparticles with a first type of attachment molecules at a molar ratio such that the attachment molecules attach to the naked gold particles at a density level below the saturation level of the naked gold particles (e.g., at a saturation level of 1-99%). In some embodiments, a second type of attachment molecules (e.g., with the opposite charge as the first type of attachment molecules) are mixed with the unsaturated conjugated gold nanoparticles to generate double-conjugated gold nanoparticles (e.g., that are zwitterionic).
Abstract:
The present disclosure provides substituted 9H-pyrimido[4,5-b]indoles and 5H-pyrido[4,3-b]indoles and related analogs represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, A, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains. Compounds of the present disclosure are especially useful for treating cancer.
Abstract:
The present invention provides methods, systems, and devices for performing photothermal therapy (e.g., to treat cancer) using photothermal nanoparticles with a biocompatible coating surrounding a highly crystallized Fe3O4 core. In certain embodiments, the highly crystallized Fe3O4 core of the photothermal nanoparticles has an X-ray diffraction (XRD) pattern where the brightest diffraction ring is from the 440 plane. In some embodiments, the photothermal therapy is conducted with a device configured to emit electromagnetic radiation in the wavelengths between about 650 nm and 1000 nm, wherein the device further comprises a visible light source that allows a user to determine where the electromagnetic radiation is contacting a subject.
Abstract translation:本发明提供了使用具有围绕高度结晶的Fe 3 O 4核心的生物相容性涂层的光热纳米颗粒进行光热治疗(例如治疗癌症)的方法,系统和装置。 在某些实施方案中,光热纳米颗粒的高度结晶的Fe 3 O 4核心具有X射线衍射(XRD)图案,其中最亮的衍射环来自440平面。 在一些实施例中,光热疗法是用配置成发射大约650nm和1000nm之间的波长的电磁辐射的装置进行的,其中所述装置还包括可见光源,其允许用户确定电磁辐射在哪里接触 学科。
Abstract:
Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.
Abstract:
The present invention provides, in some embodiments, methods, compositions, systems, and kits comprising nano-satellite complexes comprising: a core nanoparticle complex comprising a biocompatible coating surrounding a nanoparticle core; 3-25 satellite particles attached to, or absorbed to, said biocompatible coating; a plurality of antigenic peptides conjugated to, or absorbed to, said satellite particles; and at least one additional property. In other embodiments, provided herein are nano-satellite complexes comprising: a core nanoparticle complex comprising a biocompatible coating surrounding a nanoparticle core; a plurality of satellite particles attached to, or absorbed to, said biocompatible coating; a plurality of antigenic peptides conjugated to, or absorbed to, said satellite particles; and a plurality of LIGHT (TNFSF14) peptides conjugated to, or absorbed to, said satellite particles. In some embodiments, administration of the nanosatellite complexes to a subject with cancer achieves long-term cancer remission (e.g., when combined with an immune checkpoint inhibitor, such as αPD1).
Abstract:
The present invention provides methods, compositions, systems, and kits comprising nano-satellite complexes and/or serum albumin carrier complexes, which are used for modulating antigen-specific immune response (e.g., enhancing anti-tumor immunity). In certain embodiments, the nano-satellite complexes comprise: a) a core nanoparticle complex comprising a biocompatible coating surrounding a nanoparticle core; b) at least one satellite particle attached to, or absorbed to, the biocompatible coating; and c) an antigenic component conjugated to, or absorbed to, the at least one satellite particle component. In certain embodiments, the complexes further comprise: d) a type I interferon agonist agent. In some embodiments, the serum albumin complexes comprise: a) at least part of a serum albumin protein, b) an antigenic component conjugated to the carrier protein, and c) a type I interferon agonist agent.
Abstract:
The present disclosure provides compounds and methods for inhibiting the interaction of menin with its upstream or downstream signaling molecules including but not limited to MLL1, MLL2 and MLL-fusion oncoproteins. Compounds of the disclosure may be used in methods for the treatment of a wide variety of cancers and other diseases associated with one or more of MLL1, MLL2, MLL fusion proteins, and menin.