McHardy Group/CIDD Publications

“Preclinical development of brain permeable ERβ agonist for the treatment of glioblastoma.” Pratap UP, Tidwell M,  Balinda HU,  Clanton NA,  Yang U, Viswanadhapalli S,  Sareddy GR, Liang D, Xie H, Chee Y,  Lai Z, Tekmal RR, McHardy SF, Brenner AJ,  Vadlamudi RK.  2023, Molecular Cancer Therapeutics, MCT-23-0031R, In press.


“A novel small molecule PKC epsilon inhibitor reduces hyperalgesia induced by paclitaxel or opioid withdrawal.” Gregory-Flores, A., Magayewski Bonet, I.J., Desaivre, S., Levine, J.D., McHardy, S. F., de Kraker, H., Russell, N., Fleischer, C., Messing, R.O., Marinelli, M.  BioRxiv 2023, pre-print published June 6. 2023.

“Derivatives Overcome Praziquantel Treatment Limitations for Schistosomiasis.” Alwan, S., Taylor, A. B., Rhodes, J., Tidwell, M., McHardy, S.F., LoVerde, P.T.   PLOS Pathogens, 2023, 19(7), e1011018.


“Addressing the oxamniquine in vitro-in vivo paradox to facilitate a new generation of anti-schistosome treatment.” Toth, K., Alwan, S., Khan, S.,McHardy, S.F., LoVerde, P.T., Cameron, M.D.,  International Journal of Parasitology: Drugs and Drug Resistance, 2023, 21, 65-73.


“Inhibition of Ca2+ entry by capsazepine analog CIDD-99 prevents oral squamous carcinoma cell proliferation.” Sun, Y., Zboril, E.K., De La Chapa, J.J, Chai, X., Da Conceicao, V.N., Valdez, M.C., McHardy, S.F., Gonzales, C.B., Singh, B.B.,  Frontiers in physiology,2022, 13, 969000.


“A first-in-class inhibitor of ER coregulator PELP1 targets ER+ breast cancer.” Altwegg, K., Viswanadhapalli, S., Mann, M., Chakravarty, D., Krishnan, S., Liu, Z., Liu, J., Pratap, U., Ebrahimi, B., Sanchez, J., Li, X., Ma, S., Park, B. H., Santhamma, B., Chen, Y., Lai, Z., Raj, G., Yuan, Y., Zhou, D., Sareddy, G., Tekmal, R., McHardy, S. F., Huang, T. H., Rao, M., Hariprasad, V., Vadlamudi, R.  Cancer Research, 2022, 82(20), 3830-3844.


“Schistosome Sulfotransferases: Mode of Action, Expression and Localization.” Guzman, M. A., Rugel A., Alwan S. N., Taylor A. B., LoVerde P. T., Tarpley, R., McHardy S. F., Chevalier F. D., Wendt, G. R., Collins J. J., Anderson T. J. C.   Pharmaceutics, 2022, 14(7).  PMID35890311.


“HDAC inhibitors enhance ERβ expression and augment ERβ agonist mediated tumor suppression in glioblastoma.” Pratap, U.P., Sareddy, G.R., Liu, Z., Venkata, P.P., Liu, J., Tang, W., Altwegg, K.A., Ebrahimi, B., Li, X., Tekmal, R.R., Viswanadhapalli, S., McHardy, S.F., Brenner, A.J., Vadlamudi, R.K.,  Neuro-Oncology Advances, 2021, 3(1), vdab099.


“Tamoxifen derivatives alter retromer-dependent endosomal tubulation and sorting to block retrograde trafficking of Shiga toxins.” Selyunin, A.S., Nieves-Merced, K., Li, D., McHardy, S.F., Mukhopadhyay.  Toxins, 2021, 13(6).  PMID34203879.


