Publications

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2021

Lysine Demethylase 5A is Required for MYC Driven Transcription in Multiple Myeloma.

Ohguchi H, Park PMC, Wang T, Gryder BE, Ogiya D, Kurata K, Zhang X, Li D, Pei C, Masuda T, Johansson C, Wimalasena VK, Kim Y, Hino S, Usuki S, Kawano Y, Samur MK, Tai YT, Munshi NC, Matsuoka M, Ohtsuki S, Nakao M, Minami T, Lauberth S, Khan J, Oppermann U, Durbin AD, Anderson KC, Hideshima T, Qi J

Cancer Discov. 2(4):370-387. doi: 10.1158/2643-3230.BCD-20-0108

Publication date: July 15, 2021

PMID: 34258103

Controlling Intramolecular Interactions in the Design of Selective, High-Affinity Ligands for the CREBBP Bromodomain.

Brand M, Clayton J, Moroglu M, Schiedel M, Picaud S, Bluck JP, Skwarska A, Bolland H, Chan AKN, Laurin CMC, Scorah AR, See L, Rooney TPC, Andrews KH, Fedorov O, Perell G, Kalra P, Vinh KB, Cortopassi WA, Heitel P, Christensen KE, Cooper RI, Paton RS, Pomerantz WCK, Biggin PC, Hammond EM, Filippakopoulos P, Conway SJ

J Med Chem. doi: 10.1021/acs.jmedchem.1c00348

Publication date: July 13, 2021

PMID: 34255515

Histone and DNA binding ability studies of the NSD subfamily of PWWP domains.

Zhang M, Yang Y, Zhou M, Dong A, Yan X, Loppnau P, Min J, Liu Y

Biochem Biophys Res Commun. 569:199-206. doi: 10.1016/j.bbrc.2021.07.017

Publication date: July 13, 2021

PMID: 34271259

A Concerted Action of UBA5 C-Terminal Unstructured Regions Is Important for Transfer of Activated UFM1 to UFC1.

Wesch N, Löhr F, Rogova N, Dötsch V, Rogov VV

Int J Mol Sci. 22(14):. doi: 10.3390/ijms22147390

Publication date: July 9, 2021

PMID: 34299007

Integrated analysis of Shank1 PDZ interactions with C-terminal and internal binding motifs.

Ali M, McAuley MM, Lüchow S, Knapp S, Joerger AC, Ivarsson Y

Curr Res Struct Biol. 3:41-50. doi: 10.1016/j.crstbi.2021.01.001

Publication date: July 9, 2021

PMID: 34235485

Epitope-specific antibody responses differentiate COVID-19 outcomes and variants of concern.

Voss C, Esmail S, Liu X, Knauer MJ, Ackloo S, Kaneko T, Lowes L, Stogios P, Seitova A, Hutchinson A, Yusifov F, Skarina T, Evdokimova E, Loppnau P, Ghiabi P, Haijan T, Zhong S, Abdoh H, Hedley BD, Bhayana V, Martin CM, Slessarev M, Chin-Yee B, Fraser DD, Chin-Yee I, Li SS

JCI Insight. 6(13):. doi: 10.1172/jci.insight.148855

Publication date: July 8, 2021

PMID: 34081630

Opinion: Independent third-party entities as a model for validation of commercial antibodies.

Laflamme C, Edwards AM, Bandrowski AE, McPherson PS

N Biotechnol. 65:1-8. doi: 10.1016/j.nbt.2021.07.001

Publication date: July 7, 2021

PMID: 34246180

Addressing a Trapped High-Energy Water: Design and Synthesis of Highly Potent Pyrimidoindole-Based Glycogen Synthase Kinase-3β Inhibitors.

