Hacer Karatas Bristow, Ph.D.

Dr. Karatas Bristow received her Ph.D. in Medicinal Chemistry at the University of Michigan under the direction of Prof. Shaomeng Wang. After graduation, she was a postdoctoral fellow at EPFL (Switzerland), and then at the Max Planck Institute of Molecular Physiology (Germany). She worked as an Assistant Professor in Istanbul Medipol University (Turkiye) before joining WVU in 2022.

Protein-protein interaction inhibitors, fragment-based drug discovery, assay development 

Medicinal Chemistry

Publications

Akbarzadeh M, Flegel J, Patil S, Shang E, Narayan R, Buchholzer M, Kazemein Jasemi NS, Grigalunas M, Krzyzanowski A, Abegg D, Shuster A, Potowski M, Karatas H, Karageorgis G, Mosaddeghzadeh N, Zischinsky ML, Merten C, Golz C, Brieger L, Strohmann C, Antonchick AP, Janning P, Adibekian A, Goody RS, Ahmadian MR, Ziegler S, Waldmann H. The Pseudo-Natural Product Rhonin Targets RHOGDI. Angew. Chem. Int. Ed., 2022, 61(18).

Adihou H, Gopalakrishnan R, Förster T, Guéret SM, Gasper R, Geschwindner S, Karatas H, Garcia CC, Wassvik CM, Schade D, Plowright AT, Valeur E, Lemurell M, Grossmann TN, Waldmann H. A protein tertiary structure mimetic modulator of the Hippo signalling pathway. Nature Comm. 2020, 11, 5425.

Karatas H, Akbarzadeh M, Adihou H, Hahne G, Pobbati AV, Yihui Ng E, Guéret SM, Sievers S, Pahl A, Metz M, Zinken S, Dötsch L, Nowak C, Thavam S, Friese A, Kang C, Hong W, Waldmann H. Discovery of Covalent Inhibitors Targeting the Transcriptional Enhanced Associate Domain Central Pocket. J Med Chem., 2020, 63(20), 11972–11989.

Kunig V, Potowski M, Akbarzadeh M, Škopić MK, Santos-Smith DD, Arendt L, Dormuth I, Adihou H, Andlovic B, Karatas H, Shaabani S, Zarganes-Tzitzikas T, Neochoritis CG, Zhang R, Groves M, Guéret SM, Ottmann C, Rahnenführer J, Fried R, Dömling A, Brunschweiger A. TEAD-YAP Interaction Inhibitors and MDM2 Binders from DNA-encoded Indole-focused Ugi-peptidomimetics. Angew. Chem. Int. Ed., 2020, 59, 1-6.

Pobbati AV, Mejuch T, Chakraborty S, Karatas H, Guéret SM, Goy PA, Hahne G, Sievers S, Guccione E, Song H, Waldmann H, Hong W. Identification of Quinolinols as Activators of TEAD-dependent Transcription. ACS Chem. Biol., 2019, 14(12), 2909-2921.

Karatas H, D'Alessandro PL, Maric T, Yevtodiyenko A, Vorherr T, Hollingworth G, Goun EA. Real-time Imaging and Quantification of Peptide Uptake In Vitro and In Vivo. ACS Chem. Biol., 2019, 14(10), 2197-2205).

Laraia L, Friese A, Corkery DP, Konstantinidis G, Erwin N, Hofer W, Karatas H, Klewer L, Brockmeyer A, Metz M, Schölermann B, Dwivedi M, Li L, Rios-Munoz P, Köhn M, Winter R, Vetter IR, Ziegler S, Janning P, Wu YW, Waldmann H. The Cholesterol Transfer Protein GRAMD1A Regulates Autophagosome Biogenesis. Nature Chem. Biol., 2019, 15(7), 710-720.

Guo Y, Lei I, Tian S, Gao W, Karatas H, Li Y, Wang S, Liu L, Wang Z. Chemical Suppression of Specific C-C Chemokine Signaling Pathways Enhances Cardiac Reprogramming. J. Biol. Chem., 2019, 294(23), 9134-9146.

