J. Grembecka

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Targeting protein–protein interactions in hematologic malignancies: still a challenge or a great opportunity for future therapies?

Jolanta Grembecka, T. Cierpicki, J. Grembecka, 2015, Immunological reviews.

From Inhibitors of Lap to Inhibitors of Pal

J. Grembecka, W. Sokalski, Edyta Dyguda-Kazimierowicz, 2007 .

H3K36 methyltransferases as cancer drug targets: rationale and perspectives for inhibitor development.

T. Cierpicki, J. Grembecka, D. Rogawski, 2016, Future medicinal chemistry.

High-Affinity Small-Molecule Inhibitors of the Menin-Mixed Lineage Leukemia (MLL) Interaction Closely Mimic a Natural Protein–Protein Interaction

Craig W. Lindsley, Shaun R. Stauffer, Jolanta Grembecka, 2014, Journal of medicinal chemistry.

Covalent and noncovalent constraints yield a figure eight-like conformation of a peptide inhibiting the menin-MLL interaction.

T. Cierpicki, J. Grembecka, Łukasz Berlicki, 2020, European journal of medicinal chemistry.

Validation of approximate nonempirical scoring model for menin-mixed lineage leukemia inhibitors

T. Cierpicki, J. Grembecka, Wiktoria Jedwabny, 2018, Theoretical Chemistry Accounts.

Rational Design of Orthogonal Multipolar Interactions with Fluorine in Protein–Ligand Complexes

T. Cierpicki, J. Grembecka, G. Lund, 2015, Journal of medicinal chemistry.

Synthesis of Triethyl N-Formyl-N-phosphonomethylglycinate and Diethyl N-Formyl-N-phosphonomethylglycine and Studies of Their Rotational Conformers by Dynamic NMR

T. Cierpicki, J. Grembecka, Z. Ziora, 1999 .

Electrostatic models of inhibitory activity

J. Grembecka, J. Leszczynski, W. Sokalski, 2001 .

Inhibition of CDC25B Phosphatase Through Disruption of Protein–Protein Interaction

T. Cierpicki, J. Grembecka, G. Lund, 2014, ACS chemical biology.

Herbicidal Derivatives of Aminomethylenebisphosphonic Acid. Part III. Structure—Activity Relationship

G. Forlani, J. Grembecka, P. Wieczorek, 1997, Journal of Plant Growth Regulation.

High resolution structure of the HDGF PWWP domain: A potential DNA binding domain

T. Cierpicki, J. Bushweller, J. Grembecka, 2006, Protein science : a publication of the Protein Society.

Targeting the MLL complex in castration resistant prostate cancer

S. Dhanasekaran, A. Chinnaiyan, A. Nesvizhskii, 2015, Nature Medicine.

Tumorigenicity of Ewing sarcoma is critically dependent on the trithorax proteins MLL1 and menin

Dafydd G. Thomas, T. Cierpicki, J. Grembecka, 2016, Oncotarget.

Structure of Bacillus subtilis YXKO--a member of the UPF0031 family and a putative kinase.

A. Joachimiak, F. Collart, W. Minor, 2002, Journal of structural biology.

The role of HTS in drug discovery at the University of Michigan.

D. Sherman, A. Mapp, J. Grembecka, 2014, Combinatorial chemistry & high throughput screening.

Stabilizing the Mixed Lineage Leukemia Protein

T. Cierpicki, J. Grembecka, 2017, The New England journal of medicine.

A tool compound targeting the core binding factor Runt domain to disrupt binding to CBFβ in leukemic cells

Yunpeng Zhou, J. Bushweller, N. Speck, 2018, Leukemia & lymphoma.

Distinct pathways affected by menin versus MLL1/MLL2 in MLL-rearranged acute myeloid leukemia.

M. Meyerson, A. F. Stewart, J. Grembecka, 2019, Experimental hematology.

Chapter 10 – Theoretical Tools for Analysis and Modelling Electrostatic Effects in Biomolecules⋆

J. Grembecka, W. Sokalski, P. Kȩdzierski, 1999 .

The PAF Complex Regulation of Prmt5 Facilitates the Progression and Maintenance of MLL-Fusion Leukemia

Wei Chen, T. Cierpicki, J. Grembecka, 2017, Oncogene.

