Yuri Bukhtiyarov
Expert in small molecule drug discovery and preclinical/early clinical development of drug candidates with a track record of accomplishments and publications in peer-reviewed scientific journals
Research Interests
About
Publications
Photoreactive Analogues of Prenyl Diphosphates as Inhibitors and Probes of Human Protein Farnesyltransferase and Geranylgeranyltransferase Type I
Journal of Biological Chemistry / Aug 01, 1995
Bukhtiyarov, Y. E., Omer, C. A., & Allen, C. M. (1995). Photoreactive Analogues of Prenyl Diphosphates as Inhibitors and Probes of Human Protein Farnesyltransferase and Geranylgeranyltransferase Type I. Journal of Biological Chemistry, 270(32), 19035–19040. https://doi.org/10.1074/jbc.270.32.19035
Structure-Based Design and Synthesis of 1,3-Oxazinan-2-one Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1
Journal of Medicinal Chemistry / Aug 04, 2011
Xu, Z., Tice, C. M., Zhao, W., Cacatian, S., Ye, Y.-J., Singh, S. B., Lindblom, P., McKeever, B. M., Krosky, P. M., Kruk, B. A., Berbaum, J., Harrison, R. K., Johnson, J. A., Bukhtiyarov, Y., Panemangalore, R., Scott, B. B., Zhao, Y., Bruno, J. G., Togias, J., … Claremon, D. A. (2011). Structure-Based Design and Synthesis of 1,3-Oxazinan-2-one Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1. Journal of Medicinal Chemistry, 54(17), 6050–6062. https://doi.org/10.1021/jm2005354
Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility
ACS Medicinal Chemistry Letters / Aug 16, 2011
Jia, L., Simpson, R. D., Yuan, J., Xu, Z., Zhao, W., Cacatian, S., Tice, C. M., Guo, J., Ishchenko, A., Singh, S. B., Wu, Z., McKeever, B. M., Bukhtiyarov, Y., Johnson, J. A., Doe, C. P., Harrison, R. K., McGeehan, G. M., Dillard, L. W., Baldwin, J. J., & Claremon, D. A. (2011). Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility. ACS Medicinal Chemistry Letters, 2(10), 747–751. https://doi.org/10.1021/ml200137x
Three-dimensional placement of the conserved 530 loop of 16 S rRNA and of its neighboring components in the 30 S subunit
Journal of Molecular Biology / Feb 01, 1999
Wang, R., Alexander, R. W., VanLoock, M., Vladimirov, S., Bukhtiyarov, Y., Harvey, S. C., & Cooperman, B. S. (1999). Three-dimensional placement of the conserved 530 loop of 16 S rRNA and of its neighboring components in the 30 S subunit. Journal of Molecular Biology, 286(2), 521–540. https://doi.org/10.1006/jmbi.1998.2493
Spirocyclic ureas: Orally bioavailable 11β-HSD1 inhibitors identified by computer-aided drug design
Bioorganic & Medicinal Chemistry Letters / Feb 01, 2010
Tice, C. M., Zhao, W., Xu, Z., Cacatian, S. T., Simpson, R. D., Ye, Y.-J., Singh, S. B., McKeever, B. M., Lindblom, P., Guo, J., Krosky, P. M., Kruk, B. A., Berbaum, J., Harrison, R. K., Johnson, J. J., Bukhtiyarov, Y., Panemangalore, R., Scott, B. B., Zhao, Y., … Claremon, D. A. (2010). Spirocyclic ureas: Orally bioavailable 11β-HSD1 inhibitors identified by computer-aided drug design. Bioorganic & Medicinal Chemistry Letters, 20(3), 881–886. https://doi.org/10.1016/j.bmcl.2009.12.082
Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) β Agonist
Journal of Medicinal Chemistry / Mar 29, 2016
