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Sudhir Raghavan

Sudhir Raghavan, PhD

Instructor in Neurosurgery, Academic Institute
Instructor, Research Institute
Houston Methodist


Baskin Lab


Description of Research

Dr. Raghavan is a synthetic medicinal chemist whose work at the Peak center involves designing, synthesizing and developing new molecules and drug delivery systems to treat brain tumors. His projects include developing an optimized route for GLP/GMP synthesis of PAMOBG, designing and synthesizing the next generation of MAO-activated self-immolative linkers for prodrug development, asymmetric platinum complexes designed to carry the MAO activated prodrug MP, gold or carbohydrate based nanoparticle drug delivery systems and modified sugars that target the ‘sweet tooth’ of cancers.

Publications

Regulation | Monoamine oxidases
Raghavan, S, Baskin, DS & Sharpe, MA 2021, . in Encyclopedia of Biological Chemistry: Third Edition. vol. 1, Elsevier, pp. 542-560. https://doi.org/10.1016/B978-0-12-819460-7.00343-1

MP-Pt(IV): A MAOB-sensitive mitochondrial-specific prodrug for treating glioblastoma
Raghavan, S, Baskin, DS & Sharpe, MA 2020, , Molecular Cancer Therapeutics, vol. 19, no. 12, pp. 2445-2453. https://doi.org/10.1158/1535-7163.MCT-20-0420

MP-Pt(IV): A MAOB-sensitive mitochondrial-specific prodrug for treating glioblastoma
Raghavan, S, Baskin, DS & Sharpe, MA 2020, , Molecular Cancer Therapeutics. https://doi.org/10.1158/1535-7163.MCT-20-0420

A ”clickable” probe for active MGMT in glioblastoma demonstrates two discrete populations of MGMT
Raghavan, S, Baskin, DS & Sharpe, MA 2020, , Cancers, vol. 12, no. 2, 453. https://doi.org/10.3390/cancers12020453

The 3S enantiomer drives enolase inhibitory activity in SF2312 and its analogues
Pisaneschi, F, Lin, YH, Leonard, PG, Satani, N, Yan, VC, Hammoudi, N, Raghavan, S, Link, TM, Georgiou, DK, Czako, B & Muller, FL 2019, , Molecules, vol. 24, no. 13, , 2510. https://doi.org/10.3390/molecules24132510

PAM-OBG: A monoamine oxidase B specific prodrug that inhibits MGMT and generates DNA interstrand crosslinks, potentiating temozolomide and chemoradiation therapy in intracranial glioblastoma
Sharpe, MA, Raghavan, S & Baskin, DS 2018, , Oncotarget, vol. 9, no. 35, pp. 23923-23943. https://doi.org/10.18632/oncotarget.25246

Development and validation of chemical features-based proton-coupled folate transporter/activity and reduced folate carrier/activity models (pharmacophores)
Shah, K, Raghavan, S, Hou, Z, Matherly, LH & Gangjee, A 2018, , Journal of Molecular Graphics and Modelling, vol. 81, pp. 125-133. https://doi.org/10.1016/j.jmgm.2018.02.007

ENOblock does not inhibit the activity of the glycolytic enzyme enolase
Satani, N, Lin, YH, Hammoudi, N, Raghavan, S, Georgiou, DK & Muller, FL 2016, , PLoS ONE, vol. 11, no. 12, e0168739. https://doi.org/10.1371/journal.pone.0168739

Tumor Targeting with Novel 6-Substituted Pyrrolo [2,3-d] Pyrimidine Antifolates with Heteroatom Bridge Substitutions via Cellular Uptake by Folate Receptor a and the Proton-Coupled Folate Transporter and Inhibition of de Novo Purine Nucleotide Biosynthesis
Golani, LK, Wallace-Povirk, A, Deis, SM, Wong, J, Ke, J, Gu, X, Raghavan, S, Wilson, MR, Li, X, Polin, L, De Waal, PW, White, K, Kushner, J, OConnor, C, Hou, Z, Xu, HE, Melcher, K, Dann, CE, Matherly, LH & Gangjee, A 2016, , Journal of Medicinal Chemistry, vol. 59, no. 17, pp. 7856-7876. https://doi.org/10.1021/acs.jmedchem.6b00594

Erratum: Structure-Activity Profiles of Novel 6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Antifolates with Modified Amino Acids for Cellular Uptake by Folate Receptors a and ß and the Proton-Coupled Folate Transporter (Journal of Medicinal Chemistry (2014) 57 (8152-8166) DOI: 10.1021/jm501113m)
Golani, LK, George, C, Zhao, S, Raghavan, S, Orr, S, Wallace, A, Wilson, MR, Hou, Z, Matherly, LH & Gangjee, A 2016, , Journal of Medicinal Chemistry, vol. 59, no. 8, pp. 4032. https://doi.org/10.1021/acs.jmedchem.6b00502