Identification of phosphinate dipeptide analog inhibitors directed against the Plasmodium falciparum M17 leucine aminopeptidase as lead antimalarial compounds.

J. Dalton, J. Grembecka, K. Trenholme, 2007, Journal of medicinal chemistry.

Origins of the activity of PAL and LAP enzyme inhibitors: toward ab initio binding affinity prediction.

J. Grembecka, J. Leszczynski, W. Sokalski, 2005, Journal of the American Chemical Society.

The most potent organophosphorus inhibitors of leucine aminopeptidase. Structure-based design, chemistry, and activity.

T. Cierpicki, J. Grembecka, P. Kafarski, 2003, Journal of medicinal chemistry.

alpha-Aminoalkylphosphonates as a tool in experimental optimisation of P1 side chain shape of potential inhibitors in S1 pocket of leucine- and neutral aminopeptidases.

J. Grembecka, P. Kafarski, M. Drąg, 2005, European journal of medicinal chemistry.

A synthetic method for diversification of the P1' substituent in phosphinic dipeptides as a tool for exploration of the specificity of the S1' binding pockets of leucine aminopeptidases.

J. Grembecka, P. Kafarski, S. Vassiliou, 2007, Bioorganic & medicinal chemistry.

Structure-Based Design and Synthesis of Dipeptide Analogues as New Inhibitors of Leucine Aminopeptidase

T. Cierpicki, J. Grembecka, P. Kafarski, 2002 .

The Computer-Aided Design, Synthesis, and Activity Prediction of New Leucine Aminopeptidase Inhibitors

J. Grembecka, P. Kafarski, M. Drąg, 2002 .

Quantum chemical analysis of the interactions of transition state analogs with leucine aminopeptidase

J. Grembecka, W. Sokalski, P. Kafarski, 2001 .

Non-empirical analysis of the nature of the inhibitor–active-site interactions in leucine aminopeptidase

J. Grembecka, W. Sokalski, P. Kȩdzierski, 1999 .

Leucine aminopeptidase as a target for inhibitor design.

J. Grembecka, P. Kafarski, 2001, Mini reviews in medicinal chemistry.

Exploring the Sn binding pockets in gingipains by newly developed inhibitors: structure-based design, chemistry, and activity.

J. Otlewski, J. Grembecka, J. Potempa, 2006, Journal of medicinal chemistry.

A phosphonamidate containing aromatic N-terminal amino group as inhibitor of leucine aminopeptidase-design, synthesis and stability.

J. Grembecka, P. Kafarski, A. Mucha, 2006, European journal of medicinal chemistry.

Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia.

Jolanta Grembecka, Thomas Hartley, J. Hess, 2012, Nature chemical biology.

Computer-aided design and activity prediction of leucine aminopeptidase inhibitors

J. Grembecka, W. A. Sokalski, P. Kafarski, 2000, J. Comput. Aided Mol. Des..

α‐Aminoalkylphosphonates as a Tool in Experimental Optimisation of P1 Side Chain Shape of Potential Inhibitors in S1 Pocket of Leucine‐ and Neutral Aminopeptidases.

J. Grembecka, P. Kafarski, M. Drąg, 2005 .

Plasmodium falciparum neutral aminopeptidases: new targets for anti-malarials.

J. Whisstock, J. Dalton, J. Grembecka, 2010, Trends in biochemical sciences.

Theoretical models of inhibitory activity for inhibitors of protein–protein interactions: targeting menin–mixed lineage leukemia with small molecules

T. Cierpicki, J. Grembecka, S. Kłossowski, 2017, MedChemComm.

Ab initio study of the physical nature of interactions between enzyme active site fragments in vacuo

J. Grembecka, W. Sokalski, P. Kȩdzierski, 2001 .

Hydrolysis of the Phosphonamidate Bond in Phosphono Dipeptide Analogues - The Influence of the Nature of the N-Terminal Functional Group

T. Cierpicki, J. Grembecka, P. Kafarski, 2003 .

Dysregulated hematopoiesis caused by mammary cancer is associated with epigenetic changes and hox gene expression in hematopoietic cells.