“Rational approach to drug discovery for human schistosomiasis.”  LoVerde P.T., Alwan, S.N., Taylor, A.B., Rhodes J., McHardy, S.F., Chevalier, F.D., Anderson, T. International journal for parasitology. Drugs and drug resistance, 16, 140-147, 2021. PMID34111649.


“A novel catalytic heme cofactor in SfmD with a single thioether bond and a bis-His ligand set revealed by a de novo crystal structural and spectroscopic study”. Shin, I., Davis, I., Nieves-Merced, K., Wang, Y., McHardy, S.F., Liu, A. Chemical Science (2021), 12, 3984-3998. PMID33593898.



“Modulation of a α1β3γ2 GABAA receptors expressed in X. laevis oocytes using a propofol photoswitch tethered to the transmembrane helix”. Borghese, C.M., Messing, R.O., Harris, R.A., Wang, H.L., McHardy, S.F., Trudell, J.R., Bertaccini, E.J. Proceedings of the National Academy of Sciences of the United States of America, 2021118(8).  


“Diabetic strips as coulometric sensors for hydroquinone and leukocyte esterase”. Bekhit, M., Wang, H-Y., Menard, T., McHardy, S.F., Gorski, W. J. Electroanal. Chem, 2020874: 114509.


“Infection screening in biofluids with glucose test strips”. Bekhit, M., Wang, H-Y., McHardy, S.F., Gorski, W. Anal. Chem., 202092, 3860-3866. PMID32040916. 


“Molecular basis for hycanthone drug action in schistosome parasites”. Rugel, A.R., Guzman, M.A., Taylor, A.B., Chevalier, F.D., Anderson, T.J.C., Tarpley, R.S., McHardy, S.F., Cao, X., Holloway, S.P., Hart, P.J., LoVerde, P.T. Mol. Biochem. Parasitol., 2020236, 111257. PMID32027942. 


“Why does oxamniquine kill Schistosoma mansoni and not S. haematobium and S. japonicum”. Rugel, A.R., Guzman, M.A., Taylor, A.B., Chevalier, F.D., Anderson, T.J.C., Tarpley, R.S., McHardy, S.F., Cao, X., Holloway, S.P., Hart, P.J., LoVerde, P.T. Int. J. Parasitol. Drugs Drug Resistance202013, 8-15. PMID32315953.


“An iterative process produces oxamniquine derivatives that kill the major human species of schismtosomes”. Guzman, M.A., Rugel, A.R., Tarpley, R.S., Alwan, S.N., Chevalier, F.D., Kovalsky, D.P., Cao, X., Holloway, S.P., Anderson, T.J.C., Taylor, A.B., McHardy, S.F., LoVerde, P.T. PLOS Neglected Trop. Dis., 202014(8): e0008517. PMID32810153.


 “Tamoxifen blocks retrograde trafficking of Shiga toxin 1 and 2 and protects against lethal toxicosis”. Selyunin, A.S., Hutchens, S., Mukhopadhyay, S., McHardy, S.F. Life Science Alliance20192, 3. PMID31243048. 


“The novel capsazepine analog, CIDD-99, significantly inhibits oral aquamous cell carcinoma in vivo through a TRPV1-independent induction of ER stress, mitochondrial dysfunction and apoptosis”. De La Chapa, J., Singha, P., Self, K., Sallaway, M., McHardy, S.F., Hart, M., McGuff, H.S., Valdez, M., Ruiz, F. III., Gonzales, K., Mitchell, W., Srikanth, R., Polusani, S.R., Gonzales, C.B. J. Oral Pathol. Med, 201948, 389-399. PMID30825343.


“Small molecule nicotinamide N-methyltransferase inhibitors activate senescent muscle stem cells and improve regenerative capacity of aged skeletal muscle”.  Watowich, S., Neelakantan, H., Brightwell, C.R., Graber, T. G., Maroto, R., Wang, H.L., McHardy, S.F., Papaconstantinou, J., Fry, C.F. Biochemical Pharmacology2019163, 481-492. PMID30753815.


