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All Journal CHEMPUBLISH JOURNAL Biomedical Journal of Indonesia
Abdul Holik, Holis
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Biochemistry, Genetics & Molecular Biology Chemical Engineering, Chemistry & Bioengineering Chemistry Medicine & Pharmacology

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Use of 99m Tc in The Field of Radiofarmation: A Review Kelutur, Faruk Jayanto; Abdul Holik, Holis
Biomedical Journal of Indonesia Vol. 7 No. 1 (2021): Biomedical Journal of Indonesia
Publisher : Fakultas Kedokteran Universitas Sriwijaya (Faculty of Medicine, Universitas Sriwijaya) Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.32539/bji.v7i1.241

Abstract

A B S T R A C TTechnetium-99m ( 99m Tc) has been applied in nuclear medicine as a radiopharmacyfor both diagnosis and therapy. 99m Tc is obtained from a 99 Mo/ 99m Tc (half-life 66 h)generator in the form of sodium pertechnetate (Na[ 99m TcO 4 ]) by decaying to 99 Tc for 6hours and emitting gamma energy rays (Eɤ = 140 keV). This radionuclide has anelectron configuration of 4d 5 5s 2 , which will form complexes with different ligandsand have oxidation rates from +1 to +7. The coordinated complex of technetium-99mhas been utilized in nuclear medicine in tissues and organs (thyroid, red and whiteblood cells, kidneys, brain, myocardial, and bone). The resulting kit production musthave based on Good Manufacturing Practice, which consists of batch planning,washing, sterilization of glassware and stopper, starting material, preparation oflarge quantities of the solution, sterile filtration, dispensing, crimping, a summary ofprocess control, quarantine, packaging and leaving the production premises.
Perancangan Radiofarmaka Teranostik Kanker Penargetan Transporter Asam Amino Tipe-L1: Simulasi Docking Molekuler Abdul Holik, Holis; Achmad, Arifudin; Maulana Ibrahim, Faisal; Alysia Elaine, Angela; Stefanus, Jonathan; Sudarmanto, B.S. Ari Sudarmanto; S. Kartamihardja, Achmad Hussein
Chempublish Journal Vol. 9 No. 2 (2025): Chempublish Journal (July - December)
Publisher : Department of Chemistry, Faculty of Science and Technology Universitas Jambi

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.22437/chp.v9i2.48053

Abstract

Abstract. L-type amino acid transporter 1 (LAT1) is a potential pan-cancer theranostic molecular target. The LAT1 inhibitory potencies of eight theranostic radiopharmaceuticals designed based on a potent LAT1 inhibitor ADPB (in vitro pIC50 6.19), were estimated in molecular docking simulations. The designs comprised ADPB as a carrier molecule with/without 6-aminohexanoic acid (Ahx) linker, a chelating agent, and a radiometal (68Ga or 177Lu). JPH203, the most potent LAT1 inhibitor (pIC50 7.22), was utilized as a benchmark compound. A set of known LAT1 ligands (n = 15) were first docked into LAT1 to build the docking protocol. Adding a linker improved the LAT1 inhibitory potency of DOTA-conjugated and NODAGA-conjugated ADPB-based theranostic radiopharmaceutical designs. 177Lu-DOTA-Ahx-ADPB has the exceptional LAT1 inhibitory potency (pIC50 51.55 ± 17.06) while 177Lu-DOTA-ADPB, its non-linker counterpart, has LAT1 inhibitory potency significantly higher than the native JPH203. Both 177Lu-DOTA-Ahx-ADPB and 177Lu-DOTA-ADPB have strong bonds with key amino acids on the LAT1 binding pocket, particularly Asn258, Tyr259, and the gating residue Phe252. Our findings provide a quantitative and illustrative understanding of the LAT1 inhibitory potency of LAT1-targeting theranostic radiopharmaceutical designs relevant to the rational design of pan-cancer radiotheranostic drugs. Keywords: LAT1, pan-cancer, theranostic radiopharmaceutical, MOE, chelating agent, gallium-68, lutetium-177.
Co-Authors Achmad, Arifudin Alysia Elaine, Angela Kelutur, Faruk Jayanto Maulana Ibrahim, Faisal S. Kartamihardja, Achmad Hussein Stefanus, Jonathan Sudarmanto, B.S. Ari Sudarmanto