B. Nelson, T. Cierpicki, J. Grembecka, 2013, Cancer research.

Cytokine Induced Phenotypic and Epigenetic Signatures Are Key to Establishing Specific Macrophage Phenotypes

Katherine A. Gallagher, J. Westwick, T. Cierpicki, 2013, PloS one.

Structure-based discovery of a boronic acid bioisostere of combretastatin A-4.

J. Grembecka, J. Rieger, E. Hamel, 2005, Chemistry & biology.

MLL protects CpG clusters from methylation within the Hoxa9 gene, maintaining transcript expression

N. Zeleznik-Le, Z. Xia, M. Diaz, 2008, Proceedings of the National Academy of Sciences.

BMI1 regulates PRC1 architecture and activity through homo- and hetero-oligomerization

F. Gray, T. Cierpicki, J. Grembecka, 2016, Nature Communications.

A small-molecule inhibitor of the aberrant transcription factor CBFβ-SMMHC delays leukemia in mice

Yan Gao, Monica L. Guzman, Jolanta Grembecka, 2015, Science.

Targeting epigenetic protein-protein interactions with small-molecule inhibitors.

T. Cierpicki, J. Grembecka, B. Linhares, 2020, Future medicinal chemistry.

GAS41 Recognizes Diacetylated Histone H3 through a Bivalent Binding Mode.

T. Cierpicki, J. Grembecka, H. Cho, 2018, ACS chemical biology.

Structure of the MLL CXXC domain–DNA complex and its functional role in MLL-AF9 leukemia

N. Zeleznik-Le, D. Shultis, T. Cierpicki, 2010, Nature Structural &Molecular Biology.

Molecular Basis of the Mixed Lineage Leukemia-Menin Interaction

Jolanta Grembecka, Thomas Hartley, T. Cierpicki, 2010, The Journal of Biological Chemistry.

Development of potent dimeric inhibitors of GAS41 YEATS domain.

V. Keshamouni, T. Cierpicki, J. Grembecka, 2021, Cell chemical biology.

Increased slow dynamics defines ligandability of BTB domains

T. Cierpicki, J. Grembecka, Mariusz Jaremko, 2022, Nature Communications.

Genome-scale CRISPR-Cas9 screen of Wnt/β-catenin signaling identifies therapeutic targets for colorectal cancer

T. Cierpicki, J. Grembecka, Dakang Xu, 2021, Science Advances.

Small molecule inhibitors targeting Polycomb Repressive Complex 1 RING domain

P. González-Alonso, F. Gray, T. Cierpicki, 2021, Nature Chemical Biology.

EWS-FLI1 and Menin Converge to Regulate ATF4 Activity in Ewing Sarcoma

Z. Nwosu, T. Cierpicki, J. Grembecka, 2021, Molecular Cancer Research.

Menin regulates the serine biosynthetic pathway in Ewing sarcoma

Dafydd G. Thomas, Ho-Joon Lee, T. Cierpicki, 2018, The Journal of pathology.

Combinatorial treatment with menin and FLT3 inhibitors induces complete remission in AML models with activating FLT3 mutations.

T. Cierpicki, J. Grembecka, S. Kłossowski, 2020, Blood.

Complexity of Blocking Bivalent Protein-Protein Interactions: Development of a Highly Potent Inhibitor of the Menin-Mixed-Lineage Leukemia Interaction.

T. Cierpicki, J. Grembecka, S. Kłossowski, 2018, Journal of medicinal chemistry.

Pharmacologic inhibition of the Menin-MLL interaction blocks progression of MLL leukemia in vivo.

Bo Wen, Jolanta Grembecka, Hongzhi Miao, 2015, Cancer cell.

Challenges and opportunities in targeting the menin-MLL interaction.

Jolanta Grembecka, T. Cierpicki, J. Grembecka, 2014, Future medicinal chemistry.

Challenges and opportunities in targeting the

T. Cierpicki, J. Grembecka, 2014 .

Challenges and opportunities in targeting the menin-MLL interaction.

T. Cierpicki, J. Grembecka, 2014, Future medicinal chemistry.

The same site on the integrase-binding domain of lens epithelium-derived growth factor is a therapeutic target for MLL leukemia and HIV.

