ACS Chemical Biology - ACS Publications - American Chemical Society

Mar 17, 2017 - My research focuses on the development of novel chemical entities against various neurological disorders such as Parkinson's disease, ...
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Introducing Our Authors pubs.acs.org/acschemicalbiology



KEN CLEVENGER

Education: Eastern Michigan University, B.S. Biochemistry, 2011, Undergraduate Research Advisor: Dr. Hedeel Guy-Evans Current Position: University of Michigan, Ph.D. candidate in Molecular and Cellular Pathology, Advisor: Dr. Gregory Dressler Nonscientific Interests: Spending time with my wife and sons, traveling, and snorkeling My research aims to understand developmental processes that, when executed appropriately, are essential in directing the proper development of the urogenital system. When these processes are aberrantly executed or inappropriately reactivated, they can promote pathogenesis. One such process is regulated by the tissue specific developmental control gene Pax2, a transcription factor that is essential for urogenital development. While Pax2 expression is suppressed in healthy, adult renal epithelial cells, it is aberrantly expressed in renal diseases such as renal cell carcinoma or polycystic kidney disease. Considering this, we have taken a virtual screening approach to identify novel smallmolecule regulators of Pax2 transactivation activity and have developed a series of cellular, biochemical, biophysical, and functional assays to validate and characterize these molecules. (Read Grimley’s article DOI: 10.1021/acschembio.6b00782.)

Image courtesy of Dr. Caroline Dehart.

Education: B.S. in Chemistry, Butler University, Advisor: Geoffrey Hoops; Ph.D. in Chemistry and Biochemistry, The University of Texas at Austin, Advisor: Walter Fast; NIH NRSA Postdoctoral Fellow, Northwestern University, Department of Chemistry, Advisor: Neil Kelleher Nonscientific Interests: Folk music, singing, martial arts, and eastern theology My graduate work focused on studies of the Pseudomonas enzyme PvdQ. Our work in this issue provides the first structural evidence of how a fairly advanced siderophore precursor interacts with its biosynthetic machinery. Pyoverdine is a complex peptide with a high energetic cost to the cell, and it is fascinating to gain insights into how its structural features facilitate its biosynthesis. My postdoctoral work is divided between two areas. The first is the study of fungal secondary metabolism utilizing large-scale heterologous expression, high-throughput mass spectrometry, and cheminformatics to discover novel fungal secondary metabolites. The second area is the use of advanced proteomics techniques to study the post translational modification and regulation of metabolic enzymes implicated in tumorigenesis in several cancers. (Read Clevenger’s article DOI: 10.1021/acschembio.7b00031.)





MEIRONG JIA

Image courtesy of Meirong Jia.

EDWARD GRIMLEY

Education: Shandong University, B.S. in Pharmaceutical Engineering, 2009; Shandong University, M.S. in Medicinal Chemistry, 2012 with Prof. Wenfang Xu; Iowa State University, Ph.D. in Biochemistry, 2016 with Prof. Reuben J. Peters Current Position: Iowa State University, Roy J. Carver Department of Biochemistry, Biophysics and Molecular Biology, Postdoctoral research associate in the laboratory of Prof. Reuben J. Peters since Dec. 2016 Nonscientific Interests: Running, music, hiking, and reading My current research interests focus on functional investigation of the mechanisms underlying the activity of class I diterpene synthases. My Ph.D. thesis centered on studies of both substrate promiscuity and catalytic plasticity. The results of my studies not only revealed underlying structure−function relationships

Image courtesy of Mark Deming.

© 2017 American Chemical Society

Published: March 17, 2017 579

DOI: 10.1021/acschembio.7b00199 ACS Chem. Biol. 2017, 12, 579−581

ACS Chemical Biology

Introducing Our Authors

in these complex enzymes but also provided biosynthetic access to novel diterpene products. In this work, we found a pair of residues, specifically in kaurene synthases (-like) (KS(L)s) that can cooperatively affect product outcome, demonstrating the remarkably catalytic plasticity of these enzymes. Moreover, it was possible to use this insight to successfully engineer novel (predominant) production of 8α-hydroxy-ent-pimar-15-ene. (Read Jia’s article DOI: 10.1021/acschembio.6b01075.)



Education: B.Sc. Zoology, Chemistry, Botany (2005), Magadh University, Bodhgaya, Bihar, India; M.Sc. Biomedical Sciences (2007), Institute of Biomedical Science, Bundelkhand University, Jhansi, Uttar Pradesh, India; Ph.D. Biomedical Sciences (2013), Dr. B.R. Ambedkar Center for Biomedical Research, University of Delhi, India Current Position: Dr. D.S. Kothari Postdoctoral Fellow at Dr. B.R. Ambedkar Center for Biomedical Research, University of Delhi, India Nonscientific Interests: Listening to folk music, reading spiritual books, and discussions with friends My research focuses on the development of novel chemical entities against various neurological disorders such as Parkinson’s disease, epilepsy, Alzheimer’s disease, and neurodegeneration. I have been also involved in the development of potent carbonic anhydrase inhibitors by using a structure and ligand based drug designing approach. My research work is also extended to discover potent anticancer agents and to study their molecular mechanism of action. Recently, we have designed and developed novel triazole− piperazine based hybrid molecules to study their anticancer effects. The findings revealed that triazole−piperazine hybrid molecules emerged as potent anticancer agents, which acts through the intrinsic mitochondrial pathway of apoptosis and effectively reduced tumor progression in the oesteosarcoma nude mice model. (Read Mishra’s article DOI: 10.1021/acschembio.6b01007.)

SHIKHA KUMARI

Image courtesy of Dr. Rajesh Yadav.