Andreev S, Pantsar T, Tesch R, Kahlke N, El-Gokha A, Ansideri F, Grätz L, Romasco J, Sita G, Geibel C, Lämmerhofer M, Tarozzi A, Knapp S, Laufer SA, Koch P

J Med Chem. doi: 10.1021/acs.jmedchem.0c02146

Publication date: July 2, 2021

PMID: 34213342

NEK5 activity regulates the mesenchymal and migratory phenotype in breast cancer cells.

Matossian MD, Elliott S, Van Hoang T, Burks HE, Wright MK, Alzoubi MS, Yan T, Chang T, Wathieu H, Windsor GO, Hartono AB, Lee S, Zuercher WJ, Drewry DH, Wells C, Kapadia N, Buechlein A, Fang F, Nephew KP, Collins-Burow BM, Burow ME

Breast Cancer Res Treat. doi: 10.1007/s10549-021-06295-4

Publication date: July 1, 2021

PMID: 34196902

Probing the SAM Binding Site of SARS-CoV-2 Nsp14 In Vitro Using SAM Competitive Inhibitors Guides Developing Selective Bisubstrate Inhibitors.

Devkota K, Schapira M, Perveen S, Khalili Yazdi A, Li F, Chau I, Ghiabi P, Hajian T, Loppnau P, Bolotokova A, Satchell KJF, Wang K, Li D, Liu J, Smil D, Luo M, Jin J, Fish PV, Brown PJ, Vedadi M

SLAS Discov. 24725552211026261. doi: 10.1177/24725552211026261

Publication date: July 1, 2021

PMID: 34192965

Conformational plasticity of the ULK3 kinase domain.

Mathea S, Salah E, Tallant C, Chatterjee D, Berger BT, Konietzny R, Müller-Knapp S, Kessler BM, Knapp S

Biochem J. doi: 10.1042/BCJ20210257

Publication date: June 30, 2021

PMID: 34190988

MYC protein interactors in gene transcription and cancer.

Lourenco C, Resetca D, Redel C, Lin P, MacDonald AS, Ciaccio R, Kenney TMG, Wei Y, Andrews DW, Sunnerhagen M, Arrowsmith CH, Raught B, Penn LZ

Nat Rev Cancer. doi: 10.1038/s41568-021-00367-9

Publication date: June 29, 2021

PMID: 34188192

Genetic Variability of the SARS-CoV-2 Pocketome.

Yazdani S, De Maio N, Ding Y, Shahani V, Goldman N, Schapira M

J Proteome Res. doi: 10.1021/acs.jproteome.1c00206

Publication date: June 28, 2021

PMID: 34180678

Bispecific repurposed medicines targeting the viral and immunological arms of COVID-19.

Redhead MA, Owen CD, Brewitz L, Collette AH, Lukacik P, Strain-Damerell C, Robinson SW, Collins PM, Schäfer P, Swindells M, Radoux CJ, Hopkins IN, Fearon D, Douangamath A, von Delft F, Malla TR, Vangeel L, Vercruysse T, Thibaut J, Leyssen P, Nguyen TT, Hull M, Tumber A, Hallett DJ, Schofield CJ, Stuart DI, Hopkins AL, Walsh MA

Sci Rep. 11(1):13208. doi: 10.1038/s41598-021-92416-4

Publication date: June 24, 2021

PMID: 34168183

Development of LM98, a Small-Molecule TEAD Inhibitor Derived from Flufenamic Acid.

Gagnon A, Mélin L, Abdullayev S, Fnaiche A, Vu V, Gonzalez Suarez N, Zeng H, Szewczyk M, Li F, Sinisterra G, Allali-Hassani A, Chau I, Dong A, Woo S, Annabi B, Halabelian L, LaPlante S, Vedadi M, Barsyte-Lovejoy D, Santhakumar V

ChemMedChem. doi: 10.1002/cmdc.202100432

Publication date: June 23, 2021

PMID: 34164919

An automatic pipeline for the design of irreversible derivatives identifies a potent SARS-CoV-2 Mpro inhibitor.