J. Hess, T. Cierpicki, J. Grembecka, 2014, Blood.

CEBPA-mutated leukemia is sensitive to genetic and pharmacological targeting of the MLL1 complex

J. Grembecka, P. Valent, F. Grebien, 2019, Leukemia.

Epigenetic regulation of IL‐12‐dependent T cell proliferation

Y. Dou, T. Cierpicki, J. Grembecka, 2015, Journal of leukocyte biology.

Allosteric inhibition of the protein-protein interaction between the leukemia-associated proteins Runx1 and CBFbeta.

Bruce R Donald, Jolanta Grembecka, Yali Kong, 2007, Chemistry & biology.

Crystal Structure of Menin Reveals Binding Site for Mixed Lineage Leukemia (MLL) Protein*

T. Cierpicki, J. Grembecka, M. Chruszcz, 2011, The Journal of Biological Chemistry.

Structural insights into inhibition of the bivalent menin-MLL interaction by small molecules in leukemia.

Maksymilian Chruszcz, Jolanta Grembecka, Thomas Hartley, 2012, Blood.

Structure of the Plasmodium falciparum M17 aminopeptidase and significance for the design of drugs targeting the neutral exopeptidases

Woldeamanuel A. Birru, J. Whisstock, J. Dalton, 2010, Proceedings of the National Academy of Sciences.

Mutant NPM1 Hijacks Transcriptional Hubs to Maintain Pathogenic Gene Programs in Acute Myeloid Leukemia

G. Pfeifer, T. Cierpicki, J. Grembecka, 2022, Cancer discovery.

Pharmacologic Inhibition of the Menin–MLL Interaction Leads to Transcriptional Repression of PEG10 and Blocks Hepatocellular Carcinoma

T. Cierpicki, J. Grembecka, S. Kłossowski, 2017, Molecular Cancer Therapeutics.

Covalent inhibition of NSD1 histone methyltransferase

A. Ferrando, M. Sulis, P. González-Alonso, 2020, Nature Chemical Biology.

Progress towards small molecule menin-mixed lineage leukemia (MLL) interaction inhibitors with in vivo utility.

C. Lindsley, T. Cierpicki, J. Grembecka, 2015, Bioorganic & medicinal chemistry letters.

Ash1l controls quiescence and self-renewal potential in hematopoietic stem cells.

S. Malek, Y. Dou, T. Cierpicki, 2015, The Journal of clinical investigation.

Ash 1 l controls quiescence and self-renewal potential in hematopoietic stem cells

S. Malek, Y. Dou, T. Cierpicki, 2015 .

Gastrin Induces Nuclear Export and Proteasome Degradation of Menin in Enteric Glial Cells.

M. Low, T. Giordano, N. Wright, 2017, Gastroenterology.

Small Molecule Inhibitor of CBFβ-RUNX Binding for RUNX Transcription Factor Driven Cancers

Mazhar Adli, J. A. Pulikkan, K. Janes, 2016, EBioMedicine.

Menin inhibitor MI-3454 induces remission in MLL1-rearranged and NPM1-mutated models of leukemia.

O. Abdel-Wahab, Y. Dou, T. Cierpicki, 2019, The Journal of clinical investigation.

Combinatorial treatment with menin and FLT3 inhibitors induces complete remission in AML with activating FLT3 mutations.

T. Cierpicki, J. Grembecka, S. Kłossowski, 2020, Blood.

A mutation in the S-switch region of the Runt domain alters the dynamics of an allosteric network responsible for CBFbeta regulation.

J. Bushweller, N. Speck, Zhe Li, 2006, Journal of molecular biology.

The binding of the PDZ tandem of syntenin to target proteins.

Jolanta Grembecka, Zygmunt S Derewenda, T. Cierpicki, 2006, Biochemistry.

Clinically Defined Mutations in MEN1 Alter Its Tumor-suppressive Function Through Increased Menin Turnover

T. Cierpicki, J. Merchant, J. Grembecka, 2022, bioRxiv.

2-Aminobenzothiazoles in anticancer drug design and discovery.