Zheng, Y., Zhuang, L., Fan, K. Y., Tice, C. M., Zhao, W., Dong, C., Lotesta, S. D., Leftheris, K., Lindblom, P. R., Liu, Z., Shimada, J., Noto, P. B., Meng, S., Hardy, A., Howard, L., Krosky, P., Guo, J., Lipinski, K., Kandpal, G., … Singh, S. B. (2016). Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) β Agonist. Journal of Medicinal Chemistry, 59(7), 3264–3271. https://doi.org/10.1021/acs.jmedchem.5b02029
Regulation of Sphingomyelin Phosphodiesterase Acid-Like 3A Gene (SMPDL3A) by Liver X Receptors
Molecular Pharmacology / Jul 18, 2012
Noto, P. B., Bukhtiyarov, Y., Shi, M., McKeever, B. M., McGeehan, G. M., & Lala, D. S. (2012). Regulation of Sphingomyelin Phosphodiesterase Acid-Like 3A Gene (SMPDL3A) by Liver X Receptors. Molecular Pharmacology, 82(4), 719–727. https://doi.org/10.1124/mol.112.078865
Identification of spirooxindole and dibenzoxazepine motifs as potent mineralocorticoid receptor antagonists
Bioorganic & Medicinal Chemistry / Mar 01, 2016
Lotesta, S. D., Marcus, A. P., Zheng, Y., Leftheris, K., Noto, P. B., Meng, S., Kandpal, G., Chen, G., Zhou, J., McKeever, B., Bukhtiyarov, Y., Zhao, Y., Lala, D. S., Singh, S. B., & McGeehan, G. M. (2016). Identification of spirooxindole and dibenzoxazepine motifs as potent mineralocorticoid receptor antagonists. Bioorganic & Medicinal Chemistry, 24(6), 1384–1391. https://doi.org/10.1016/j.bmc.2016.02.014
Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11β hydroxysteroid dehydrogenase type 1 inhibitor
Bioorganic & Medicinal Chemistry / Jul 01, 2017
Zhuang, L., Tice, C. M., Xu, Z., Zhao, W., Cacatian, S., Ye, Y.-J., Singh, S. B., Lindblom, P., McKeever, B. M., Krosky, P. M., Zhao, Y., Lala, D., Kruk, B. A., Meng, S., Howard, L., Johnson, J. A., Bukhtiyarov, Y., Panemangalore, R., Guo, J., … Claremon, D. A. (2017). Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11β hydroxysteroid dehydrogenase type 1 inhibitor. Bioorganic & Medicinal Chemistry, 25(14), 3649–3657. https://doi.org/10.1016/j.bmc.2017.04.033
P1‐314: Pharmacological characterization of the new bace1 inhibitor bi 1181181
Alzheimer's & Dementia / Jul 01, 2015
Dorner-Ciossek, C., Hobson, S., Fuchs, K., Sauer, A., Bauer, M., Morales-Ramos, A., Venkatraman, S., Dillard, L. W., Kruk, B., Howard, L., Bukhtiyarov, Y., Zhao, Y., & Lala, D. S. (2015). P1‐314: Pharmacological characterization of the new bace1 inhibitor bi 1181181. Alzheimer’s & Dementia, 11(7S_Part_10). Portico. https://doi.org/10.1016/j.jalz.2015.06.529
Solubilization and Characterization of Dehydrodolichy Diphosphate Synthase from the Yeast Saccharomoyces Carlsbergensis
The Journal of Biochemistry / Jun 01, 1993
Bukhtiyarov, Y. E., Shabalin, Y. A., & Kulaev, I. s. (1993). Solubilization and Characterization of Dehydrodolichy Diphosphate Synthase from the Yeast Saccharomoyces Carlsbergensis. The Journal of Biochemistry, 113(6), 721–728. https://doi.org/10.1093/oxfordjournals.jbchem.a124110
Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core
Bioorganic & Medicinal Chemistry Letters / Oct 01, 2016
Tice, C. M., Noto, P. B., Fan, K. Y., Zhao, W., Lotesta, S. D., Dong, C., Marcus, A. P., Zheng, Y.-J., Chen, G., Wu, Z., Van Orden, R., Zhou, J., Bukhtiyarov, Y., Zhao, Y., Lipinski, K., Howard, L., Guo, J., Kandpal, G., Meng, S., … Claremon, D. A. (2016). Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core. Bioorganic & Medicinal Chemistry Letters, 26(20), 5044–5050. https://doi.org/10.1016/j.bmcl.2016.08.089