Zaidman D, Gehrtz P, Filep M, Fearon D, Gabizon R, Douangamath A, Prilusky J, Duberstein S, Cohen G, Owen CD, Resnick E, Strain-Damerell C, Lukacik P, Barr H, Walsh MA, von Delft F, London N

Cell Chem Biol. doi: 10.1016/j.chembiol.2021.05.018

Publication date: June 22, 2021

PMID: 34174194

Discovery of the SMYD3 Inhibitor BAY-6035 Using Thermal Shift Assay (TSA)-Based High-Throughput Screening.

Gradl S, Steuber H, Weiske J, Szewczyk MM, Schmees N, Siegel S, Stoeckigt D, Christ CD, Li F, Organ S, Abbey M, Kennedy S, Chau I, Trush V, Barsyte-Lovejoy D, Brown PJ, Vedadi M, Arrowsmith C, Husemann M, Badock V, Bauser M, Haegebarth A, Hartung IV, Stresemann C

SLAS Discov. 24725552211019409. doi: 10.1177/24725552211019409

Publication date: June 21, 2021

PMID: 34154424

Rapid and accurate agglutination-based testing for SARS-CoV-2 antibodies.

Esmail S, Knauer MJ, Abdoh H, Voss C, Chin-Yee B, Stogios P, Seitova A, Hutchinson A, Yusifov F, Skarina T, Evdokimova E, Ackloo S, Lowes L, Hedley BD, Bhayana V, Chin-Yee I, Li SS

Cell Rep Methods. 1(2):100011. doi: 10.1016/j.crmeth.2021.100011

Publication date: June 21, 2021

PMID: 34235498

The Structure-Based Design of SARS-CoV-2 nsp14 Methyltransferase Ligands Yields Nanomolar Inhibitors.

Otava T, Šála M, Li F, Fanfrlík J, Devkota K, Perveen S, Chau I, Pakarian P, Hobza P, Vedadi M, Boura E, Nencka R

ACS Infect Dis. doi: 10.1021/acsinfecdis.1c00131

Publication date: June 21, 2021

PMID: 34152728

The structural basis of fatty acid elongation by the ELOVL elongases.

Nie L, Pascoa TC, Pike ACW, Bushell SR, Quigley A, Ruda GF, Chu A, Cole V, Speedman D, Moreira T, Shrestha L, Mukhopadhyay SMM, Burgess-Brown NA, Love JD, Brennan PE, Carpenter EP

Nat Struct Mol Biol. 28(6):512-520. doi: 10.1038/s41594-021-00605-6

Publication date: June 13, 2021

PMID: 34117479

Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells.

Faudone G, Bischoff-Kont I, Rachor L, Willems S, Zhubi R, Kaiser A, Chaikuad A, Knapp S, Fürst R, Heering J, Merk D

J Med Chem. doi: 10.1021/acs.jmedchem.1c00733

Publication date: June 11, 2021

PMID: 34115934

Remodelin Is a Cryptic Assay Interference Chemotype That Does Not Inhibit NAT10-Dependent Cytidine Acetylation.

Shrimp JH, Jing Y, Gamage ST, Nelson KM, Han J, Bryson KM, Montgomery DC, Thomas JM, Nance KD, Sharma S, Fox SD, Andressen T, Sinclair WR, Wu H, Allali-Hassani A, Senisterra G, Vedadi M, Lafontaine D, Dahlin JL, Marmorstein R, Walters MA, Meier JL

ACS Med Chem Lett. 12(6):887-892. doi: 10.1021/acsmedchemlett.0c00193

Publication date: June 10, 2021

PMID: 34141066

Conformation and dynamics of the kinase domain drive subcellular location and activation of LRRK2.

