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 Expertise

Drug Discovery
Cell Biology
Biochemistry
Molecular Biology
Molecular Medicine
Organic Chemistry
Structural Biology
Clinical Biochemistry
Pharmaceutical Science
Pharmacology
Neurology (clinical)
Health Policy
Developmental Neuroscience
Epidemiology
Cellular and Molecular Neuroscience
Geriatrics and Gerontology
Psychiatry and Mental health
Immunology
Immunology and Allergy
Genetics
Cardiology and Cardiovascular Medicine
Internal Medicine
Physiology

About

Extensive industrial research experience focused on Drug Discovery, In Vitro Diagnostics, Biochemistry, Molecular and Cell Biology. • A record of accomplishments including five research projects taken from their inception to IND filing and advancing seven compounds into clinic. • Experience with validation of novel drug targets and evaluation of small molecule drug candidates in functional assays and animal models. Deep knowledge of assay development, including cell-based and enzyme/receptor assays. • Broad expertise in Biological Sciences - enzymology, molecular biology, bioanalytical protocols, protein expression and purification, protein chemistry, immunochemistry, cell biology and cell signal transduction. • Experience with outsourcing of DMPK, in vitro Pharmacology, DDI and efficacy studies, working with CRO and Academic groups on Target Validation and Preclinical Drug Development. • Expertise with database management, deposition of structured results and analysis of large data arrays including data mining and statistical analysis.

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Publications

Photoreactive Analogues of Prenyl Diphosphates as Inhibitors and Probes of Human Protein Farnesyltransferase and Geranylgeranyltransferase Type I
Journal of Biological Chemistry
1995
Structure-Based Design and Synthesis of 1,3-Oxazinan-2-one Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1
Journal of Medicinal Chemistry
2011
Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility
ACS Medicinal Chemistry Letters
2011
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
1999
Spirocyclic ureas: Orally bioavailable 11β-HSD1 inhibitors identified by computer-aided drug design
Bioorganic & Medicinal Chemistry Letters
2010
Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) β Agonist
Journal of Medicinal Chemistry
2016
Regulation of Sphingomyelin Phosphodiesterase Acid-Like 3A Gene (SMPDL3A) by Liver X Receptors
Molecular Pharmacology
2012
Identification of spirooxindole and dibenzoxazepine motifs as potent mineralocorticoid receptor antagonists
Bioorganic & Medicinal Chemistry
2016
Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11β hydroxysteroid dehydrogenase type 1 inhibitor
Bioorganic & Medicinal Chemistry
2017
P1‐314: Pharmacological characterization of the new bace1 inhibitor bi 1181181
Alzheimer's & Dementia
2015
Solubilization and Characterization of Dehydrodolichy Diphosphate Synthase from the Yeast Saccharomoyces Carlsbergensis
The Journal of Biochemistry
1993
Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core
Bioorganic & Medicinal Chemistry Letters
2016
In Vitro and In Vivo Assessment of the Potential of Supersaturation to Enhance the Absorption of Poorly Soluble Basic Drugs
Journal of Pharmaceutical Innovation
2019
Safety, tolerability, pharmacokinetics and pharmacodynamics of VTP-43742, a RORγt inhibitor, in normal healthy volunteers
The Journal of Immunology
2016
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
2015
[9] Photolabile derivatives of oligonucleotides as probes of ribosomal structure
Methods in Enzymology
2000
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
2015
Applying Photolabile Derivatives of Oligonucleotides To Probe the Peptidyltransferase Center
The Ribosome
2014
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
2015
Roles of Organic Anion Transporting Polypeptide 2A1 (OATP2A1/SLCO2A1) in Regulating the Pathophysiological Actions of Prostaglandins
The AAPS Journal
2017
RORgamma in complex with inverse agonist BIO399.
Unknown Venue
2016
Discovery and Characterization of Benzimidazole Derivative XY123 as a Potent, Selective, and Orally Available ROR Inverse Agonist
Unknown Venue
Prolonged stability by cyclization: Macrocyclic phosphino dipeptide isostere inhibitors of β-secretase (BACE1)
Bioorganic & Medicinal Chemistry Letters
2009
ROR-gamma-T Modulators for Th17-Driven Diseases: Progress Into the Clinic
2017 Medicinal Chemistry Reviews
2017
Encuestas para estimar la demanda de propóleo como coadyuvante en el tratamiento de enfermedades reumáticas en el Área Metropolitana de Bucaramanga.
Unknown Venue
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
2013
P4‐217: EFFECTS OF BACE1 INHIBITION ON ABETA IN RATS AND TG2576
Alzheimer's & Dementia
2014
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
2012
THE RENIN INHIBITOR VTP-27999 BLOCKS STORED RENIN MORE POTENTLY THAN ALISKIREN
Journal of Hypertension
2011
Biphenyl/diphenyl ether renin inhibitors: Filling the S1 pocket of renin via the S3 pocket
Bioorganic & Medicinal Chemistry Letters
2011
Discovery and optimization of adamantyl carbamate inhibitors of 11β-HSD1
Bioorganic & Medicinal Chemistry Letters
2010
Optimization of orally bioavailable alkyl amine renin inhibitors
Bioorganic & Medicinal Chemistry Letters
2010
Design and optimization of renin inhibitors: Orally bioavailable alkyl amines
Bioorganic & Medicinal Chemistry Letters
2009
Purification and characterization of recombinant human renin for X-ray crystallization studies
BMC Biochemistry
2008
Cloning, Characterization and Site-Directed Mutagenesis of Canine Renin
Journal of Biochemistry
2007
Identification of Inhibitors of Bacterial Transcription/Translation Machinery Utilizing a Miniaturized 1536-Well Format Screen
Journal of Biomolecular Screening
2001
Identification of 23S rRNA nucleotides neighboring the P-loop in the Escherichia coli 50S subunit
Nucleic Acids Research
1999

Education

Drexel University Bennett S LeBow College of Business

MBA, Finance / June, 2002

Philadelphia, Pennsylvania, United States of America

Russian Academy of Sciences

PhD, Memebrane Biochemistry / May, 1997

Pushchino

Moscow State University Department of General Chemistry

MS, Radiochemistry / June, 1986

Moscow

Experience

Vitae Pharmaceuticals Inc

Senior Research Fellow / September, 2002December, 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, 2002August, 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, 1999October, 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, 2017May, 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, 2020December, 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, 2017March, 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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