In Vitro and In Vivo Assessment of the Potential of Supersaturation to Enhance the Absorption of Poorly Soluble Basic Drugs
Journal of Pharmaceutical Innovation / Sep 07, 2019
Li, J., Bukhtiyarov, Y., Spivey, N., Force, C., Hidalgo, C., Huang, Y., Owen, A. J., & Hidalgo, I. J. (2019). In Vitro and In Vivo Assessment of the Potential of Supersaturation to Enhance the Absorption of Poorly Soluble Basic Drugs. Journal of Pharmaceutical Innovation, 15(4), 591–602. https://doi.org/10.1007/s12247-019-09404-5
Safety, tolerability, pharmacokinetics and pharmacodynamics of VTP-43742, a RORγt inhibitor, in normal healthy volunteers
The Journal of Immunology / May 01, 2016
McGeehan, G. M., Palmer, S. A., Bryson, C. C., Zhao, Y., Shi, M., Lipinski, K. K., Bukhtiyarov, Y., Guo, J., Claremon, D. A., Lala, D. S., & Gregg, R. E. (2016). Safety, tolerability, pharmacokinetics and pharmacodynamics of VTP-43742, a RORγt inhibitor, in normal healthy volunteers. The Journal of Immunology, 196(1_Supplement), 71.4-71.4. https://doi.org/10.4049/jimmunol.196.supp.71.4
VTP-43742 is a potent and selective RORγt blocker that demonstrates oral efficacy in a mouse model of autoimmunity through suppression of IL-17A production (THER7P.945)
The Journal of Immunology / May 01, 2015
McGeehan, G., Bukhtiyarov, Y., Zhao, Y., Meng, S., Noto, P., Stadanlick, J., Kruk, B., Hardy, A., Lipinski, K., Kandpal, G., Algayer, B., Guo, J., Guo, R., Marcus, A., Lotesta, S., Dong, C., Fan, K., Jia, L., Yuan, J., … Lala, D. (2015). VTP-43742 is a potent and selective RORγt blocker that demonstrates oral efficacy in a mouse model of autoimmunity through suppression of IL-17A production (THER7P.945). The Journal of Immunology, 194(1_Supplement), 208.5-208.5|68.3. https://doi.org/10.4049/jimmunol.194.supp.208.5
[9] Photolabile derivatives of oligonucleotides as probes of ribosomal structure
Methods in Enzymology / Jan 01, 2000
Cooperman, B. S., Alexander, R. W., Bukhtiyarov, Y., Vladimirov, S. N., Druzina, Z., Wang, R., & Zuño, N. (2000). [9] Photolabile derivatives of oligonucleotides as probes of ribosomal structure. In RNA-Ligand Interactions Part B (pp. 118–136). Elsevier. https://doi.org/10.1016/s0076-6879(00)18048-6
The potent, selective RORγt blocker, VTP-43742, suppresses Th17 production in vivo and provides greater benefit than IL-17 blockade in the EAE model of autoimmunity (THER3P.968)
The Journal of Immunology / May 01, 2015
Zhao, Y., Meng, S., Noto, P., Bukhtiyarov, Y., Stadanlick, J., Zhuang, L., Dillard, L., Claremon, D., Gregg, R., McGeehan, G., & Lala, D. (2015). The potent, selective RORγt blocker, VTP-43742, suppresses Th17 production in vivo and provides greater benefit than IL-17 blockade in the EAE model of autoimmunity (THER3P.968). The Journal of Immunology, 194(1_Supplement), 68.1-68.1. https://doi.org/10.4049/jimmunol.194.supp.68.1
Applying Photolabile Derivatives of Oligonucleotides To Probe the Peptidyltransferase Center
The Ribosome / Apr 08, 2014
Cooperman, B. S., Vladimirov, S. N., Bukhtiyarov, Y., Druzina, Z., Wang, R., & Seo, H.-S. (2014). Applying Photolabile Derivatives of Oligonucleotides To Probe the Peptidyltransferase Center. In The Ribosome (pp. 271–285). ASM Press. https://doi.org/10.1128/9781555818142.ch23