Schmidt SH, Weng JH, Aoto PC, Boassa D, Mathea S, Silletti S, Hu J, Wallbott M, Komives EA, Knapp S, Herberg FW, Taylor SS

Proc Natl Acad Sci U S A. 118(23):. doi: 10.1073/pnas.2100844118

Publication date: June 8, 2021

PMID: 34088839

Human MettL3-MettL14 RNA adenine methyltransferase complex is active on double-stranded DNA containing lesions.

Yu D, Horton JR, Yang J, Hajian T, Vedadi M, Sagum CA, Bedford MT, Blumenthal RM, Zhang X, Cheng X

Nucleic Acids Res. doi: 10.1093/nar/gkab460

Publication date: June 4, 2021

PMID: 34086966

Structure-Based Design of Selective Salt-Inducible Kinase Inhibitors.

Tesch R, Rak M, Raab M, Berger LM, Kronenberger T, Joerger AC, Berger BT, Abdi I, Hanke T, Poso A, Strebhardt K, Sanhaji M, Knapp S

J Med Chem. doi: 10.1021/acs.jmedchem.0c02144

Publication date: June 4, 2021

PMID: 34086472

Controlling the Covalent Reactivity of a Kinase Inhibitor with Light.

Reynders M, Chaikuad A, Berger BT, Bauer K, Koch P, Laufer S, Knapp S, Trauner D

Angew Chem Int Ed Engl. doi: 10.1002/anie.202103767

Publication date: June 3, 2021

PMID: 34081840

Crowdsourced mapping of unexplored target space of kinase inhibitors.

Cichońska A, Ravikumar B, Allaway RJ, Wan F, Park S, Isayev O, Li S, Mason M, Lamb A, Tanoli Z, Jeon M, Kim S, Popova M, Capuzzi S, Zeng J, Dang K, Koytiger G, Kang J, Wells CI, Willson TM, Oprea TI, Schlessinger A, Drewry DH, Stolovitzky G, Wennerberg K, Guinney J, Aittokallio T

Nat Commun. 12(1):3307. doi: 10.1038/s41467-021-23165-1

Publication date: June 3, 2021

PMID: 34083538

Structure-Guided Development of Small-Molecule PRC2 Inhibitors Targeting EZH2-EED Interaction.

Du D, Xu D, Zhu L, Stazi G, Zwergel C, Liu Y, Luo Z, Li Y, Zhang Y, Zhu K, Ding Y, Liu J, Fan S, Zhao K, Zhang N, Kong X, Jiang H, Chen K, Zhao K, Valente S, Min J, Duan W, Luo C

J Med Chem. doi: 10.1021/acs.jmedchem.0c02261

Publication date: June 2, 2021

PMID: 34077206

Synthetic Opportunities and Challenges for Macrocyclic Kinase Inhibitors.

Amrhein JA, Knapp S, Hanke T

J Med Chem. doi: 10.1021/acs.jmedchem.1c00217

Publication date: June 2, 2021

PMID: 34076436

Achieving Efficient Fragment Screening at XChem Facility at Diamond Light Source.

Douangamath A, Powell A, Fearon D, Collins PM, Talon R, Krojer T, Skyner R, Brandao-Neto J, Dunnett L, Dias A, Aimon A, Pearce NM, Wild C, Gorrie-Stone T, von Delft F

J Vis Exp. doi: 10.3791/62414

Publication date: May 29, 2021

PMID: 34125095

BRD4 methylation by the methyltransferase SETD6 regulates selective transcription to control mRNA translation.

Vershinin Z, Feldman M, Werner T, Weil LE, Kublanovsky M, Abaev-Schneiderman E, Sklarz M, Lam EYN, Alasad K, Picaud S, Rotblat B, McAdam RA, Chalifa-Caspi V, Bantscheff M, Chapman T, Lewis HD, Filippakopoulos P, Dawson MA, Grandi P, Prinjha RK, Levy D

Sci Adv. 7(22):. doi: 10.1126/sciadv.abf5374

Publication date: May 28, 2021

PMID: 34039605

C81-evoked inhibition of the TNFR1-NFκB pathway during inflammatory processes for stabilization of the impaired vascular endothelial barrier for leukocytes.

