Improved Pharmacokinetic Profiles of HDAC6 Inhibitors via Cap Group Modifications

Hydroxamic acid (HA)-based HDAC inhibitors often suffer from poor pharmacokinetic (PK) profiles, limiting their in vivo applications. Cap group modification offers a promising strategy to address these challenges. Here, we optimized the cap group of TO-317, a selective HDAC6 inhibitor with a bisecte...

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Hlavní autor:	Olasunkanmi O. Olaoye (10131945) (author)
Další autoři:	Fettah Erdogan (9193635) (author), Maria Gracia-Hernandez (14941524) (author), Harsimran Kaur Garcha (12046713) (author), Abootaleb Sedighi (1449262) (author), Qirat F. Ashraf (21251095) (author), Nabanita Nawar (8200374) (author), Mulu Geletu (1343361) (author), Hyuk-Soo Seo (2649460) (author), Diaaeldin I. Abdallah (20854528) (author), Ayah Abdeldayem (10131951) (author), Muhammad Murtaza Hassan (10131954) (author), Sirano Dhe-Paganon (141171) (author), Elvin D. de Araujo (8200395) (author), Alejandro Villagra (2359234) (author), Patrick T. Gunning (545679) (author)
Vydáno:	2025
Témata:	Biophysics Biochemistry Medicine Pharmacology Biotechnology Immunology Developmental Biology Cancer Infectious Diseases Space Science Mathematical Sciences not elsewhere classified Chemical Sciences not elsewhere classified tumor growth inhibition selective hdac6 inhibitor based hdac inhibitors 27 å resolution chlorobenzene sulfonamide cap bisected cap structure preclinical studies showed generating 26 analogs 24 – 1 14 </ b improved pharmacokinetic profiles cap group poor pharmacokinetic five analogs advanced preclinical vivo applications ray crystallography promising strategy powerful approach plasma concentration mice compared fold enhancement enhance ha clinical development achieved 56
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Improved Pharmacokinetic Profiles of HDAC6 Inhibitors via Cap Group Modifications

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