T. Cierpicki, J. Grembecka, Guang Huang, 2023, Bioorganic chemistry.

Characterization of the Plasmodium falciparum M17 Leucyl Aminopeptidase

A. Bell, J. Dalton, J. Grembecka, 2007, Journal of Biological Chemistry.

Property Focused Structure-Based Optimization of Small Molecule Inhibitors of the Protein-Protein Interaction between Menin and Mixed Lineage Leukemia (MLL).

T. Cierpicki, J. Grembecka, Ting Zhao, 2016, Journal of medicinal chemistry.

The same site on LEDGF IBD domain represents therapeutic target for MLL leukemia and HIV

J. Hess, T. Cierpicki, J. Grembecka, 2014 .

leukemia and HIV The same site on LEDGF IBD domain represents therapeutic target for MLL

T. Cierpicki, J. Grembecka, Marcelo J. Murai, 2014 .

Two Loops Undergoing Concerted Dynamics Regulate the Activity of the ASH1L Histone Methyltransferase.

T. Cierpicki, J. Grembecka, H. Cho, 2015, Biochemistry.

Structural basis for the inhibition of the essential Plasmodium falciparum M1 neutral aminopeptidase

J. Whisstock, J. Dalton, A. Buckle, 2009, Proceedings of the National Academy of Sciences.

Menin-MLL inhibitors block oncogenic transformation by MLL-fusion proteins in a fusion partner-independent manner

S. Malek, T. Cierpicki, J. Grembecka, 2016, Leukemia.

Abstract 3225: LEDGF IBD domain represents therapeutic target for MLL leukemia and HIV

J. Hess, T. Cierpicki, J. Grembecka, 2014 .

Combined MAPK Pathway and HDAC Inhibition Breaks Melanoma.

T. Cierpicki, J. Grembecka, D. Lombard, 2019, Cancer discovery.

Molecular Basis of Menin-MLL Interaction: Implication for Targeted Therapies in MLL Leukemias.

T. Cierpicki, J. Grembecka, Amalia M Belcher, 2009 .

Progress towards small molecule inhibitors of the Menin-Mixed Lineage Leukemia (MLL) interaction with in vivo utility

C. Lindsley, T. Cierpicki, J. Grembecka, 2015 .

Applications of oxetanes in drug discovery and medicinal chemistry.

T. Cierpicki, J. Grembecka, Guang Huang, 2023, European journal of medicinal chemistry.

Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity

Y. Dou, T. Cierpicki, J. Grembecka, 2021, Nature Communications.

Trithorax group genes in hematopoiesis

J. Grembecka, I. Maillard, Jennifer Chase, 2015, Oncotarget.

Molecular Basis of the Mixed Lineage Leukemia-Menin Interaction

T. Cierpicki, J. Grembecka, Amalia M Belcher, 2010, The Journal of Biological Chemistry.

From the Cover: Structural basis for the inhibition of the essential Plasmodium falciparum M1 neutral aminopeptidase

J. Whisstock, J. Dalton, A. Buckle, 2009 .

Distinct pathways affected by menin versus MLL1/MLL2 in MLL-rearranged acute myeloid leukemia.

M. Meyerson, J. Grembecka, A. Kranz, 2019, Experimental hematology.

Gastrin Induces Nuclear Export and Proteasome Degradation of Menin in Enteric Glial Cells.

M. Low, T. Giordano, N. Wright, 2017, Gastroenterology.

Characterization of the Plasmodium falciparum M17 Leucyl Aminopeptidase

A. Bell, J. Dalton, J. Grembecka, 2007, Journal of Biological Chemistry.

Thioamides in medicinal chemistry and as small molecule therapeutic agents.

T. Cierpicki, J. Grembecka, Guang Huang, 2024, European journal of medicinal chemistry.

Menin in complex with MI-3454

Y. Dou, T. Cierpicki, J. Grembecka, 2020 .

Combination of menin and kinase inhibitors as an effective treatment for leukemia with NUP98 translocations.

M. Sulis, J. Grembecka, H. Miao, 2024, Leukemia.

Drug-resistant menin variants retain high binding affinity and interactions with MLL1

J. Grembecka, Tomasz Cierpicki, Joshua Ray, 2024, The Journal of biological chemistry.