“A modular PROTAC design for target destruction using a degradation signal based on a single amino acid”. Shanmugasundaram, K., Shao, P., Chen, H., Campos, B., McHardy, S.F., Luo, T., Rao, H. J. Biol. Chem.2019, 294, 15172-15173. PMID31511327.


“Structure activity relationships for capsazepine analogs that induce mitochondrial dysfunction and S-phase accumulation in OSCC”. Self, K., De La Chapa, J.J., Valdez, M., Ruiz III, F., Mitchell, W., McHardy, S.F., Hart, M., Gonzales, C.B. Bioorganic & Medicinal Chemistry201927, 208-215.


“Design, synthesis, and characterization of novel small molecules as broad range anti-schistosomal agents”. Stahl, S., Tarpley, R., Lopez, A., Menard, T., Guzman, M.A., Taylor, A.B., Cao, X., Chevalier, F.D., Anderson, T.J.C., Hart, J., LoVerde, P.T., McHardy, S.F. ACS Med. Chem. Letters, 20189, 967-973 (Editor selected as featured letter and highlighted on the journal cover).


“Synthesis and characterization of pyridine compounds for amperometric measurements of leukocyte esterase”. Hanson, D., Menard, T., Shoemake, T., McHardy, S.F., Gorski, W. Chembiochem, 201819, 1488-1491.


“Selective and membrane-permeable small molecule inhibitor of nicotinamide N-methyltransferase reverses high fat diet-induced obesity in mice”. Neelakantan, H., Vance, V., Wetzel, M., Wang, H.L., McHardy, S.F., Finnerty, C., Hommel, J.D., Watowich, S.J. Biochemical Pharmacology, 2018, 147, 141-152.


“Novel small molecule inhibitors of protein kinase C Epsilon reduce ethanol consumption in mice”. Blasio, A., Wang, D., Wang, J., Varodayan, F.P., Miller, J., Lee, A.M., McMahon, T., Pomrenze, M.B., Gyawali, S., Wang, H., Roberto, M., McHardy, S.F., Pleiss, M.A., Messing, R.O. Biological Psychiatry201884, 193-201.


“Development of anti-virulence approaches for Candidiasis via a novel series of small-molecule inhibitors of Candida albicans filamentation”. Romo,  J.A., Chaturvedi,  A.K., Lazzell, A.L., Saville, S.P., Lopez-Ribot, J.L., Pierce,  C.G., McHardy, S.F. mBio2017, 8(6).


“Structure activity relationship studies of new cytotoxic oxazoles with selectivity for androgen receptor-positive breast cancer cells”. Robles, A.J.,  McCowen, S., Cai, S., Cichewicz, R.H., Mooberry, S.L., McHardy, S.F.  J. Med. Chem.201760, 9275-9289.


“Electrochemical substrate and assay for esterolytic activity of human white blood cells”. Hanson, D., Menard, T., McHardy, S.F., Fleischman, A., Gorski, W. Analytical Chemistry201789, 7781-7787.


“Structural and enzymatic insights into species-specific resistance to schistosome parasite drug therapy”. Taylor, A.B., Cao, X., Clark, N., Holloway, S.P., LoVerde, P.T.,  Fitzpatrick, P.F., Hart, J.P., Roberts, K.M., Donati, E., Polcaro, C.M., Pica-Mattoccia, L., Cioli, D., Tarpley, R.S., McHardy, S.F. J. Biol. Chem.2017292, 11154-11164. (Paper highlighted on journal cover)


“Structure-activity relationship for Small molecule inhibitors of nicotinamide N-methyltransferase”. Neelakantan, H., Wang, H., Vance, V., Hommel, J.D., McHardy, S.F., Watowich, S.J. J. Med. Chem., 201760, 5015-5028.


“Noncoupled fluorescent assay for direct real-time monitoring of nicotinamide N-methyltransferase activity”. Neelakantan, H., Vance, V., Wang, H., McHardy, S.F., Watowich, S.J. Biochemistry201756, 824-832.