Abstract 334: The LXRβ Selective Agonist, VTP-38443, Significantly Decreases Plaque Cholesterol Ester Content and Inflammation in a Murine Model of Accelerated Atherosclerosis
Arteriosclerosis, Thrombosis, and Vascular Biology / May 01, 2015
McGeehan, G. M., Lala, D. S., Zhao, Y., Noto, P. B., Zhuang, L., Claremon, D. A., Meng, S., Bukhtiyarov, Y., & Gregg, R. R. (2015). Abstract 334: The LXRβ Selective Agonist, VTP-38443, Significantly Decreases Plaque Cholesterol Ester Content and Inflammation in a Murine Model of Accelerated Atherosclerosis. Arteriosclerosis, Thrombosis, and Vascular Biology, 35(suppl_1). https://doi.org/10.1161/atvb.35.suppl_1.334
Abstract 334: The LXRβ Selective Agonist, VTP-38443, Significantly Decreases Plaque Cholesterol Ester Content and Inflammation in a Murine Model of Accelerated Atherosclerosis
Arteriosclerosis, Thrombosis, and Vascular Biology / May 01, 2015
McGeehan, G. M., Lala, D. S., Zhao, Y., Noto, P. B., Zhuang, L., Claremon, D. A., Meng, S., Bukhtiyarov, Y., & Gregg, R. R. (2015). Abstract 334: The LXRβ Selective Agonist, VTP-38443, Significantly Decreases Plaque Cholesterol Ester Content and Inflammation in a Murine Model of Accelerated Atherosclerosis. Arteriosclerosis, Thrombosis, and Vascular Biology, 35(suppl_1). https://doi.org/10.1161/atvb.35.suppl_1.334
Roles of Organic Anion Transporting Polypeptide 2A1 (OATP2A1/SLCO2A1) in Regulating the Pathophysiological Actions of Prostaglandins
The AAPS Journal / Dec 04, 2017
Nakanishi, T., & Tamai, I. (2017). Roles of Organic Anion Transporting Polypeptide 2A1 (OATP2A1/SLCO2A1) in Regulating the Pathophysiological Actions of Prostaglandins. The AAPS Journal, 20(1). https://doi.org/10.1208/s12248-017-0163-8
RORgamma in complex with inverse agonist BIO399.
Jun 15, 2016
Marcotte, D. J. (2016). RORgamma in complex with inverse agonist BIO399. Worldwide Protein Data Bank. https://doi.org/10.2210/pdb5ixk/pdb
Discovery and Characterization of Benzimidazole Derivative XY123 as a Potent, Selective, and Orally Available ROR Inverse Agonist
Discovery and Characterization of Benzimidazole Derivative XY123 as a Potent, Selective, and Orally Available ROR Inverse Agonist. (n.d.). American Chemical Society (ACS). https://doi.org/10.1021/acs.jmedchem.1c00763.s003
Prolonged stability by cyclization: Macrocyclic phosphino dipeptide isostere inhibitors of β-secretase (BACE1)
Bioorganic & Medicinal Chemistry Letters / Aug 01, 2009
Huber, T., Manzenrieder, F., Kuttruff, C. A., Dorner-Ciossek, C., & Kessler, H. (2009). Prolonged stability by cyclization: Macrocyclic phosphino dipeptide isostere inhibitors of β-secretase (BACE1). Bioorganic & Medicinal Chemistry Letters, 19(15), 4427–4431. https://doi.org/10.1016/j.bmcl.2009.05.053
ROR-gamma-T Modulators for Th17-Driven Diseases: Progress Into the Clinic
2017 Medicinal Chemistry Reviews / Nov 30, 2017
Tice, C. M., Bukhtiyarov, Y., Zheng, Y.-J., Lala, D., & Singh, S. B. (2017). ROR-gamma-T Modulators for Th17-Driven Diseases: Progress Into the Clinic. In Medicinal Chemistry Reviews (pp. 195–216). Medicinal Chemistry Division of the American Chemical Society. https://doi.org/10.29200/acsmedchemrev-v52.ch11
Encuestas para estimar la demanda de propóleo como coadyuvante en el tratamiento de enfermedades reumáticas en el Área Metropolitana de Bucaramanga.
