Enhancing the Safety and Efficacy of PSMA-Based Small-Molecule Drug Conjugates by Linker Stabilization and Conjugation to Transthyretin Binding Ligand.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01423
Abstract: This work describes the enhancement of a novel antitumor therapeutic platform that combines advantages from small-molecule drug conjugates (SMDCs) and antibody drug conjugates (ADCs). Valine-citrulline (VCit) dipeptide linkers are commonly used cathepsin B cleavable linkers… read more here.
Keywords: small molecule; drug conjugates; ligand; efficacy ... See more keywords
Impact of target interactions on small-molecule drug disposition: an overlooked area
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DOI: 10.1038/nrd.2018.26
Abstract: The selection of an appropriate drug target, as well as a solid understanding of drug pharmacokinetics and pharmacodynamics, are crucial for successful drug discovery1. Although it is generally accepted that the free (unbound) concentration of… read more here.
Keywords: drug binding; molecule drug; small molecule; target ... See more keywords
First small-molecule drug targeting RNA gains momentum
Sign Up to like & getrecommendations! Published in 2021 at "Nature Biotechnology"
DOI: 10.1038/s41587-020-00788-1
Abstract: The new drug not only is a boon for patients with spinal muscular atrophy, but also may spearhead the development of further chemical RNA modulators for a broad range of conditions. read more here.
Keywords: molecule drug; small molecule; rna; drug ... See more keywords
A small molecule drug conjugate (SMDC) of DUPA and a duocarmycin built on the solid phase.
Sign Up to like & getrecommendations! Published in 2019 at "MedChemComm"
DOI: 10.1039/c9md00279k
Abstract: In a proof-of-concept study, solid phase synthesis allowed the rapid generation of a small molecule drug conjugate in which the glutamate carboxypeptidase II (GCPII) targeting small molecule DUPA was conjugated to the alkylating subunit of… read more here.
Keywords: drug conjugate; molecule drug; small molecule; solid phase ... See more keywords
Abstract 1987: Delivery of potent cytotoxic camptothecin derivatives to tumors by OncoFAP-based small molecule-drug conjugates
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-1987
Abstract: Small Molecule-Drug Conjugates (SMDCs) are anti-cancer pro-drugs composed by a tumor-targeting small organic ligand, a linker structure and a potent cytotoxic payload. OncoFAP is an ultra-high affinity ligand of Fibroblast Activation Protein (FAP), a stromal… read more here.
Keywords: small molecule; drug conjugates; potent; molecule drug ... See more keywords
Signaling Pathway and Small-Molecule Drug Discovery of FGFR: A Comprehensive Review
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Chemistry"
DOI: 10.3389/fchem.2022.860985
Abstract: Targeted therapy is a groundbreaking innovation for cancer treatment. Among the receptor tyrosine kinases, the fibroblast growth factor receptors (FGFRs) garnered substantial attention as promising therapeutic targets due to their fundamental biological functions and frequently… read more here.
Keywords: small molecule; fgfr; signaling pathway; review ... See more keywords
Construction of immunotherapy-related prognostic gene signature and small molecule drug prediction for cutaneous melanoma
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Oncology"
DOI: 10.3389/fonc.2022.939385
Abstract: Background Cutaneous melanoma (CM), a kind of skin cancer with a high rate of advanced mortality, exhibits a wide variety of driver and transmitter gene alterations in the immunological tumor microenvironment (TME) associated with tumor… read more here.
Keywords: small molecule; immunotherapy; molecule drug; cutaneous melanoma ... See more keywords
Synthesis and Evaluation of Small Molecule Drug Conjugates Harnessing Thioester-Linked Maytansinoids
Sign Up to like & getrecommendations! Published in 2022 at "Pharmaceutics"
DOI: 10.3390/pharmaceutics14071316
Abstract: Ligand-targeting drug conjugates are a class of clinically validated biopharmaceutical drugs constructed by conjugating cytotoxic drugs with specific disease antigen targeting ligands through appropriate linkers. The integrated linker-drug motif embedded within such a system can… read more here.
Keywords: small molecule; thioester linked; drug conjugates; molecule drug ... See more keywords