Krishnathas GM, Strödke B, Mittmann L, Zech T, Berger LM, Reichel CA, Rösser S, Schmid T, Knapp S, Müller S, Bracher F, Fürst R, Bischoff-Kont I

FASEB J. 35(6):e21656. doi: 10.1096/fj.202100037R

Publication date: May 28, 2021

PMID: 34042211

Large-Scale Recombinant Production of the SARS-CoV-2 Proteome for High-Throughput and Structural Biology Applications.

Altincekic N, Korn SM, Qureshi NS, Dujardin M, Ninot-Pedrosa M, Abele R, Abi Saad MJ, Alfano C, Almeida FCL, Alshamleh I, de Amorim GC, Anderson TK, Anobom CD, Anorma C, Bains JK, Bax A, Blackledge M, Blechar J, Böckmann A, Brigandat L, Bula A, Bütikofer M, Camacho-Zarco AR, Carlomagno T, Caruso IP, Ceylan B, Chaikuad A, Chu F, Cole L, Crosby MG, de Jesus V, Dhamotharan K, Felli IC, Ferner J, Fleischmann Y, Fogeron ML, Fourkiotis NK, Fuks C, Fürtig B, Gallo A, Gande SL, Gerez JA, Ghosh D, Gomes-Neto F, Gorbatyuk O, Guseva S, Hacker C, Häfner S, Hao B, Hargittay B, Henzler-Wildman K, Hoch JC, Hohmann KF, Hutchison MT, Jaudzems K, Jović K, Kaderli J, Kalniņš G, Kaņepe I, Kirchdoerfer RN, Kirkpatrick J, Knapp S, Krishnathas R, Kutz F, Zur Lage S, Lambertz R, Lang A, Laurents D, Lecoq L, Linhard V, Löhr F, Malki A, Bessa LM, Martin RW, Matzel T, Maurin D, McNutt SW, Mebus-Antunes NC, Meier BH, Meiser N, Mompeán M, Monaca E, Montserret R, Mariño Perez L, Moser C, Muhle-Goll C, Neves-Martins TC, Ni X, Norton-Baker B, Pierattelli R, Pontoriero L, Pustovalova Y, Ohlenschläger O, Orts J, Da Poian AT, Pyper DJ, Richter C, Riek R, Rienstra CM, Robertson A, Pinheiro AS, Sabbatella R, Salvi N, Saxena K, Schulte L, Schiavina M, Schwalbe H, Silber M, Almeida MDS, Sprague-Piercy MA, Spyroulias GA, Sreeramulu S, Tants JN, Tārs K, Torres F, Töws S, Treviño MÁ, Trucks S, Tsika AC, Varga K, Wang Y, Weber ME, Weigand JE, Wiedemann C, Wirmer-Bartoschek J, Wirtz Martin MA, Zehnder J, Hengesbach M, Schlundt A

Front Mol Biosci. 8:653148. doi: 10.3389/fmolb.2021.653148

Publication date: May 28, 2021

PMID: 34041264

Exploring protein hotspots by optimized fragment pharmacophores.

Bajusz D, Wade WS, Satała G, Bojarski AJ, Ilaš J, Ebner J, Grebien F, Papp H, Jakab F, Douangamath A, Fearon D, von Delft F, Schuller M, Ahel I, Wakefield A, Vajda S, Gerencsér J, Pallai P, Keserű GM

Nat Commun. 12(1):3201. doi: 10.1038/s41467-021-23443-y

Publication date: May 27, 2021

PMID: 34045440

Allosteric Antagonist Modulation of TRPV2 by Piperlongumine Impairs Glioblastoma Progression.