Encuestas para estimar la demanda de propóleo como coadyuvante en el tratamiento de enfermedades reumáticas en el Área Metropolitana de Bucaramanga. (n.d.). [dataset]. Instituto de Investigacion de Recursos Biologicos Alexander von Humboldt (IAVH). https://doi.org/10.21068/6fuxjr
Céphalosporines et association bêta-lactamines-inhibiteurs de bêta lactamase dans le traitement des infections à entérobactéries productrices de bêta lactamase à spectre élargi
Option/Bio / Apr 01, 2013
Emile, C. (2013). Céphalosporines et association bêta-lactamines-inhibiteurs de bêta lactamase dans le traitement des infections à entérobactéries productrices de bêta lactamase à spectre élargi. Option/Bio, 24(489), 21–22. https://doi.org/10.1016/s0992-5945(13)71408-9
P4‐217: EFFECTS OF BACE1 INHIBITION ON ABETA IN RATS AND TG2576
Alzheimer's & Dementia / Jul 01, 2014
Dorner‐Ciossek, C., Hobson, S., Lenter, M., Bukhtiyarov, Y., & Lala, D. (2014). P4‐217: EFFECTS OF BACE1 INHIBITION ON ABETA IN RATS AND TG2576. Alzheimer’s & Dementia, 10(4S_Part_23). Portico. https://doi.org/10.1016/j.jalz.2014.05.1735
P4‐268: A novel LXR beta‐selective partial agonist increases the ApoE‐ABCA1 pathway and decreases hippocampal BETA‐AMYLOID in cynomolgus monkeys without increasing liver triglycerides
Alzheimer's & Dementia / Jul 01, 2012
Bukhtiyarov, Y., Noto, P., Hardy, A., Meng, S., Kandpal, G., Lipinski, K., Howard, L., Kruk, B., Krosky, P., Guo, J., Guo, R., Gregg, R., Zhao, Y., McGeehan, G., & Lala, D. (2012). P4‐268: A novel LXR beta‐selective partial agonist increases the ApoE‐ABCA1 pathway and decreases hippocampal BETA‐AMYLOID in cynomolgus monkeys without increasing liver triglycerides. Alzheimer’s & Dementia, 8(4S_Part_20). Portico. https://doi.org/10.1016/j.jalz.2013.08.049
THE RENIN INHIBITOR VTP-27999 BLOCKS STORED RENIN MORE POTENTLY THAN ALISKIREN
Journal of Hypertension / Jun 01, 2011
Krop, M., Gregg, R., McGeehan, G., & Danser, A. (2011). THE RENIN INHIBITOR VTP-27999 BLOCKS STORED RENIN MORE POTENTLY THAN ALISKIREN: PP.25.286. Journal of Hypertension, 29, e377. https://doi.org/10.1097/00004872-201106001-01110
THE RENIN INHIBITOR VTP-27999 BLOCKS STORED RENIN MORE POTENTLY THAN ALISKIREN
Journal of Hypertension / Jun 01, 2011
Krop, M., Gregg, R., McGeehan, G., & Danser, A. (2011). THE RENIN INHIBITOR VTP-27999 BLOCKS STORED RENIN MORE POTENTLY THAN ALISKIREN: PP.25.286. Journal of Hypertension, 29, e377. https://doi.org/10.1097/00004872-201106001-01110
Biphenyl/diphenyl ether renin inhibitors: Filling the S1 pocket of renin via the S3 pocket
Bioorganic & Medicinal Chemistry Letters / Aug 01, 2011
Yuan, J., Simpson, R. D., Zhao, W., Tice, C. M., Xu, Z., Cacatian, S., Jia, L., Flaherty, P. T., Guo, J., Ishchenko, A., Wu, Z., McKeever, B. M., Scott, B. B., Bukhtiyarov, Y., Berbaum, J., Panemangalore, R., Bentley, R., Doe, C. P., Harrison, R. K., … Claremon, D. A. (2011). Biphenyl/diphenyl ether renin inhibitors: Filling the S1 pocket of renin via the S3 pocket. Bioorganic & Medicinal Chemistry Letters, 21(16), 4836–4843. https://doi.org/10.1016/j.bmcl.2011.06.043
Discovery and optimization of adamantyl carbamate inhibitors of 11β-HSD1
Bioorganic & Medicinal Chemistry Letters / Nov 01, 2010