Education: B.Sc. Chemistry, Botany and Zoology (2005), Shivaji College, University of Delhi, New Delhi, India; M.Sc. Pharmaceutical Chemistry (2008), Banasthali University, Rajasthan, India; Ph.D. Biomedical Sciences (2016), Dr. B.R. Ambedkar Center for Biomedical Research, University of Delhi, India Current Position: Postdoctoral Fellow at Dr. B.R. Ambedkar Center for Biomedical Research, University of Delhi, India Nonscientific Interests: Listening to all kinds of music, especially inspirational songs, dancing, gardening, cooking, and traveling My research emphasizes the design, synthesis, and development of novel heterocyclic compounds against several neurological disorders and cancer. In my Ph.D. work, I have designed and synthesized a library of 201 novel compounds via adopting rational drug designing approaches and screened them for their potential against epilepsy. Several compounds showed marked in vitro carbonic anhydrase activity and good in vivo anticonvulsant activity as compared to certain marketed antiepileptic drugs. Moreover, novel triazole-piperazine based hybrid molecules were also synthesized as potent anticancer agents. This work is important because it provides MCS-5 as a most active anticancer agent against osteosarcoma. (Read Kumari’s article DOI: 10.1021/ acschembio.6b01007.)



RAJ KUMAR MONGRE

Image courtesy of Dr. Rajesh Yadav.

Education: B.Sc. Biochemistry (2007), Robetson Model Science College, Jabalpur, India; M.Sc. Bioscience (2013), Barkatullah University, Bhopal, Madhya Pradesh, India; Ph.D. Biotechnology (2016), Department of Animal Biotechnology and Advance Next Generation Convergence, Faculty of Biotechnology, Jeju National University, Republic of Korea Current Position: Postdoctoral Fellow at Research Center for Innovative Cancer Therapeutics, College of Pharmacy, Chungbuk National University, South Korea Nonscientific Interests: Listening to music, cooking, reading books, and playing cricket My research interests are focused on cancer stem cells, tumor biology, tumor metastasis, and systematic drug delivery. Moreover, my research work expands to screening various small bioactive anticancer molecules and naturaceuticals like BRM 270 in various types of carcinomas including multiple drug resistance carcinomas models. We also investigated the role of various cytokines in cancer, and in due course several efforts have been made to establish these cytokines as potent anticancer targets. We investigated the anticancer potential of novel hybrid molecule

CHANDRA BHUSHAN MISHRA

Image courtesy of Dr. Rajesh Yadav.

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DOI: 10.1021/acschembio.7b00199 ACS Chem. Biol. 2017, 12, 579−581

ACS Chemical Biology

Introducing Our Authors

MCS-5 in in vitro as well as in vivo models. Mechanistic studies point out that this novel hybrid compound activates the intrinsic mitochondrial pathway of apoptosis, which leads to exerting superior anticancer activity in the oesteosarcoma nude mouse model. (Read Mongre’s article DOI: 10.1021/acschembio.6b01007.)



Education: BSc (Hons), 2009, The University of Adelaide; Ph.D. in Chemistry, 2014, UNSW Sydney, Advisor: A/Prof Jonathan C. Morris; UNSW Sydney, Postdoctoral research fellow, 2015−16, Exonate Current Position: UNSW Sydney, Postdoctoral research fellow, MetroBiotech Nonscientific Interests: Surfing, supporting Port Adelaide in the AFL, gym, cooking, and beer My current research interests are in the design and synthesis of biologically active molecules, focusing on developing their biomedical potential. Recently, this has involved work developing small molecule inhibitors of SRPK1, a kinase involved in regulating mRNA splicing of VEGF into either anti- or pro-angiogenic isoforms. Disruption of the balance between these two isoforms can lead to diseases such as age-related macular degeneration (AMD). We report in ACS Chemical Biology the development of SPHINX31, a potent and selective inhibitor of SRPK1 which shifts the splicing event from a pro-angiogenic to an antiangiogenic isoform of VEGF. Importantly, we show that SPHINX31 can be used in an eye drop to prevent angiogenesis in a model for AMD and thus represents a new direction for the treatment of AMD. (Read Toop’s article DOI: 10.1021/ acschembio.6b01048.)

DANA THORNLOW

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Education: B.S. Chemical Engineering, University of Massachusetts Amherst, Research Advisor: Neil S. Forbes; Ph.D. Candidate in Chemical and Biomolecular Engineering, Cornell University, Research Advisor: Christopher A. Alabi Current Position: Ph.D. Candidate in Chemical and Biomolecular Engineering, Cornell University, Research Advisor: Christopher A. Alabi Nonscientific Interests: Dance, music, running, and baking My Ph.D. research has focused on engineering synthetic therapeutics for a variety of applications. The Alabi lab’s expertise lies in designing sequence-defined oligomers with tunable backbone and pendant groups using our oligothioetheramide (oligoTEA) platform. These oligomers can be tailored for interaction with different membranes, such as in the given manuscript where we selectively target and disrupt bacterial membranes. Additionally, modularity of the oligoTEA backbone with constant pendant groups gives rise to another activity-tuning parameter, which is unachievable with peptides. My concurrent work involves engineering oligomers to disrupt mammalian endosomal membranes for drug delivery. We hope that the modularity and proteolytic stability of these oligomers will make them unique alternatives to peptides across a range of therapeutics such as antibacterial agents, drug carriers, and cell-penetrating agents. (Read Thornlow’s article DOI: 10.1021/acschembio.6b00837.)



HAMISH D. TOOP

Image courtesy of Andrew John Vegter.

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DOI: 10.1021/acschembio.7b00199 ACS Chem. Biol. 2017, 12, 579−581