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Advanced Search Results For "SMALL molecules"

1 - 10 of 43,042 results for
 "SMALL molecules"
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A screen of repurposed drugs identifies AMHR2/MISR2 agonists as potential contraceptives.

Publication Type: Academic Journal

Source(s): Proceedings of the National Academy of Sciences of the United States of America [Proc Natl Acad Sci U S A] 2022 Apr 12; Vol. 119 (15), pp. e2122512119. Date of Electronic Publication: 2022 Apr 05.

Abstract: We identified the anti-Mullerian hormone (also known as Müllerian inhibiting substance or MIS) as an inhibitory hormone that induces long-term contraception in mammals. The type II receptor to this hormone, AMHR2 (also known as MISR2), represents a pro...

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A structure-specific small molecule inhibits a miRNA-200 family member precursor and reverses a type 2 diabetes phenotype.

Publication Type: Academic Journal

Source(s): Cell chemical biology [Cell Chem Biol] 2022 Feb 17; Vol. 29 (2), pp. 300-311.e10. Date of Electronic Publication: 2021 Jul 27.

Abstract: MicroRNA families are ubiquitous in the human transcriptome, yet targeting of individual members is challenging because of sequence homology. Many secondary structures of the precursors to these miRNAs (pri- and pre-miRNAs), however, are quite differen...

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Analysis of DNA-Encoded Library Screening Data: Selection of Molecules for Synthesis.

Publication Type: Academic Journal

Source(s): Methods in molecular biology (Clifton, N.J.) [Methods Mol Biol] 2022; Vol. 2541, pp. 195-205.

Authors:

Abstract: DNA-encoded library (DEL) screens are used to discover novel chemical matter capable of modulating the activity of pharmaceutically interesting protein targets. DEL selections are accomplished by immobilizing a target protein on a resin and capturing l...

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Discovery of phenyl-linked symmetric small molecules as inhibitors of the programmed cell death-1/programmed cell death-ligand 1 interaction.

Publication Type: Academic Journal

Source(s): European journal of medicinal chemistry [Eur J Med Chem] 2021 Nov 05; Vol. 223, pp. 113637. Date of Electronic Publication: 2021 Jun 11.

Authors:

Abstract: Programmed cell death-1/programmed cell death ligand 1 (PD-1/PD-L1) is one of the most promising targets in the field of immune checkpoint blockade therapy. Beginning with our exploration of linkers and structure-activity relationship research, we foun...

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An Autophagy-Disrupting Small Molecule Promotes Cancer Cell Death via Caspase Activation.

Publication Type: Academic Journal

Source(s): Chembiochem : a European journal of chemical biology [Chembiochem] 2021 Dec 10; Vol. 22 (24), pp. 3425-3430. Date of Electronic Publication: 2021 Jul 24.

Authors:

Abstract: A novel autophagy inhibitor, autophazole (Atz), which promoted cancer cell death via caspase activation, is described. This compound was identified from cell-based high-content screening of an imidazole library. The results showed that Atz was internal...

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Drug affinity responsive target stability (DARTS) accelerated small molecules target discovery: Principles and application.

Publication Type: Academic Journal

Source(s): Biochemical pharmacology [Biochem Pharmacol] 2021 Dec; Vol. 194, pp. 114798. Date of Electronic Publication: 2021 Oct 19.

Authors:

Abstract: Drug affinity responsive target stability (DARTS) is a novel target discovery approach and is particularly adept at screening small molecule (SM) targets without requiring any structural modifications. The DARTS method is capable of revealing drug-targ...

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Understanding the brain uptake and permeability of small molecules through the BBB: A technical overview.

Publication Type: Academic Journal

Source(s): Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism [J Cereb Blood Flow Metab] 2021 Aug; Vol. 41 (8), pp. 1797-1820. Date of Electronic Publication: 2021 Jan 14.

Abstract: The brain is the most important organ in our body requiring its unique microenvironment. By the virtue of its function, the blood-brain barrier poses a significant hurdle in drug delivery for the treatment of neurological diseases. There are also diffe...

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Diversity-oriented synthesis as a tool to expand the chemical space of DNA-encoded libraries.

Publication Type: Academic Journal

Source(s): Bioorganic & medicinal chemistry [Bioorg Med Chem] 2021 Jul 01; Vol. 41, pp. 116218. Date of Electronic Publication: 2021 May 15.

Abstract: DNA-encoded libraries (DEL) represent a powerful technology for generating compound collections for drug discovery campaigns, that have allowed for the selection of many hit compounds over last three decades. However, the application of split-and-pool ...

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Exploring interactions between extracellular vesicles and cells for innovative drug delivery system design.

Publication Type: Academic Journal

Source(s): Advanced drug delivery reviews [Adv Drug Deliv Rev] 2021 Jun; Vol. 173, pp. 252-278. Date of Electronic Publication: 2021 Mar 31.

Abstract: Extracellular vesicles (EVs) are submicron cell-secreted structures containing proteins, nucleic acids and lipids. EVs can functionally transfer these cargoes from one cell to another to modulate physiological and pathological processes. Due to their p...

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Recent advances in the development of small molecules targeting RNA G-quadruplexes for drug discovery.

Publication Type: Academic Journal

Source(s): Bioorganic chemistry [Bioorg Chem] 2021 May; Vol. 110, pp. 104804. Date of Electronic Publication: 2021 Mar 06.

Authors:

Abstract: Extensive evidence indicates that RNA G-quadruplexes have associated with some important cellular events. Investigation of RNA G-quadruplexes is thus vital to revealing their biofunctions. Several small molecules have been developed to target RNA G-qua...

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