Improved Pharmacokinetic Profiles of HDAC6 Inhibitors via Cap Group Modifications

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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Main Author: Olasunkanmi O. Olaoye (10131945) (author)
Other Authors: 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)
Published: 2025
Subjects:
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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