“Targeting Candida albicans filamentation for antifungal drug development”. Vila, T., Romo, J.A., Saville, S.P., Lopez-Ribot, J.L., Pierce, C.G., McHardy, S.F. Virulence20178, 150-158.


“Recent advances in acetylcholinesterase inhibitors and reactivators: an update on the patent literature (2012-2015)”. McHardy, S.F., Wang, H., McCowen, S., Valdez, M. Expert Opinion On Therapeutic Patents2016, 1354-3776.


“Tyrosine phosphorylation regulates ERβ ubiquitination, protein turnover, and inhibition of breast cancer”.  Long Cheng, B.Y., Ye, Q., Gupta, K., Chiang, H., Hu,  Y., Li, R., Gupta, H.B., Lathrop, K., Elledge, R., Curiel, T.J., Sareddy, G.R., Vadlamudi, R., Wang,  D., Wang , P., McHardy, S.F. Oncotarget, 2016, 42585-42597.


“Targeting Candida albicans filamentation for antifungal drug development”. Vila, T., Romo, J.A., Saville, S.P.,  Lopez-Ribot, J.L., Pierce, C.G., McHardy, S.F. Virulence, 2016, 1-9.


“1,3-Propanediol binds deep inside the channel to inhibit water permeation through aquaporins”. Yu, L., Rodriguez, R.A., Chen, L.,  Chen, L.Y., Perry, G., McHardy, S.F.,Yeh, C. Protein Sciences, 2016, 25, 433-441.


“Molecular dynamics study of human carbonic anhydrase II in complex with Zn2+ and acetazolamide on the basis of all-atom force field simulations”.  Wambo, T.O., Chen, L.Y.,  McHardy, S.F.,  Tsin, A.T. Biophysical Chemistry, 2016, 214-215, 54-60.


“A novel small molecule inhibitor of Candida albicans biofilm formation, filamentation and virulence with low potential for the development of resistance”, Pierce,  C.G., Chaturvedi, A.K., Lazzell, A.L., Powell, A.T., Saville, S.P., McHardy, S.F., Lopez-Ribot, J.L. NPJ Biofilms and Microbiomes, 2015, 15012.


“Design, synthesis, and characterization of novel, nonquaternary reactivators of GF-inhibited human acetylcholinesterase”,  McHardy, S.F., Bohmann, H.A., Corbett, M.R., Campos, B., Tidwell, M.W., Thompson, P.M., Bemben, C.J., Menchaca, T.A., Reeves, T.E., Cantrell, W.R., Bauta, W.E., Lopez, A., Maxwell, D.M., Brecht, K.M., Sweeney, R.E., McDonough, J. Bioorganic & Medicinal Chemistry Letters, 2014, 24, 1711-1714.


“18F-FDG microPET imaging detects early transient response to an IGF1R inhibitor in genetically-engineered rhabdomyosarcoma models”,  Soundararajan, A., Abraham, J., Nelon, L.D., Prajapati, S.I., Zarzabal, L.A., Michael, J.E., McHardy, S.F., Hawkins, D.S., Malempati, S., Keller, C. Pediatric Blood & Cancer, 2012, 59(3), 485-92.




U.S. Patents

Inhibition of OLIG2 Activity U.S Patent No. 11,691,951 B2; Jul. 4, 2023

Inventors: Graham Beaton, Fabio C. Tucci, Satheesh B. Ravula, Stanton F. McHardy, Francisco Xavier Ruiz, Ambrosio Lopez, Bismarck Campos, Hua-Yu Leo Wang


Inhibition of OLIG2 Activity U.S. Patent No. 11,685,722 B2; Issued Jun. 27, 2023

Inventors: Graham Beaton, Stanton F. McHardy, Ambrosio Lopez, Jr., Bismarck Campos, Hua-Yu Leo Wang