Tice, C. M., Zhao, W., Krosky, P. M., Kruk, B. A., Berbaum, J., Johnson, J. A., Bukhtiyarov, Y., Panemangalore, R., Scott, B. B., Zhao, Y., Bruno, J. G., Howard, L., Togias, J., Ye, Y.-J., Singh, S. B., McKeever, B. M., Lindblom, P. R., Guo, J., Guo, R., … Claremon, D. A. (2010). Discovery and optimization of adamantyl carbamate inhibitors of 11β-HSD1. Bioorganic & Medicinal Chemistry Letters, 20(22), 6725–6729. https://doi.org/10.1016/j.bmcl.2010.08.142
Optimization of orally bioavailable alkyl amine renin inhibitors
Bioorganic & Medicinal Chemistry Letters / Jan 01, 2010
Xu, Z., Cacatian, S., Yuan, J., Simpson, R. D., Jia, L., Zhao, W., Tice, C. M., Flaherty, P. T., Guo, J., Ishchenko, A., Singh, S. B., Wu, Z., McKeever, B. M., Scott, B. B., Bukhtiyarov, Y., Berbaum, J., Mason, J., Panemangalore, R., Cappiello, M. G., … Claremon, D. A. (2010). Optimization of orally bioavailable alkyl amine renin inhibitors. Bioorganic & Medicinal Chemistry Letters, 20(2), 694–699. https://doi.org/10.1016/j.bmcl.2009.11.066
Design and optimization of renin inhibitors: Orally bioavailable alkyl amines
Bioorganic & Medicinal Chemistry Letters / Jul 01, 2009
Tice, C. M., Xu, Z., Yuan, J., Simpson, R. D., Cacatian, S. T., Flaherty, P. T., Zhao, W., Guo, J., Ishchenko, A., Singh, S. B., Wu, Z., Scott, B. B., Bukhtiyarov, Y., Berbaum, J., Mason, J., Panemangalore, R., Cappiello, M. G., Müller, D., Harrison, R. K., … Claremon, D. A. (2009). Design and optimization of renin inhibitors: Orally bioavailable alkyl amines. Bioorganic & Medicinal Chemistry Letters, 19(13), 3541–3545. https://doi.org/10.1016/j.bmcl.2009.04.140
Purification and characterization of recombinant human renin for X-ray crystallization studies
BMC Biochemistry / Jan 01, 2008
Wu, Z., Cappiello, M. G., Scott, B. B., Bukhtiyarov, Y., & McGeehan, G. M. (2008). Purification and characterization of recombinant human renin for X-ray crystallization studies. BMC Biochemistry, 9(1), 19. https://doi.org/10.1186/1471-2091-9-19
Cloning, Characterization and Site-Directed Mutagenesis of Canine Renin
Journal of Biochemistry / Sep 28, 2007
Bukhtiyarov, Y., Zecher, M., Panemangalore, R., Wu, Z., Bruno, J. G., Yuan, J., Xu, Z., Dillard, L. W., McGeehan, G. M., Harrison, R. K., & Scott, B. B. (2007). Cloning, Characterization and Site-Directed Mutagenesis of Canine Renin. Journal of Biochemistry, 142(6), 671–680. https://doi.org/10.1093/jb/mvm182
Identification of Inhibitors of Bacterial Transcription/Translation Machinery Utilizing a Miniaturized 1536-Well Format Screen
Journal of Biomolecular Screening / Aug 01, 2001
Kariv, I., Cao, H., Marvil, P. D., Bobkova, E. V., Bukhtiyarov, Y. E., Yan, Y. P., Patel, U., Coudurier, L., Chung, T. D. Y., & Oldenburg, K. R. (2001). Identification of Inhibitors of Bacterial Transcription/Translation Machinery Utilizing a Miniaturized 1536-Well Format Screen. Journal of Biomolecular Screening, 6(4), 233–243. https://doi.org/10.1089/10870570152488437
Identification of 23S rRNA nucleotides neighboring the P-loop in the Escherichia coli 50S subunit
Nucleic Acids Research / Nov 01, 1999
Bukhtiyarov, Y., Druzina, Z., & Cooperman, B. S. (1999). Identification of 23S rRNA nucleotides neighboring the P-loop in the Escherichia coli 50S subunit. Nucleic Acids Research, 27(22), 4376–4384. https://doi.org/10.1093/nar/27.22.4376
Education
Drexel University Bennett S LeBow College of Business
MBA, Finance / June, 2002
Russian Academy of Sciences
PhD, Memebrane Biochemistry / May, 1997
