Lipophilicity Determines Routes of Uptake and Clearance, and Toxicity of an Alpha-Particle-Emitting Peptide Receptor Radiotherapy.
Tafreshi NK, Kil H, Pandya DN, Tichacek CJ, Doligalski ML, Budzevich MM, Delva NC, Langsen ML, Vallas JA, Boulware DC, Engelman RW, Gage KL, Moros EG, Wadas TJ, McLaughlin ML and Morse DL.
ACS Pharmacol Transl Sci. 2021;4(2):953-965.
Bioactivity improvement via display of the hydrophobic core of HYD1 in a cyclic ß-hairpin-like scaffold, MTI-101.
Jain P, Badger DB, Liang Y, Gebhard AW, Santiago D, Murray P, Kaulagari SR, Gauthier TJ, Nair R, Kumar M, Guida WC, Hazlehurst LA and McLaughlin ML.
Peptide Science. 2021;113(3).
Biodistribution and Multicompartment Pharmacokinetic Analysis of a Targeted alpha Particle Therapy.
Tichacek CJ, Tafreshi NK, Kil H, Engelman RW, Doligalski ML, Budzevich MM, Gage KL, McLaughlin ML, Wadas TJ, Silva A, Moros E and Morse DL.
Mol Pharm. 2020;17(11):4180-4188.
Melanocortin 1 receptor targeted alpha-particle therapy for metastatic uveal melanoma.
Tafreshi NK, Tichacek CJ, Pandya DN, Doligalski ML, Budzevich MM, Kil H, Bhatt NB, Kock ND, Messina JL, Ruiz EE, Delva NC, Weaver A, Gibbons WR, Boulware DC, Khushalani NI, El-Haddad G, Triozzi PL, Moros EG, McLaughlin ML, Wadas TJ and Morse DL.
J Nucl Med. 2019;60(8):1124-1133.
Development of targeted alpha particle therapy for solid tumors.
Tafreshi NK, Doligalski ML, Tichacek CJ, Pandya DN, Budzevich MM, El-Haddad G, Khushalani NI, Moros EG, McLaughlin ML, Wadas TJ and Morse DL.
Structure and properties of DOTA-chelated radiopharmaceuticals within the (225)Ac decay pathway.
Khabibullin AR, Karolak A, Budzevich MM, McLaughlin ML, Morse DL and Woods LM.
MTI-101 treatment inducing activation of Stim1 and TRPC1 expression is a determinant of response in multiple myeloma.
Emmons MF, Anreddy N, Cuevas J, Steinberger KJ, Yang S, McLaughlin ML, Silva AS and Hazlehurst LA.
Sci Rep. 2017;7(1):2685.
MTI-101 (cyclized HYD1) binds a CD44 containing complex and induces necrotic cell death in multiple myeloma.
Gebhard AW, Jain P, Nair RR, Emmons MF, Argilagos RF, Koomen JM, McLaughlin ML and Hazlehurst LA.
Mol Cancer Ther. 2013;12(11):2446-2458.
Acquisition of resistance toward HYD1 correlates with a reduction in cleaved alpha4 integrin expression and a compromised CAM-DR phenotype.
Emmons MF, Gebhard AW, Nair RR, Baz R, McLaughlin ML, Cress AE and Hazlehurst LA.
Mol Cancer Ther. 2011;10(12):2257-2266.
About Mark McLaughlin
Mark L. McLaughlin, Professor of Medicinal Chemistry, Department of Pharmaceutical Sciences, B.S., Chemistry, Christian Brothers University, Ph.D., Organic Chemistry, Georgia Institute of Technology. After postdoctoral appointments at Rice and Ohio State Universities, he was promoted through the ranks to Professor of Chemistry, Louisiana State University. In 2002, he moved to Professor of Chemistry and Oncological Sciences, University of South Florida, Senior Member, Drug Discovery Department, Moffitt Cancer Center. McLaughlin’s research group is pursuing anticancer drug discovery and development focused on protein-protein interaction inhibitor design, molecularly targeted radiotherapy, and molecularly targeted immunotherapy for the treatment/cure of targeted cancers.