Redox Substrates for Leukocyte Esterase U.S. Patent No. 11,492,331 B2; Issued Nov. 8, 2022

Inventors: Waldemar Gorski, Stanton McHardy, Douglas Hanson, Travis Menard, Andrew Fleischman


Quinoline Derived Small Molecule Inhibitors of Nicotinamide N-Methyltransferase (NNMT) and Uses Thereof (Licensed to Ridgeline Therapeutics) U.S. Patent No. 11,401,243 B2; Issued Aug. 2, 2022

Inventors: Stanley Watowich, Harshini Neelakantan, Hua-Yu Wang, Stanton McHardy


Methods and Compositions for the Treatment of Shiga Toxicosis U.S. Patent No. 11,304,916 B2; Issued Apr. 19, 2022

Inventors: Somshuvra Mukhopadhyay, Andrey S. Selyunin, Stanton F. McHardy


Capsazepine Analogs for the Treatment of Cancer and Other Proliferative Diseases U.S. Patent No. 10,475,676 B2; Issued Oct. 29, 2019

Inventors: Cara B. Gonzales, Stanton McHardy

International / Foreign Patents

SMARCA2/4 inhibition as a strategy to treat tumors that harbor aberrant Baf gene assemblies WIPO Patent WO2023133221

Stanton F. McHardy and Yogesh K Gupta


Biaryl amide and heteroaryl amides for treatment of candida albicans infection WIPO Patent WO2022197740

Stanton F. Mchardy; Jose Lopez-Ribot; Stephen Saville; Matthew Valdez; Jesus Romo


Indanone and tetralone-keto or hydroxyl oximes as cancer therapeutics WIPO Patent WO2022235492

Stanton F. Mchardy; Michael W. Tidwell; Andrew J. Brenner; Ratna K. Vadlamudi,


Glucosyl esters for infection screening WIPO Patent WO 2021242945

Waldemar Gorski; Stanton F. McHardy, Michael Bekhit; Hua-Yu Wang


Compositions and methods for treating schistosoma infections WIPO Patent WO 2020223370: issued November 5, 2020.

Stanton F. McHardy; Philip T. Loverde; Alexander Bryan Taylor; Reid Samuel Tarpley; Tim J. C. Anderson, Tim J. C.


Preparation of ammonium compounds as antibiotics and methods for the treatment of bacterial infections WIPO Patent WO 2020163479: issued August 13, 2020.

Davies, Bryan; McHardy, Stanton; Cunningham, Ashley; Wang, Hua-Yu, inventors


Redox Substrates for Leukocyte Esterase WIPO Patent No. WO 2019094575: issued May 16, 2019.

Waldek Gorski, Stanton F. McHardy, Travis Menard, Doug Hanson, Andrew Fleischman, inventors


Quinoline Derived Small Molecule Inhibitors of Nicrotinamide N-Methyltransferase WIPO Patent No. WO 2018183668: issued October 4, 2018.

Stanley J. Watowich, Stanton F. McHardy, Hua-Yu Wang, Harshini Neelakantan, inventors


Preparation of Pyrimidinyl Ureas for Inhibition of Olig2 Activity WIPO Patent No. WO 2018039621: issued March 1, 2018.

Graham Beaton, Stanton F. McHardy, Ambrosio Lopez Jr., Bismarck Campos, Hua-Yu Wang, inventors


Preparation of N-Aryl-N’-Heteroaryl-Ureas and Their Use for Inhibition of Olig2 Activity WIPO Patent No. WO 2016138479: issued September 1, 2016.

Graham Beaton, Fabio C. Tucci, Satheesh B. Ravula, Stanton F. McHardy, Francisco X. Ruiz, Ambrosio Lopez, Bismarck Campos, Hua-Yu Wang, inventors


Novel Capsazepine Analogs for the Treatment of Cancer and Other Proliferative Diseases WIPO Patent No. WO 2016033105: issued March 3, 2016.

Stanton F. McHardy, Cara Gonzales, inventors