Moscow State University Department of General Chemistry
MS, Radiochemistry / June, 1986
Experience
Vitae Pharmaceuticals Inc
Senior Research Fellow / September, 2002 — December, 2016
Principal Investigator overseeing assay development, in vitro pharmacology and animal studies on multiple drug discovery projects. Directed development and implementation of cell proliferation, differentiation and apoptosis assays for oncology and immunology projects, functional assays and target engagement studies in tissues, plasma, primary human and rodent cells. • Designed and managed various studies conducted by the CROs and academic groups including efficacy studies in rodents and Cynomolgus monkeys, DNA microarray and RNA-Seq differential gene expression analysis studies, PK, tissue distribution, DDI and off-target activity assays. • Contributed to the IND filing of several clinical candidates, prepared IND-enabling documents using submission authoring templates StartingPoint (Accenture). Conducted preliminary analysis of clinical results from the Psoriasis (RORγt inverse agonist) and Atopic Dermatitis (LXR agonist) trials.
Dade Behring
Senior Research Scientist / February, 2002 — August, 2002
Method Leader on development of clinical immunochemical assays for cardiac markers on the Dimension instruments platform. • Served as R&D Project Leader on a cross-functional product development teams focused on validation of clinical assays in a GLP/ISO9001 environment. Made a major contribution to invention of new highly sensitive assays for adulteration of urine in analysis of drugs of abuse.
EI Dupont de Nemours and Co
Research Scientist / April, 1999 — October, 2001
Principal investigator in Anti-Bacterial Department working on assay development for projects targeting protein synthesis, tRNA aminoacylation, cell-wall biosynthesis and DNA replication. • Developed and validated HTS-compatible assays for inhibition of protein synthesis in bacteria based on the in vitro transcription/translation of the firefly luciferase reporter gene. • Established assays for inhibition of bacterial aminoacyl-tRNA synthetases (AARS) by monitoring aminoacylation status of individual tRNA’s in bacterial cells by Northern blot analysis.
Absorption Systems
Associate Director / September, 2017 — May, 2020
Principal Scientist in R&D Department working on in vitro pharmacology, transporter assays, in vitro dissolution-absorption system, cell lines for assessing DDI of drug candidates. Assay development and implementation for gene and cell therapy products aimed at evaluation of their potency, transduction efficiency and establishing efficacy in vitro.
Claim Therapeutics
Director of Biology / June, 2020 — December, 2023
Oversaw Biology operations on several drug discovery programs in oncology. Partnered biochemistry and cell biology efforts with multiple CROs in the US and overseas. Responsible for establishing centralized database and data management/presentation. Outsourcing in vitro and in vivo pharmacology studies and data analysis.
Allergan
Associate Director / January, 2017 — March, 2017
Following acquisition of Vitae Pharmaceuticals by Allergan and closing Vitae's site in Fort Washington, PA, I was responsible for transfer of scientific results, data, cell lines, reagents and equipment to Allergan.
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