Karatas H, Li Y, Liu L, Ji J, Lee S, Chen Y, Yang J, Huang L, Bernard D, Townsend EC, Cao F, Xu J, Ran X, Li X, Wen B, Sun D, Lei M, Dou Y, Wang S. Discovery of MM-589 as A Highly Potent, Cell-Permeable Macrocyclic Peptidomimetic Targeting the Mixed Lineage Leukemia (MLL)-WD Repeat Domain 5 Protein (WDR5) Protein-Protein Interaction. J. Med. Chem., 2017, 60(12), 4818-4839.

Mezzanotte L, van 't Root M, Karatas H, Goun EA, Löwik CWGM. In vivo Molecular Bioluminescence Imaging: New Tools and Applications. Trends Biotechnol., 2017, 35(7), 640-652.

Liu L, Lei I, Karatas H, Li Y, Wang L, Gnatovskiy L, Dou Y, Wang S, Qian L. Targeting MLL1 H3K4 methyltransferase Activity to Guide Cardiac Lineage Specific Reprogramming of Fibroblasts. Cell Discovery, 2016, 2, 16036.

Xu J, Li L, Xiong J, Dekker A, Ye A, Karatas H, Liu L, Wang H, Qin ZS, Wang S, Dou Y. MLL1 and MLL1 Fusion Proteins Have Distinct Functions in Regulating Leukemic Transcription Program. Cell Discovery, 2016, 2, 16008.

Zhang H, Gayen S, Xiong J, Zhou B, Shanmugam AK, Sun Y, Karatas H, Liu L, Rao RC, Wang S, Nesvizhskii AI, Kalantry S, Dou Y. MLL1 Inhibition Reprograms Epiblast Stem Cells to Naive Pluripotency. Cell Stem Cell, 2016, 18(4), 481-494.

Karatas H, Lee S, Townsend EC, Cao F, Xu J, Bernard D, Liu L, Dou Y, Wang S. Structure-based Design of Conformationally Constrained Cyclic Peptidomimetics to Target the MLL1-WDR5 Protein-Protein Interaction as Inhibitors of the MLL1 Methyltransferase Activity. Chin. Chem. Lett., 2015, 26(4), 455-458.

Cao F, Townsend EC, Karatas H, Xu J, Li L, Lee S, Liu L, Chen Y, Ouillette P, Zhu J, Hess JL, Atadja P, Lei M, Qin ZS, Malek S, Wang S, Dou Y. Targeting MLL1 H3K4 Methyltransferase Activity in Mixed-Lineage Leukemia. Mol. Cell, 2014, 53(2), 247-261.

Zhou H, Liu L, Huang J, Bernard D, Karatas H, Navarro A, Lei M, Wang S. Structure-based Design of High-Affinity Macrocyclic Peptidomimetics to Block the Menin-MLL1 Protein-Protein Interaction. J. Med. Chem., 2013, 56(3), 1113-1123.

Karatas H, Townsend EC, Chen Y, Liu L, Bernard D, Cao F, Dou Y, Lei M, Wang S. Development of Highly Potent Small-Molecule Peptidomimetic Inhibitors of MLL1-WDR5 Interaction. J. Am. Chem. Soc., 2013, 135(2), 669-682. 

Karatas H, Alp M, Yıldız S, Göker H. Synthesis and Potent in vitro Activity of Novel 1H-Benzimidazoles as anti-MRSA agents. Chem. Biol. Drug Design, 2012, 80(2), 237-244.

Karatas H, Townsend EC, Bernard D, Dou Y, Wang S. Analysis of the Binding of Mixed Lineage Leukemia 1 (MLL1) and Histone 3 Peptides to WD Repeat Domain 5 (WDR5) for the Design of Inhibitors of the MLL1-WDR5 Interaction. J. Med. Chem., 2010, 53(14), 5179-5185.

Ozden S, Karatas H, Yildiz S, Goker H. Synthesis and Potent Antimicrobial Activity of Some Novel 4-(5, 6-dichloro-1H-benzimidazol-2-yl)-N-substituted benzamides. Arch. Pharm., 2004, 337(10), 556-62.