Discovery of KT-474a Potent, Selective, and Orally Bioavailable IRAK4 Degrader for the Treatment of Autoimmune Diseases.

Authors: Zheng, Xiaozhang, Ji, Nan, Campbell, Veronica, Slavin, Anthony, Zhu, Xiao, Chen, Dapeng, Rong, Haojing, Enerson, Brad, Mayo, Michele, Sharma, Kirti, Browne, Chris M., Klaus, Christine R., Li, Haoran, Massa, Ginny, McDonald, Alice A., Shi, Yatao, Sintchak, Mike, Skouras, Stephanie, Walther, Dirk M., Yuan, Karen

Source: Journal of Medicinal Chemistry; 10/24/2024, Vol. 67 Issue 20, p18022-18037, 16p

Leveraging Quantitative Systems Pharmacology Approach into Development of Human Recombinant Follistatin Fusion Protein for Duchenne Muscular Dystrophy

Authors: Nguyen, Hoa Q., Iskenderian, Andrea, Ehmann, David, Jasper, Paul, Zhang, Zhiwei, Rong, Haojing, Welty, Devin, Narayanan, Rangaraj

Source: CPT: pharmacometrics & systems pharmacology. 9(6):342-352

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100108412193.0x000001&indx=1&recIds=ETOCvdc_100108412193.0x000001

Discovery of KT-413, a Targeted Protein Degrader of IRAK4 and IMiD Substrates Targeting MYD88 Mutant Diffuse Large B‑Cell Lymphoma.

Authors: Weiss, Matthew M., Zheng, Xiaozhang, Ji, Nan, Browne, Chris M., Campbell, Veronica, Chen, Dapeng, Enerson, Brad, Fei, Xue, Huang, Xin, Klaus, Christine R., Li, Haoran, Mayo, Michele, McDonald, Alice A., Paul, Atanu, Rong, Haojing, Sharma, Kirti, Shi, Yatao, Slavin, Anthony, Walther, Dirk M., Yuan, Karen

Source: Journal of Medicinal Chemistry; 7/11/2024, Vol. 67 Issue 13, p10548-10566, 19p

Quantitative Translational Analysis of Brain Kynurenic Acid Modulation via Irreversible Kynurenine Aminotransferase II Inhibition

Authors: Chang, Cheng ^{1, *}, Fonseca, Kari R. ¹, Li, Cheryl, Horner, Weldon, Zawadzke, Laura E., Salafia, Michelle A., Welch, Kathryn A., Strick, Christine A., Campbell, Brian M., Gernhardt, Steve S., Rong, Haojing, Sawant-Basak, Aarti, Liras, Jennifer, Dounay, Amy, Tuttle, Jamison B., Verhoest, Patrick, Maurer, Tristan S.

Source: In Molecular Pharmacology August 2018 94(2):823-833

Protein Engineering on Human Recombinant Follistatin: Enhancing Pharmacokinetic Characteristics for Therapeutic Application

Authors: Shen, Chuan, Iskenderian, Andrea, Lundberg, Dianna, He, Tao, Palmieri, Kathleen, Crooker, Robert, Deng, Qingwei, Traylor, Matthew, Gu, Sheng, Rong, Haojing, Ehmann, David, Pescatore, Brian, Strack-Logue, Bettina, Romashko, Alla, Baviello, George, Gill, John, Zhang, Bohong, Meiyappan, Muthuraman, Pan, Clark, Norton, Angela W. ^*

Source: In The Journal of Pharmacology and Experimental Therapeutics August 2018 366(2):291-302

Prediction of pharmacokinetics and pharmacodynamics in human for IRAK4 targeted protein degrader

Authors: Chen, Dapeng, Rong, Haojing, Mayo, Michele, McDonald, Alice, Campbell, Veronica, Zheng, Xiaozhang, Agarwal, Sagar, Weiss, Matt, Slavin, Anthony

Source: In Drug Metabolism and Pharmacokinetics April 2024 55 Supplement

Myostatin and activin blockade by engineered follistatin results in hypertrophy and improves dystrophic pathology in mdx mouse more than myostatin blockade alone

Authors: Iskenderian, Andrea, Liu, Nan, Deng, Qingwei, Huang, Yan, Shen, Chuan, Palmieri, Kathleen, Crooker, Robert, Lundberg, Dianna, Kastrapeli, Niksa, Pescatore, Brian, Romashko, Alla, Dumas, John, Comeau, Robert, Norton, Angela, Pan, Jing, Rong, Haojing, Derakhchan, Katayoun, Ehmann, David

Source: Skeletal muscle. 8(1):1-16

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Development of Guanfacine Extended-Release Dosing Strategies in Children and Adolescents with ADHD Using a Physiologically Based Pharmacokinetic Model to Predict Drug–Drug Interactions with Moderate CYP3A4 Inhibitors or Inducers

Authors: Li, Aiqun, Yeo, Karen, Welty, Devin, Rong, Haojing

Source: Paediatric drugs. 20(2):181-194

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100130221736.0x000001&indx=1&recIds=ETOCvdc_100130221736.0x000001

Discovery of a novel Kv7 channel opener as a treatment for epilepsy

Authors: Davoren, Jennifer E., Claffey, Michelle M., Snow, Sheri L., Reese, Matthew R., Arora, Gaurav, Butler, Christopher R., Boscoe, Brian P., Chenard, Lois, DeNinno, Shari L., Drozda, Susan E., Duplantier, Allen J., Moine, Ludivine, Rogers, Bruce N., Rong, SuoBao, Schuyten, Katherine, Wright, Ann S., Zhang, Lei, Serpa, Kevin A., Weber, Mark L., Stolyar, Polina, Whisman, Tammy L., Baker, Karen, Tse, Karen, Clark, Alan J., Rong, Haojing, Mather, Robert J., Lowe, John A.