Conde J, Pumroy RA, Baker C, Rodrigues T, Guerreiro A, Sousa BB, Marques MC, de Almeida BP, Lee S, Leites EP, Picard D, Samanta A, Vaz SH, Sieglitz F, Langini M, Remke M, Roque R, Weiss T, Weller M, Liu Y, Han S, Corzana F, Morais VA, Faria CC, Carvalho T, Filippakopoulos P, Snijder B, Barbosa-Morais NL, Moiseenkova-Bell VY, Bernardes GJL

ACS Cent Sci. 7(5):868-881. doi: 10.1021/acscentsci.1c00070

Publication date: May 26, 2021

PMID: 34079902

Phospho-regulation, nucleotide binding and ion access control in potassium-chloride cotransporters.

Chi G, Ebenhoch R, Man H, Tang H, Tremblay LE, Reggiano G, Qiu X, Bohstedt T, Liko I, Almeida FG, Garneau AP, Wang D, McKinley G, Moreau CP, Bountra KD, Abrusci P, Mukhopadhyay SMM, Fernandez-Cid A, Slimani S, Lavoie JL, Burgess-Brown NA, Tehan B, DiMaio F, Jazayeri A, Isenring P, Robinson CV, Dürr KL

EMBO J. e107294. doi: 10.15252/embj.2020107294

Publication date: May 25, 2021

PMID: 34031912

Identifying and Validating MYC:Protein Interactors in Pursuit of Novel Anti-MYC Therapies.

Resetca D, MacDonald AS, Kenney TMG, Wei Y, Arrowsmith CH, Raught B, Penn LZ

Methods Mol Biol. 2318:45-67. doi: 10.1007/978-1-0716-1476-1_4

Publication date: May 22, 2021

PMID: 34019286

Editorial: Structural Studies of Protein Complexes in Signaling Pathways.

Prischi F, Filippakopoulos P

Front Mol Biosci. 8:641932. doi: 10.3389/fmolb.2021.641932

Publication date: May 18, 2021

PMID: 33996897

Design, Synthesis, and Evaluation of WD-Repeat-Containing Protein 5 (WDR5) Degraders.

Dölle A, Adhikari B, Krämer A, Weckesser J, Berner N, Berger LM, Diebold M, Szewczyk MM, Barsyte-Lovejoy D, Arrowsmith CH, Gebel J, Löhr F, Dötsch V, Eilers M, Heinzlmeir S, Kuster B, Sotriffer C, Wolf E, Knapp S

J Med Chem. doi: 10.1021/acs.jmedchem.1c00146

Publication date: May 13, 2021

PMID: 33980013

Endogenous vitamin E metabolites mediate allosteric PPARγ activation with unprecedented co-regulatory interactions.

Willems S, Gellrich L, Chaikuad A, Kluge S, Werz O, Heering J, Knapp S, Lorkowski S, Schubert-Zsilavecz M, Merk D

Cell Chem Biol. doi: 10.1016/j.chembiol.2021.04.019

Publication date: May 12, 2021

PMID: 33989565

Exploiting vulnerabilities of SWI/SNF chromatin remodelling complexes for cancer therapy.

Wanior M, Krämer A, Knapp S, Joerger AC

Oncogene. doi: 10.1038/s41388-021-01781-x

Publication date: May 3, 2021

PMID: 33941852

Reprogramming Transcription Factors Oct4 and Sox2 Induce a BRD-Dependent Immunosuppressive Transcriptome in GBM-Propagating Cells.

Ma T, Hu C, Lal B, Zhou W, Ma Y, Ying M, Prinos P, Quiñones-Hinojosa A, Lim M, Laterra J, Li Y

Cancer Res. 81(9):2457-2469. doi: 10.1158/0008-5472.CAN-20-2489

Publication date: May 1, 2021

PMID: 33574085

Hepatitis B virus resistance to tenofovir: fact or fiction? A systematic literature review and structural analysis of drug resistance mechanisms.