6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Regioisomers as Targeted Antifolates for Folate Receptor a and the Proton-Coupled Folate Transporter in Human Tumors
Wang, L, Wallace, A, Raghavan, S, Deis, SM, Wilson, MR, Yang, S, Polin, L, White, K, Kushner, J, Orr, S, George, C, OConnor, C, Hou, Z, Mitchell-Ryan, S, Dann, CE, Matherly, LH & Gangjee, A 2015, , Journal of Medicinal Chemistry, vol. 58, no. 17, pp. 6938-6959. https://doi.org/10.1021/acs.jmedchem.5b00801

The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents
Zhang, X, Raghavan, S, Ihnat, M, Hamel, E, Zammiello, C, Bastian, A, Mooberry, SL & Gangjee, A 2015, , Bioorganic and Medicinal Chemistry, vol. 23, no. 10, pp. 2408-2423. https://doi.org/10.1016/j.bmc.2015.03.061

Novel 5-substituted pyrrolo[2,3- d ]pyrimidines as dual inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase and as potential antitumor agents
Wang, Y, Mitchell-Ryan, S, Raghavan, S, George, C, Orr, S, Hou, Z, Matherly, LH & Gangjee, A 2015, , Journal of Medicinal Chemistry, vol. 58, no. 3, pp. 1479-1493. https://doi.org/10.1021/jm501787c

Structure-activity profiles of novel 6-substituted pyrrolo[2,3- d ]pyrimidine thienoyl antifolates with modified amino acids for cellular uptake by folate receptors a and ß and the proton-coupled folate transporter
Golani, LK, George, C, Zhao, S, Raghavan, S, Orr, S, Wallace, A, Wilson, MR, Hou, Z, Matherly, LH & Gangjee, A 2014, , Journal of Medicinal Chemistry, vol. 57, no. 19, pp. 8152-8166. https://doi.org/10.1021/jm501113m

The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2, 3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents
Zhang, X, Raghavan, S, Ihnat, M, Thorpe, JE, Disch, BC, Bastian, A, Bailey-Downs, LC, Dybdal-Hargreaves, NF, Rohena, CC, Hamel, E, Mooberry, SL & Gangjee, A 2014, , Bioorganic and Medicinal Chemistry, vol. 22, no. 14, pp. 3753-3772. https://doi.org/10.1016/j.bmc.2014.04.049

Discovery of 5-substituted pyrrolo[2,3- d ]pyrimidine antifolates as dual-acting inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase in de novo purine nucleotide biosynthesis: Implications of inhibiting 5-aminoimidazole-4- carboxamide ribonucleotide formyltransferase to AMPK activation and antitumor activity
Mitchell-Ryan, S, Wang, Y, Raghavan, S, Ravindra, MP, Hales, E, Orr, S, Cherian, C, Hou, Z, Matherly, LH & Gangjee, A 2013, , Journal of Medicinal Chemistry, vol. 56, no. 24, pp. 10016-10032. https://doi.org/10.1021/jm401328u

Tumor-targeting with novel non-benzoyl 6-substituted straight chain pyrrolo[2,3-d ]pyrimidine antifolates via cellular uptake by folate receptor a and inhibition of de novo purine nucleotide biosynthesis
Wang, Y, Cherian, C, Orr, S, Mitchell-Ryan, S, Hou, Z, Raghavan, S, Matherly, LH & Gangjee, A 2013, , Journal of Medicinal Chemistry, vol. 56, no. 21, pp. 8684-8695. https://doi.org/10.1021/jm401139z

Structure-activity relationship and in vitro and in vivo evaluation of the potent cytotoxic anti-microtubule agent N-(4-methoxyphenyl)-N,2,6-trimethyl-6,7- dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride and its analogues as antitumor agents
Gangjee, A, Zhao, Y, Raghavan, S, Rohena, CC, Mooberry, SL & Hamel, E 2013, , Journal of Medicinal Chemistry, vol. 56, no. 17, pp. 6829-6844. https://doi.org/10.1021/jm400639z

Design, synthesis, and molecular modeling of novel pyrido[2,3-d]pyrimidine analogues as antifolates; Application of buchwald-hartwig aminations of heterocycles
Gangjee, A, Namjoshi, OA, Raghavan, S, Queener, SF, Kisliuk, RL & Cody, V 2013, , Journal of Medicinal Chemistry, vol. 56, no. 11, pp. 4422-4441. https://doi.org/10.1021/jm400086g

Synthesis and biological activity of 5-chloro-N4-substituted phenyl-9H-pyrimido[4,5-b]indole-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic agents
Gangjee, A, Zaware, N, Raghavan, S, Disch, BC, Thorpe, JE, Bastian, A & Ihnat, MA 2013, , Bioorganic and Medicinal Chemistry, vol. 21, no. 7, pp. 1857-1864. https://doi.org/10.1016/j.bmc.2013.01.040

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