Source: Bioorganic & medicinal chemistry letters. 25(21):4941-4944

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100064270633.0x000001&indx=1&recIds=ETOCvdc_100064270633.0x000001

490c – C1Inh: A Novel Therapeutic Target to Treat Biliary Atresia and Liver Fibrosis

Authors: Navabi, Nazanin, Gutta, Sridevi, Mourya, Reena, Holmes, Kevin, Iskenderian, Andrea, Islam, Rizwana, Rong, Haojing, Norton, Angela, Sypek, Joseph, Shivakumar, Pranavkumar

Source: Gastroenterology. 156(6):S-1507-S-1507

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100080954887.0x000001&indx=1&recIds=ETOCvdc_100080954887.0x000001

IRAK4 degrader in hidradenitis suppurativa and atopic dermatitis: a phase 1 trial

Authors: Ackerman, Lindsay, Acloque, Gerard, Bacchelli, Sandro, Schwartz, Howard, Feinstein, Brian J., La Stella, Phillip, Alavi, Afsaneh, Gollerkeri, Ashwin, Davis, Jeffrey, Campbell, Veronica, McDonald, Alice, Agarwal, Sagar, Karnik, Rahul, Shi, Kelvin, Mishkin, Aimee, Culbertson, Jennifer, Klaus, Christine, Enerson, Bradley, Massa, Virginia, Kuhn, Eric, Sharma, Kirti, Keaney, Erin, Barnes, Randy, Chen, Dapeng, Zheng, Xiaozhang, Rong, Haojing, Sabesan, Vijay, Ho, Chris, Mainolfi, Nello, Slavin, Anthony, Gollob, Jared A.

Source: Nature Medicine; 20230101, Issue: Preprints p1-10, 10p

Targeted Delivery of Small Interfering RNA (siRNA) to Proximal Tubule Cells in the Kidneys

Authors: Ding, Shiying, Long, Kimberly R., Cunniff, Jeremy, Lucas, Johnny, Rong, Haojing, Belanger, Adam, Zhang, Hongmei, Lawrence, Jonathan F., Rbaibi, Youssef, Weisz, Ora A., Sehgal, Alfica

Source: Journal of the American Society of Nephrology; October 2024, Vol. 35 Issue: 10, Number 10 Supplement 10

8-Prenylnaringenin, the phytoestrogen in hops and beer, upregulates the function of the E-cadherin/catenin complex in human mammary carcinoma cells

Authors: Rong, Haojing, Boterberg, Tom, Maubach, Julie, Stove, Christophe, Depypere, Herman, Van Slambrouck, Séverine, Serreyn, Rudolphe, De Keukeleire, Denis, Mareel, Marc, Bracke, Marc

Source: In European Journal of Cell Biology 2001 80(9):580-585

A First-in-Class STAT3 Degrader KT-333 in Development for Treatment of Hematologic Cancers

Authors: Liu, Phillip CC, Dixit, Vaishali, Mayo, Michele, Dey, Joyoti, Yuan, Karen, Karnik, Rahul, Walther, Dirk, Shi, Yatao, Sharma, Kirti, Rong, Haojing, Yang, Bin, Gollerkeri, Ashwin, Gollob, Jared, DeSavi, Chris

Source: In Blood 23 November 2021 138 Supplement 1:1865-1865

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Mechanisms of the Anti-Tumor Activity of STAT3 Degraders in Lymphoma

Authors: Rong, Haojing ^*, Sharma, Kirti ^*, Csibi, Fred ^*, Yang, Bin ^*, Rusin, Scott ^*, Shi, Yatao ^*, Dey, Joyoti ^*, Karnik, Rahul ^*, Mayo, Michele ^*, Yuan, Karen ^*, Chutake, Yogesh ^*, McDonald, Alice ^*, Zhu, Sean ^*, Ji, Nan ^*, Liu, Phillip ^*, Li, Henry ^*, Walker, Duncan, Gollob, Jared ^*, Mainolfi, Nello ^*, Desavi, Chris ^*

Source: In Blood 5 November 2020 136 Supplement 1:42-42

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Small Molecule-Induced, Selective STAT3 Degradation Leads to Anti-Tumor Activity in STAT3-Dependent Heme Malignancies

Authors: Csibi, Fred ^*, Ji, Nan ^*, Yang, Bin ^*, Yuan, Karen ^*, Mayo, Michele ^*, Rong, Haojing ^*, Rusin, Scott ^*, Sharma, Kirti ^*, Loh, Christine ^*, Li, Henry ^*, Townson, Sharon ^*, Chen, Jesse ^*, Kamadurai, Hari ^*, Walker, Duncan, Gollob, Jared ^*, Mainolfi, Nello ^*

Source: In Blood 13 November 2019 134 Supplement 1:3803-3803