Mokaya J, McNaughton AL, Bester PA, Goedhals D, Barnes E, Marsden BD, Matthews PC

Wellcome Open Res. 5:151. doi: 10.12688/wellcomeopenres.15992.1

Publication date: April 20, 2021

PMID: 33869791

A High-Throughput Radioactivity-Based Assay for Screening SARS-CoV-2 nsp10-nsp16 Complex.

Khalili Yazdi A, Li F, Devkota K, Perveen S, Ghiabi P, Hajian T, Bolotokova A, Vedadi M

SLAS Discov. 24725552211008863. doi: 10.1177/24725552211008863

Publication date: April 19, 2021

PMID: 33874769

Fragment binding to the Nsp3 macrodomain of SARS-CoV-2 identified through crystallographic screening and computational docking.

Schuller M, Correy GJ, Gahbauer S, Fearon D, Wu T, Díaz RE, Young ID, Carvalho Martins L, Smith DH, Schulze-Gahmen U, Owens TW, Deshpande I, Merz GE, Thwin AC, Biel JT, Peters JK, Moritz M, Herrera N, Kratochvil HT, Aimon A, Bennett JM, Brandao Neto J, Cohen AE, Dias A, Douangamath A, Dunnett L, Fedorov O, Ferla MP, Fuchs MR, Gorrie-Stone TJ, Holton JM, Johnson MG, Krojer T, Meigs G, Powell AJ, Rack JGM, Rangel VL, Russi S, Skyner RE, Smith CA, Soares AS, Wierman JL, Zhu K, O'Brien P, Jura N, Ashworth A, Irwin JJ, Thompson MC, Gestwicki JE, von Delft F, Shoichet BK, Fraser JS, Ahel I

Sci Adv. 7(16):. doi: 10.1126/sciadv.abf8711

Publication date: April 16, 2021

PMID: 33853786

Structural Insights into Plasticity and Discovery of Remdesivir Metabolite GS-441524 Binding in SARS-CoV-2 Macrodomain.

Ni X, Schröder M, Olieric V, Sharpe ME, Hernandez-Olmos V, Proschak E, Merk D, Knapp S, Chaikuad A

ACS Med Chem Lett. 12(4):603-609. doi: 10.1021/acsmedchemlett.0c00684

Publication date: April 8, 2021

PMID: 33850605

Structures of chromatin modulators in complex with nucleosome.

Min J, Liu K

Curr Opin Chem Biol. 63:105-114. doi: 10.1016/j.cbpa.2021.02.018

Publication date: April 3, 2021

PMID: 33823458

Oxaprozin Analogues as Selective RXR Agonists with Superior Properties and Pharmacokinetics.

Schierle S, Chaikuad A, Lillich FF, Ni X, Woltersdorf S, Schallmayer E, Renelt B, Ronchetti R, Knapp S, Proschak E, Merk D

J Med Chem. doi: 10.1021/acs.jmedchem.1c00235

Publication date: April 1, 2021

PMID: 33793232

Application of a small molecule inhibitor screen approach to identify CXCR4 downstream signaling pathways that promote a mesenchymal and fulvestrant-resistant phenotype in breast cancer cells.

Matossian MD, Elliott S, Rhodes LV, Martin EC, Hoang VT, Burks HE, Zuercher WJ, Drewry DH, Collins-Burow BM, Burow ME

Oncol Lett. 21(5):380. doi: 10.3892/ol.2021.12641

Publication date: March 30, 2021

PMID: 33777204

Genotoxicity and Epigenotoxicity of Carbazole-Derived Molecules on MCF-7 Breast Cancer Cells.

Luparello C, Cruciata I, Joerger AC, Ocasio CA, Jones R, Tareque RK, Bagley MC, Spencer J, Walker M, Austin C, Ferrara T, D Oca P, Bellina R, Branni R, Caradonna F

Int J Mol Sci. 22(7):. doi: 10.3390/ijms22073410

Publication date: March 26, 2021

PMID: 33810274

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